Page last updated: 2024-11-08

linezolid

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Cross-References

ID SourceID
PubMed CID441401
CHEMBL ID126
CHEBI ID63607
SCHEMBL ID5027
MeSH IDM0257529

Synonyms (134)

Synonym
BIDD:GT0404
HY-10394
AB00639994-08
n-(((s)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide
c16h20fn3o4
zyvoxa
zyvoxid
acetamide, n-((3-(3-fluoro-4-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)-, (s)-
acetamide, n-(((5s)-3-(3-fluoro-4-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)-
u 100766
hsdb 7478
pnu 100766
zyvoxam
n-((3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide
linezolid & vrc3375
MLS001424075
C08146
165800-03-3
LINEZOLID ,
pnu-100766
zyvox
nda 21-132 zyvox oral suspension (linzolid oral suspension)
nda 21-130 zyvox (linezolid tablets)
(s)-n-[[3-(3-fluoro-4-morpholinylphenyl)-2-oxo-5-oxazolidinyl]methyl]acetamide
nda 21-131 zyvox for injection (linezolid injection)
u-100766
n-[[(5s)-3-(3-fluoro-4-morpholino-phenyl)-2-oxo-oxazolidin-5-yl]methyl]acetamide
MLS000759444
smr000466335
cpd000466335
DB00601
D00947
linezolid (jan/usan/inn)
zyvox (tn)
NCGC00164628-01
ZLD ,
n-{[(5s)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide
HMS2089K06
HMS2051F08
CHEMBL126 ,
u-100,766
chebi:63607 ,
111GE017 ,
benzotriazol-2-yl-acetonitrile
(s)-n-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide
n-[(r)-3-(3-fluoro-4-morpholin-4-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide
n-((s)-2-oxo-3-(s)-2,3,3a,4-tetrahydro-1h-benzo[b]pyrrolo[1,2-d][1,4]oxazin-7-yl-oxazolidin-5-ylmethyl)-acetamide
(s)-3-(3-fluoro-4-morpholin-4-yl-phenyl)-5-[(1-hydroxy-ethylamino)-methyl]-oxazolidin-2-one
n-[(s)-3-(3-fluoro-4-morpholin-4-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide
n-[3-(3-fluoro-4-morpholin-4-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide(linezolid)
(linezolid)n-[3-(3-fluoro-4-morpholin-4-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide
(s)-n-((3-fluoro-4-morpholinophenyl)-2-oxaoxazolidin-5-yl)methyl)acetamide
bdbm50116067
linezoid
cid_441401
n-[3-(3-fluoro-4-morpholin-4-yl-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-acetamide
n-[[(5s)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
A810662
n-[[(5s)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide
n-[[(5s)-3-(3-fluoranyl-4-morpholin-4-yl-phenyl)-2-oxidanylidene-1,3-oxazolidin-5-yl]methyl]ethanamide
HMS3260C14
linezolide
dtxcid3026489
dtxsid5046489 ,
tox21_112246
cas-165800-03-3
CCG-101009
linezolid [usan:inn:ban]
isq9i6j12j ,
zivoxid
unii-isq9i6j12j
BCP9000855
NCGC00263531-03
n-({(5s)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide
linezolid [hsdb]
n-[[(s)-3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazolidinyl]methyl]acetamide
linezolid [usp-rs]
linezolid [usp monograph]
linezolid [inn]
linezolid [mart.]
linezolid [jan]
linezolid [usan]
linezolid [vandf]
linezolid [who-dd]
linezolid [orange book]
linezolid [mi]
AM84567
CS-0756
S1408
KS-1178
AKOS016340522
AB00639994-06
NC00259
SCHEMBL5027
AB00639994-09
tox21_500096
NCGC00260781-01
(s)-n-((3-(3-fluoro-4-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl)methyl)acetamide
(s)-n-[ [3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-oxazolidin-5-yl]methyl]-acetamide
(s)-n-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide
Q-201308
linezolid, pharmaceutical secondary standard; certified reference material
acetamide, n-[[(5s)-3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-
AB00639994_11
AB00639994_10
n-{[(5s)-3-[3-fluoro-4-(morpholin-4-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide
pnu100766
SR-01000759376-5
sr-01000759376
SR-01000759376-4
linezolid, united states pharmacopeia (usp) reference standard
linezolid, >=98% (hplc)
NCGC00263531-10
HMS3713K10
linezolid (pnu-100766)
SW197639-3
BCP05586
Q411377
linezolid (zyvox)
gtpl10827
NCGC00263531-05
SR-01000759376-11
linezolid 100 microg/ml in acetonitrile
HB4443
L0362
Z1515385084
n-(((5s)-3-(3-fluoro-4-(morpholin-4-yl)phenyl)-2-oxo-1,3-oxazolidin-5-yl)methyl)acetamide
linezolid (usp-rs)
n-(((5s)-3-(3-fluoro-4-(4-morpholinyl)phenyl)-2-oxo-5-oxazolidinyl)acetamide
linezolidum
linezolid in sodium chloride 0.9% in plastic container
j01xx08
linezolid (mart.)
linezolid (usp monograph)

Research Excerpts

Overview

Linezolid is a critically important antibiotic used to treat human infections caused by MRSA and VRE. It is an oxazolidinone antibacterial drug, and its therapeutic drug monitoring and individualized treatment have been challenged since its approval.

ExcerptReferenceRelevance
"Linezolid is an oxazolidinone antimicrobial regarded as a "last resort" antimicrobial, used typically for treatment of Gram-positive bacterial infections. "( Prevalence of linezolid-resistant organisms among patients admitted to a tertiary hospital for critical care or dialysis.
Brennan, G; Dembicka, KM; Dunne, CP; Hennessy, N; O'Connell, NH; Powell, J, 2022
)
2.52
"Linezolid is a critically important antibiotic used to treat human infections caused by MRSA and VRE. "( Large diversity of linezolid-resistant isolates discovered in food-producing animals through linezolid selective monitoring in Belgium in 2019.
Argudín, MA; Bogaerts, B; Boland, C; De Keersmaecker, SCJ; Denis, O; Deplano, A; Fretin, D; Hallin, M; Kowalewicz, C; Roosens, NHC; Simon, G; Timmermans, M; Vanneste, K; Wattiau, P, 2021
)
2.39
"Linezolid is an antimicrobial with broad activity against Gram-positive bacteria. "( Linezolid induced thrombocytopenia in critically ill patients: Risk factors and development of a machine learning-based prediction model.
Alaguero-Calero, M; Álvarez-Asteinza, C; Fernández, J; Maray, I; Rodríguez-Ferreras, A; Valledor, P, 2022
)
3.61
"Linezolid is an oral antibiotic which is widely used for serious infections caused by Methicillin Resistant Staphylococcus aureus (MRSA). "( First study on detection of cryptic resistance to linezolid among clinical isolates of methicillin resistant Staphylococcus aureus from India.
Agarwal, AN; Gupta, A; Gupta, K; Kaur, IR; Rai, S; Saha, R; Singh, NP; Tayal, A,
)
1.83
"Linezolid is a good choice for treatment of SIAI."( Linezolid in the treatment of severe intraabdominal infection: A STROBE-compliant retrospective study.
Liu, Y; Su, Y; Sun, X; Wang, J; You, D; Zheng, Y, 2022
)
2.89
"Linezolid is an oxazolidinone antibacterial drug, and its therapeutic drug monitoring and individualized treatment have been challenged since its approval. "( Expert consensus statement on therapeutic drug monitoring and individualization of linezolid.
Cai, X; Cao, H; Chen, C; Chen, M; Chen, Z; Dai, H; Dai, Y; Fang, L; Fang, Q; Federico, P; He, L; Hu, Y; Ji, Y; Jiang, S; Li, L; Li, X; Lin, B; Lin, G; Lin, Q; Lu, X; Lv, S; Miao, J; Shi, C; Wang, C; Xu, P; Xu, Q; Xu, T; Xu, Y; Ying, Y; Yu, X; Zhan, H; Zhang, C; Zhang, Y; Zhou, M; Zhu, J; Zhu, Y; Zhu, Z, 2022
)
2.39
"Linezolid is an alternative first-line agent for MRSA pneumonia. "( Evaluating linezolid dose regimens against methicillin-resistant Staphylococcus aureus based on renal function in populations with different body weight.
Chen, J; Sun, Y; Wang, N; Xu, G; Yang, W; Zhao, M; Zhao, X; Zhu, L; Zuo, M, 2022
)
2.55
"Linezolid is a promising alternative adjunctive agent to which US GAS isolates remain near-universally susceptible, with a similar mechanism of action and similar in vitro evidence of GAS virulence factor attenuation."( Should Linezolid Replace Clindamycin as the Adjunctive Antimicrobial of Choice in Group A Streptococcal Necrotizing Soft Tissue Infection and Toxic Shock Syndrome? A Focused Debate.
Cortés-Penfield, N; Ryder, JH, 2023
)
2.09
"Linezolid is a synthetic oxazolidinone antimicrobial drug with a broad spectrum and a unique mechanism of inhibiting resistant pathogenic strains, and it was approved by the Food and Drug Administration (FDA) in April 2000. "( A case of linezolid-induced SIADH in elderly and a review of the literature.
Dong, QW; Ge, DD; Ma, CH; Sun, P; Tang, L; Zhao, YC; Zhou, TY, 2022
)
2.57
"Linezolid (LNZ) is a new-generation synthetic molecule for the antibacterial treatment of severe infections, particularly in infective cases where the bacterial resistance to first-choice drugs is caused by Gram-positive pathogens. "( Linezolid@MOF-74 as a host-guest system with antimicrobial activity.
Aguila-Rosas, J; Guzmán, A; Ibarra, IA; Lara-García, HA; Lima, E; Quirino-Barreda, CT; Ramos, D; Santiago-Tellez, A, 2022
)
3.61
"Linezolid (LZD) is an effective drug in treating multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis. "( Linezolid-related adverse effects in the treatment of rifampicin resistant tuberculosis: a retrospective study.
Chen, G; Cui, D; Hu, X; Shi, L; Wang, D, 2023
)
3.8
"Linezolid is a valuable therapeutic option for infections of the central nervous system caused by multi-drug resistant Gram-positive pathogens. "( Population Pharmacokinetics and Dosing Regimen Optimization of Linezolid in Cerebrospinal Fluid and Plasma of Post-operative Neurosurgical Patients.
Cao, P; Dong, H; Li, S; Meng, L; Wang, Y; Zhu, Y, 2023
)
2.59
"Linezolid is an effective, but toxic anti-tuberculosis drug that is currently recommended for the treatment of drug-resistant tuberculosis. "( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
2.35
"Linezolid is an antibiotic used to treat infectious diseases caused by vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. "( Complete genome sequence of cfr(B)-carrying Enterococcus raffinosus isolated from bile in a patient in Japan.
Hisatsune, J; Ishida-Kuroki, K; Kashiyama, S; Kawada-Matsuo, M; Komatsuzawa, H; Le, MN; Masuda, K; Ohge, H; Segawa, T; Sugai, M; Sugawara, Y; Tadera, K; Yokozaki, M, 2023
)
2.35
"Linezolid is an oxazolidin commonly related to the development of hematological toxicity, being renal clearance the major factor involved in the drug clearance. "( Influence of augmented renal clearance on the lower incidence of linezolid-related hematological toxicity.
Caro-Teller, JM; Ferrari-Piquero, JM; Gonzalez-Barrios, I; Hernández-Ramos, JA; Rodríguez-Quesada, PP; Sánchez-Sanz, B,
)
1.81
"Linezolid is an effective medication for treating drug-resistant infections; however, it may result in optic neuropathy. "( Linezolid optic neuropathy.
Cao, AA; Lee, MS; McClelland, CM; Miller, HV, 2023
)
3.8
"Linezolid is an oxazolidin commonly related to the development of haematological toxicity, being renal clearance the major factor involved in the drug clearance. "( [Translated article] Influence of augmented renal clearance in the lower incidence of linezolid-related haematological toxicity.
Caro-Teller, JM; Ferrari-Piquero, JM; González-Barrios, I; Hernández-Ramos, JA; Rodríguez-Quesada, PP; Sánchez-Sanz, B,
)
1.8
"Linezolid is an oral oxazolidine used to treat methicillin-resistant Staphylococcus aureus infections."( A Rare Skin Rash: Linezolid-Induced Purpuric Drug Eruption without Vasculitis in a Puerto Rican Man.
Cruz-Díaz, CN; Engel-Rodriguez, N; Rivera-Bobé, N; Tirú-Vega, MA, 2023
)
1.97
"Linezolid is an important therapeutic option for the treatment of infections caused by VRE. "( Phenotypic and genotypic characterization of linezolid-resistant Enterococcus faecium from the USA and Pakistan.
Andleeb, S; Burnham, CD; D'Souza, AW; Dantas, G; Hussain, T; Potter, RF; Wallace, MA; Wardenburg, KE, 2019
)
2.22
"Linezolid is an oxazolidinone antibiotic that effectively treats methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). "( Effects of a rifampicin pre-treatment on linezolid pharmacokinetics.
Ogami, C; Okazaki, F; Seto, Y; To, H; Tsuji, Y; Yamamoto, Y, 2019
)
2.22
"Linezolid is an antibiotic used to treat infections caused by drug-resistant gram-positive organisms, including vancomycin-resistant Enterococcus faecium, multi-drug resistant Streptococcus pneumoniae, and methicillin-resistant Staphylococcus aureus. "( Therapeutic Drug Monitoring Can Improve Linezolid Dosing Regimens in Current Clinical Practice: A Review of Linezolid Pharmacokinetics and Pharmacodynamics.
Alffenaar, JW; Cattaneo, D; Konicki, R; Marriott, DJE; Neely, M; Rao, GG, 2020
)
2.27
"Linezolid is an alternative treatment option for infections with multidrug-resistant Gram-positive bacteria including vancomycin-resistant enterococci. "( Validating a screening agar for linezolid-resistant enterococci.
Bender, JK; Fleige, C; Klare, I; Weber, RE; Werner, G, 2019
)
2.24
"Linezolid is a synthetic oxazolidinone antibiotic frequently used to treat vancomycin-resistant enterococcal infections. "( Risk factors and outcome associated with the acquisition of linezolid-resistant Enterococcus faecalis.
Bocanegra-Ibarias, P; Esparza-Ahumada, S; Flores-Treviño, S; Garza-Gonzalez, E; González-Díaz, E; Hernández-Morfin, N; León-Garnica, G; Mendoza-Mujica, C; Morfín-Otero, R; Pérez-Gómez, HR; Rodríguez-Noriega, E, 2020
)
2.24
"Linezolid is a synthetic antimicrobial agent with a broad spectrum of activity against virtually all Gram-positive bacteria. "( Risk factors for linezolid-associated thrombocytopenia and negative effect of carbapenem combination.
Ataman Hatipoğlu, Ç; Bulut, C; Kaya Kılıç, E; Kınıklı, S; Ozel, Ö; Sönmezer, MÇ; Tülek, N; Tuncer Ertem, G, 2019
)
2.3
"Linezolid is an appropriate choice for these patients when coverage of positive bacteria is needed."( Linezolid is safe on platelet count for AML patients during myelosuppression after consolidation chemotherapy.
Shi, T; Xie, W; Yang, X; Ye, X; Zhao, S; Zhu, J; Zhu, L, 2020
)
2.72
"Linezolid is an antibiotic used to treat infections caused by multi-drug-resistant Gram-positive bacteria. "( Hospital outbreak of linezolid-resistant and vancomycin-resistant ST80 Enterococcus faecium harbouring an optrA-encoding conjugative plasmid investigated by whole-genome sequencing.
Brennan, GI; Coleman, DC; Corcoran, S; Cullen, A; Egan, SA; Fitzpatrick, M; Hoyne, A; McCormack, O; McDermott, H; O'Connell, B, 2020
)
2.32
"Linezolid (LZD) is a potent antibiotic for drug-resistant Gram-positive infections and is an effective treatment for TB."( Evaluation of IL-1 Blockade as an Adjunct to Linezolid Therapy for Tuberculosis in Mice and Macaques.
Ameel, CL; Borish, HJ; Causgrove, CM; Dartois, V; Flynn, JL; Klein, EC; Lin, PL; Maiello, P; Mishra, BB; Nelson, SJ; Phuah, JY; Saqib, M; Sassetti, CM; Stein, B; White, AG; Winchell, CG; Zimmerman, MD, 2020
)
1.54
"Linezolid is an oxazolidinone antimicrobial agent often used to treat multidrug-resistant Gram-positive bacterial infections. "( The first case of teeth discoloration induced by linezolid in children in China Mainland.
Leng, B; Lu, C; Wang, J; Xu, P; Zhang, W; Zhang, Y; Zou, D, 2020
)
2.26
"Linezolid is a synthetic antibiotic which is active against most Gram-positive bacteria, especially on Staphylococcus aureus. "( Staphylococcal meningitis therapy with linezolid in a young infant: efficacy, CSF levels and side effects.
Amante, PG; Auriti, C; Bersani, I; Cairoli, S; Goffredo, BM; Longo, D; Piersigilli, F, 2020
)
2.27
"Linezolid is an antibiotic increasingly used for treatment of resistant Gram-positive infections, which blocks bacterial proteosythesis through direct inhibition of mitochondrial ribosomes. "( Severe linezolid-induced lactic acidosis in a child with acute lymphoblastic leukemia: A case report.
Ludikova, B; Novak, Z; Pospisilova, D; Rohanova, M; Smolka, V; Volejnikova, J; Zapalka, M, 2020
)
2.46
"Linezolid is an oxazolidinone class antibiotic used for treatment infections caused by various multidrug-resistant gram-positive pathogens including enterococci. "( Characteristics of linezolid-resistant Enterococcus faecalis isolates from broiler breeder farms.
Ha, JS; Kim, YB; Lee, YJ; Noh, EB; Seo, KW; Yoon, S, 2020
)
2.33
"Linezolid is a monoamine oxidase inhibitor that may increase the risk of serotonin syndrome in patients receiving combination selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs). "( Incidence of Serotonin Syndrome With Combined Use of Linezolid and Serotonin Reuptake Inhibitors Compared With Linezolid Monotherapy.
Ernst, EJ; Karkow, DC; Kauer, JF, 2017
)
2.15
"Linezolid is an antibiotic of oxazolidinones family that inhibits proteical synthesis. "( [Myelosupression induced by linezolid: a pediatric case].
Alarcón Alacio, MT; Ballesteros García, MDM; Díaz Velázquez, E; Galán Del Río, P; Orós Milián, ME, 2017
)
2.19
"Linezolid (LZD) serves as an effective option in the treatment of Mycobacterium abscessus complex (MABC) infection. "( In vitro activity between linezolid and other antimicrobial agents against Mycobacterium abscessus complex.
Lu, J; Pang, Y; Song, Y; Zhang, Z, 2018
)
2.22
"Linezolid is an oxazolidinone antibiotic commonly used to treat serious infections caused by vancomycin-resistant enterococcus. "( Whole transcriptome analysis reveals potential novel mechanisms of low-level linezolid resistance in Enterococcus faecalis.
Hua, R; Wu, W; Xia, Y; Yan, J; Yang, M, 2018
)
2.15
"Linezolid is a potent antibiotic against resistant Gram-positive microorganisms that has been associated with mild hyponatremia, yet with a mechanism different from SIADH."( A case of severe hyponatremia due to linezolid-induced SIADH.
Ioannou, P; Mavrikaki, V; Panagiotakis, S; Papakitsou, I; Stavroulaki, M, 2018
)
1.48
"Linezolid is an oxazolidinone antibiotic used in the treatment of infections caused by a range of Gram-positive pathogens."( Manuka honey and methylglyoxal increase the sensitivity of Staphylococcus aureus to linezolid.
Gardner, SL; Hayes, G; Telzrow, CL; Vigueira, PA; Wommack, AJ; Wright, N, 2018
)
1.43
"Linezolid is a widely used antibiotic with broad-spectrum action. "( LINEZOLID-INDUCED MITOCHONDRIAL TOXICITY PRESENTING AS RETINAL NERVE FIBER LAYER MICROCYSTS AND OPTIC AND PERIPHERAL NEUROPATHY IN A PATIENT WITH CHRONIC GRANULOMATOUS DISEASE.
Agarwal, A; Aggarwal, K; Arora, A; Gupta, A; Gupta, V; Jindal, AK; Krishnan, G; Pilania, RK; Singh, S; Suri, D, 2021
)
3.51
"Linezolid is a bacteriostatic antibiotic of the Oxazolidinone class; it works by inhibiting the initiation of protein synthesis on bacterial ribosomes. "( Linezolid-induced pancytopenia.
Allan, A; Carter, P; Hackett, J; Leader, R, 2018
)
3.37
"Linezolid is a useful drug for treating drug-resistant tuberculosis. "( Is Severe and Long-lasting Linezolid-induced Optic Neuropathy Reversible?
Kang, BH; Lee, S; Roh, MS; Ryu, WY; Son, C; Um, SJ, 2018
)
2.22
"Linezolid is a synthetic antibiotic very effective in the treatment of infections caused by Gram-positive pathogens. "( Population Pharmacokinetics and Dosing Optimization of Linezolid in Pediatric Patients.
Li, SC; Wang, Y; Xu, H; Ye, Q; Zhang, L, 2019
)
2.2
"Linezolid is a synthetic antimicrobial agent belonging to the oxazolidinone class. "( A critical review of HPLC-based analytical methods for quantification of Linezolid.
Fernandes, GFDS; Salgado, HRN; Santos, JLD, 2020
)
2.23
"Linezolid is a reversible inhibitor of mitochondrial function in various cell types."( Prolonged inhibition and incomplete recovery of mitochondrial function in oxazolidinone-treated megakaryoblastic cell lines.
Constantinescu, SN; Milosevic, TV; Payen, VL; Sonveaux, P; Tulkens, PM; Van Bambeke, F; Vertenoeil, G, 2019
)
1.24
"Linezolid is an oxazolidinone group of antibiotic with activity against Gram-positive bacteria."( Linezolid Resistance in Staphylococcus haemolyticus - Case Series and Review of Literature.
Chander, J; Gulati, N; Gupta, R; Gupta, V; Sharma, S; Soni, A, 2020
)
2.72
"Linezolid is an antibiotic with time-dependent activity, and both the percentage of time that plasma concentrations exceed the MIC and the area under the concentration-time curve over 24 h in the steady state divided by the MIC (AUC24/MIC ratio) are associated with clinical response. "( Risk factors for a low linezolid trough plasma concentration in acute infections.
Brunet, M; Casals, G; Cobos, N; Cuesta, M; Hernandez, C; Martínez, JA; Mensa, J; Morata, L; Rodriguez, S; Rojas, JF; Soriano, A, 2013
)
2.14
"Linezolid is an effective antimicrobial agent to treat methicillin-resistant Staphylococcus aureus (MRSA). "( Low prevalence of Cfr-mediated linezolid resistance among methicillin-resistant Staphylococcus aureus in a Spanish hospital: case report on linezolid resistance acquired during linezolid therapy.
Camoez, M; Domínguez, MA; Gasch, O; Martin, R; Pujol, M; Sierra, JM; Tubau, F, 2013
)
2.12
"Linezolid is an oxazolidinone antibiotic used for the treatment of pneumonia and uncomplicated and complicated skin and soft tissues infections caused by Gram positive bacteria. "( Development and validation of a new UPLC-PDA method to quantify linezolid in plasma and in dried plasma spots.
Ariaudo, A; Baietto, L; Corcione, S; Cusato, J; D'Avolio, A; De Rosa, FG; Di Perri, G; Ranieri, VM; Simiele, M; Urbino, R, 2013
)
2.07
"Linezolid is a synthetic oxazolidinone broad spectrum antibiotic and has been in off label use for multidrug resistant tuberculosis (MDR-TB). "( Optic neuropathy secondary to Linezolid for multidrug-resistant mycobacterial spinal tuberculosis.
Addison, P; Agrawal, R; Pavesio, C; Pefkianaki, M; Saihan, Z, 2015
)
2.15
"Linezolid (LNZ) is a promising antimicrobial agent for the treatment of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB). "( Beijing genotype of Mycobacterium tuberculosis is significantly associated with linezolid resistance in multidrug-resistant and extensively drug-resistant tuberculosis in China.
Liu, C; Pang, Y; Wang, Y; Zhang, Z; Zhao, Y, 2014
)
2.07
"Linezolid is an appropriate initial therapy for severe infections in patients with acute renal dysfunction, but monitoring of platelet counts is essential after initiation of therapy."( Impact of vancomycin or linezolid therapy on development of renal dysfunction and thrombocytopenia in Japanese patients.
Fujii, S; Kunimoto, Y; Makino, S; Miyamoto, A; Nakata, H; Noda, N; Sakurai, K; Takahashi, S, 2013
)
1.42
"Linezolid is an antimicrobial agent for the treatment of multiresistant Gram-positive infections. "( The emergence of linezolid resistance among Enterococci in intestinal microbiota of treated patients is unrelated to individual pharmacokinetic characteristics.
Alavoine, L; Andremont, A; Bourgeois-Nicolaos, N; Defrance, G; Doucet-Populaire, F; Duval, X; Lefort, A; Massias, L; Mentré, F; Nguyen, TT; Noel, V; Senneville, E, 2014
)
2.18
"Linezolid is an alternative, however it is only recommended for up to 4 weeks treatment due to risk of hematological side effects."( [Vancomycin resistant Staphylococcus epidermidis caused prosthesis infection. Linezolid and rifampicin healed the complicated infection].
Fröding, I; Håkanson, A; Ottosson, C, 2014
)
1.35
"Linezolid is an oxazolidinone antibacterial agent, with activity against Gram-positive bacteria. "( Efficacy and safety of linezolid for the treatment of infections in children: a meta-analysis.
Apostolidou-Kiouti, F; Haidich, AB; Ioannidou, M; Niopas, I; Roilides, E, 2014
)
2.16
"Linezolid is an antimicrobial drug frequently used in critically ill patients."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
1.48
"Linezolid is a valuable treatment option for central nervous system (CNS) infections caused by multidrug-resistant Gram-positive micro-organisms. "( Plasma and cerebrospinal fluid concentrations of linezolid in neurosurgical critically ill patients with proven or suspected central nervous system infections.
Alvarez-Lerma, F; Basas, M; Campillo, N; Ferrández, O; Grau, S; Horcajada, JP; Lipman, J; Luque, S; Roberts, JA, 2014
)
2.1
"Linezolid is a member of the oxazolidinone antibiotic family which can be used in serious infections caused by vancomycin resistant E."( Cataract in a preterm newborn: a possible side effect of linezolid therapy.
AydÊn, B; Beken, S; Dilli, D; Ilarslan, E; Kabatas, EU; Okumus, N; Zenciroglu, A, 2014
)
1.37
"Linezolid is an effective drug against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). "( Detection of the classical G2576U mutation in linezolid resistant Staphylococcus aureus along with isolation of linezolid resistant Enterococcus faecium from a patient on short-term linezolid therapy: first report from India.
Hada, V; Kaur, IR; Kaur, T; Niranjan, DK; Rai, S; Singh, NP,
)
1.83
"Linezolid is an antimicrobial agent for the treatment of multiresistant Gram-positive infections. "( A simple high-performance liquid chromatography for the determination of linezolid in human plasma and saliva.
Hara, S; Jimi, S; Matsumoto, T; Takamatsu, Y; Takata, T; Togawa, A; Uchiyama, M; Yoshinari, M, 2015
)
2.09
"Linezolid seems to be a better choice than vancomycin for the treatment of MRSA ventilator-associated pneumonia. "( What is the best therapeutic approach to methicillin-resistant Staphylococcus aureus pneumonia?
Peyrani, P; Ramirez, J, 2015
)
1.86
"Linezolid (LZD) is an oxazolidinone antibiotic that is active against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci. "( The association between risk factors and time of onset for thrombocytopenia in Japanese patients receiving linezolid therapy: a retrospective analysis.
Hayashi, H; Ichie, T; Matsuda, M; Sugiura, Y; Sugiyama, T; Suzuki, D; Takahashi, H; Yasui, K, 2015
)
2.07
"Linezolid is an effective antibiotic reagent for Gram-positive bacterial infection; its most common side effect is thrombocytopenia. "( High frequency of thrombocytopenia in patients with acute-on-chronic liver failure treated with linezolid.
Li, JZ; Li, LJ; Lu, YF; Xie, ZY; Xu, LC; Yu, W; Zhang, YM; Zhou, N, 2015
)
2.08
"Linezolid is a broad spectrum antibiotic known for its unique mechanism of inhibition of resistant pathogenic strains."( Linezolid Induced Adverse Drug Reactions - An Update.
Dhasmana, N; Kamble, SS; Kishor, K; Sahu, RK, 2015
)
2.58
"Linezolid is an oxazolidinone with potent activity against Mycobacterium tuberculosis. "( Preclinical Evaluations To Identify Optimal Linezolid Regimens for Tuberculosis Therapy.
Adams, JR; Baluya, DL; Brown, AN; Brown, DL; Drusano, GL; Hafner, R; Jambunathan, K; Kwara, A; Louie, A; Mirsalis, JC; Rodriquez, JL, 2015
)
2.12
"Linezolid is an oxazolidinone that is licensed for human use and has demonstrated potent activity against multidrug-resistant M."( Preclinical Evaluations To Identify Optimal Linezolid Regimens for Tuberculosis Therapy.
Adams, JR; Baluya, DL; Brown, AN; Brown, DL; Drusano, GL; Hafner, R; Jambunathan, K; Kwara, A; Louie, A; Mirsalis, JC; Rodriquez, JL, 2015
)
1.4
"Linezolid is an effective antibiotic against most gram-positive bacteria including drug-resistant strains such as methicillin-resistant Staphylococcus aureus. "( Successful treatment of methicillin-resistant Staphylococcus aureus osteomyelitis with combination therapy using linezolid and rifampicin under therapeutic drug monitoring.
Ashizawa, N; Gejo, R; Higashi, Y; Kawago, K; Kimura, T; Narukawa, M; Nogami, M; Tashiro, M; Tsuji, Y; Yamamoto, Y, 2016
)
2.09
"Linezolid serves as an important component for the treatment of drug-resistant tuberculosis although there is little published data about linezolid use in children, especially in childhood tuberculous meningitis (TBM)."( Linezolid is Associated with Improved Early Outcomes of Childhood Tuberculous Meningitis.
Li, H; Liu, J; Lu, J; Ni, X; Zhao, S; Zhao, Y, 2016
)
3.32
"Linezolid is an oxazolidinone antibiotic active against Gram-positive bacteria, and is most commonly used to treat life-threatening infections in critically ill patients. "( Pharmacokinetics of linezolid in critically ill patients.
Dimitrijevic, A; Jankovic, SM; Kostic, M; Sazdanovic, P; Stefanovic, S, 2016
)
2.2
"Linezolid is a valuable treatment option for treating infections caused by multi-resistant gram-positive pathogens. "( Decreased Linezolid Serum Concentrations in Three Critically Ill Patients: Clinical Case Studies of a Potential Drug Interaction between Linezolid and Rifampicin.
Blassmann, U; Briegel, J; Frey, OR; Huge, V; Koeberer, A; Roehr, AC; Vetter-Kerkhoff, C, 2016
)
2.28
"Linezolid is a new drug with potent activity on Gram-positive pathogens such as MRSA."( EFFECT OF LINEZOLID ALONE AND IN COMBINATION WITH OTHER ANTIBIOTICS, ON METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS.
Azmy, M; Badawy, M; El Said, M; Gohar, H; Madany, N; Mansy, S; Yehia, H, 2016
)
1.56
"Linezolid is an oxazolidinone with potent activity against M tuberculosis, and improves culture conversion and cure rates when added to treatment regimens for drug resistant tuberculosis. "( Linezolid in the treatment of drug-resistant tuberculosis: the challenge of its narrow therapeutic index.
Maartens, G; Meintjes, G; Wasserman, S, 2016
)
3.32
"Linezolid (LZD) is an antimicrobial that is commonly used for treatment of vancomycin-resistant Enterococci and methicillin-resistant Staphylococcus aureus infections. "( Linezolid-Induced Thrombocytopenia Is Caused by Suppression of Platelet Production via Phosphorylation of Myosin Light Chain 2.
Hirosawa, I; Kato, Y; Matsumoto, J; Nishi, Y; Suzuki, M; Tajima, M; Takashio, Y; Yamada, H; Yamamoto, M, 2016
)
3.32
"Linezolid is an oxazolidinone antibiotic against Gram-positive bacteria. "( A Retrospective Analysis of Risk Factors for Linezolid-Associated Hyponatremia in Japanese Patients.
Hashinaga, K; Hiramatsu, K; Itoh, H; Iwao, M; Kadota, JI; Sato, Y; Suzuki, Y; Takumi, Y; Tanaka, R, 2016
)
2.14
"Linezolid is an oxazolidinone antibiotic with activity against gram-positive organisms, particularly methicillin-resistant Staphylococcus aureus (MRSA). "( Two cases of serious rhabdomyolysis during linezolid treatment.
Hoppe, U; Kern, JM; Lechner, AM; Past, E; Porsche, U; Pretsch, I, 2017
)
2.16
"Linezolid (1) is an oxazolidinone antibiotic that is partially metabolized in vivo via ring cleavage of its morpholine moiety to mainly form two metabolites, PNU-142300 (2) and PNU-142586 (3). "( Synthesis of Linezolid Metabolites PNU-142300 and PNU-142586 toward the Exploration of Metabolite-Related Events.
Hanaya, K; Kizu, J; Matsumoto, K; Shoji, M; Sugai, T; Yokoyama, Y, 2017
)
2.27
"Linezolid is an interesting therapeutic alternative in case of infections due to multi-resistant bacteria and/or complex clinical situations."( Proper use of antibiotics: situation of linezolid at the intensive care unit of the Tunisian Military Hospital.
Afif, N; Ali, YM; Mehdi, D; Safa, L; Zied, H, 2016
)
1.42
"Linezolid is an oxazolidinone, a new class of antibacterial with a unique mechanism of action, namely inhibition of the formation of a functional 70S initiation complex in the 50S bacterial ribosomal subunit. "( Benefit-risk assessment of linezolid for serious gram-positive bacterial infections.
Falagas, ME; Vardakas, KZ, 2008
)
2.09
"Linezolid is an effective and well-tolerated antibiotic for the treatment of infections caused by Gram-positive pathogens. "( [Sideroblastic anemia after prolonged linezolid therapy].
Ishida, A; Kakimoto, T; Kurai, H; Miura, R; Nakazato, T; Sagara, Y; Yamashita, D, 2008
)
2.06
"Linezolid is a popular choice of antibiotic, especially for the treatment of orthopedic-related MRSA infections."( Serotonin toxicity as a consequence of linezolid use in revision hip arthroplasty.
Carpenter, EC; Mason, LW; Randhawa, KS, 2008
)
1.34
"Linezolid is a member of a novel class of antibiotics, with resistance already being reported. "( Genome sequencing of linezolid-resistant Streptococcus pneumoniae mutants reveals novel mechanisms of resistance.
Dewar, K; Feng, J; Gingras, H; Légaré, D; Lupien, A; Ouellette, M; Wasserscheid, J, 2009
)
2.11
"Linezolid is a representative of a new antibiotic class, i.e."( [Case report: severe thrombocytopenia].
Knüttgen, D; Sakka, SG; Schürmann, A; Wappler, F, 2009
)
1.07
"Linezolid is an antibiotic used to treat highly resistant infections, including vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. "( Bacteremia caused by an Enterococcus faecalis isolate with high-level linezolid resistance in a teenager with Crohn's disease.
Jhaveri, R; Lopez Marti, MG, 2009
)
2.03
"Linezolid (LZD) is a new antibacterial agent with potent antibacterial activity against MRSA."( Efficacy of linezolid against Panton-Valentine leukocidin (PVL)-positive meticillin-resistant Staphylococcus aureus (MRSA) in a mouse model of haematogenous pulmonary infection.
Araki, N; Izumikawa, K; Kakeya, H; Kamihira, S; Kihara, R; Kohno, S; Morinaga, Y; Seki, M; Tsukamoto, K; Yamada, Y; Yamamoto, Y; Yanagihara, K, 2009
)
1.45
"Linezolid is a recent addition to the antibiotic armamentarium against Gram-positive bacteria, including multiresistant staphylococci and enterococci. "( Linezolid-associated acute interstitial nephritis and drug rash with eosinophilia and systemic symptoms (DRESS) syndrome.
Agharazii, M; Desmeules, S; Riopel, J; Savard, S, 2009
)
3.24
"Linezolid is an oxazolidinone approved for the treatment of vancomycin-resistant Enterococcus faecium infections, complicated skin and soft tissue infections, and nosocomial pneumonia caused by various Gram-positive species including methicillin-resistant Staphylococcus aureus (MRSA)."( Zyvox Annual Appraisal of Potency and Spectrum program: linezolid surveillance program results for 2008.
Bell, JM; Fumiaki, I; Jones, RN; Kobayashi, I; Ross, JE; Turnidge, JD; Utsuki, U, 2009
)
1.32
"Linezolid is an oxazolidinone antibiotic agent active against Gram-positive bacteria. "( Retrospective cohort chart review study of factors associated with the development of thrombocytopenia in adult Japanese patients who received intravenous linezolid therapy.
Fukao, A; Goto, C; Itoh, Y; Kasahara, S; Matsuura, K; Murakami, N; Niwa, T; Sakakibara, S; Suzuki, A; Yasuda, M, 2009
)
1.99
"Linezolid is a new antibiotic with activity against Mycobacterium tuberculosis in vitro and in animal studies. "( Linezolid in the treatment of multidrug-resistant tuberculosis.
Flood, J; Mase, S; Raftery, A; Schecter, GF; Scott, C; True, L, 2010
)
3.25
"Linezolid is an option for the treatment of infections caused by multiresistant Gram-positive bacteria. "( Pharmacokinetics of linezolid in septic patients with and without extended dialysis.
Haefeli, WE; Hempel, G; Hoppe-Tichy, T; Lichtenstern, C; Ober, MC; Saleh, S; Schwenger, V; Sonntag, HG; Swoboda, S; Weigand, MA, 2010
)
2.13
"Linezolid is an oxazolidinone antibiotic which has MAOI-like properties."( [Serotonin syndrome associated with linezolid use: a case report].
Erden Aki, SO; Sahiner, V, 2009
)
1.35
"Linezolid is a potential drug for the treatment of multidrug-resistant tuberculosis but its use is limited because of severe adverse effects such as anemia, thrombocytopenia, and peripheral neuropathy. "( Limited sampling strategies for therapeutic drug monitoring of linezolid in patients with multidrug-resistant tuberculosis.
Alffenaar, JW; Kosterink, JG; Proost, JH; Uges, DR; van Altena, R; van der Werf, TS, 2010
)
2.04
"Linezolid is an effective alternative to vancomycin for the treatment of cSSTI caused by MRSA."( Efficacy and safety of linezolid versus vancomycin for the treatment of complicated skin and soft-tissue infections proven to be caused by methicillin-resistant Staphylococcus aureus.
Baruch, AM; Bhattacharyya, H; Dryden, MS; Itani, KM; Kunkel, MJ; Weigelt, JA, 2010
)
2.11
"Linezolid is an alternative to conventional treatment of infections with gram positive cocci."( [Linezolid therapy for infectious endocarditis].
Arpi, M; Bruun, NE; Lauridsen, TK, 2010
)
1.99
"Linezolid is an important antibiotic against severe infections caused by multi-resistant bacterial pathogens."( Rapid and sensitive determination of the antibiotic linezolid in low plasma volumes by high-performance liquid chromatography.
Joukhadar, C; Mauric, O; Popovic, M; Traunmüller, F,
)
1.1
"Linezolid is a weak, reversible monoamine oxidase inhibitor. "( Dietary tyramine restriction for hospitalized patients on linezolid: an update.
Orfanos, A; Roth, M; Rumore, MM, 2010
)
2.05
"Linezolid is an antibiotic of the oxazolidinone class that has bacteriostatic and bactericidal activity against a broad range of Gram-positive bacteria, including multiresistant pathogens. "( Linezolid treatment of nosocomial bacterial infection with multiresistant Gram-positive pathogens in preterm infants: a systematic review.
Kocher, S; Müller, W; Resch, B, 2010
)
3.25
"Linezolid is a promising drug, but its use is limited by adverse effects with prolonged administration of 600 mg twice daily."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
1.32
"Linezolid is an oxazolidinone antibiotic with a large spectrum of action."( In vitro characterization of calcium phosphate biomaterial loaded with linezolid for osseous bone defect implantation.
Amador, G; Bouler, JM; Gautier, H; Merle, C; Plumecocq, A; Weiss, P, 2012
)
1.33
"Linezolid is an effective salvage agent for bone and joint infections. "( Compassionate use of linezolid for adult Taiwanese patients with bone and joint infections.
Chang, SC; Chen, CJ; Chen, TC; Chen, WC; Hwang, YC; Lu, PL; Wang, JT, 2010
)
2.12
"Linezolid is a safe and effective antibiotic used in hematological disease patients complicated with infections of gram positive coccus."( [Clinical analysis of 102 blood disease patients with gram positive cocci infection treated with Linezolid].
Fu, R; Guan, J; Liang, Y; Liu, H; Qu, W; Ruan, EB; Shao, ZH; Song, J; Wang, GJ; Wang, HQ; Wang, XM; Wu, YH; Xing, LM, 2010
)
2.02
"Linezolid is an effective antibiotic for treatment of infections caused by resistant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). "( Chronic liver disease increases the risk of linezolid-related thrombocytopenia in methicillin-resistant Staphylococcus aureus-infected patients after digestive surgery.
Aihara, T; Beppu, N; Iida, H; Ikuta, S; Kurimoto, A; Mitsunobu, M; Tanimura, K; Yamanaka, N; Yanagi, H; Yasui, C; Yoshie, H, 2011
)
2.07
"Linezolid is an antimicrobial agent to treat infections by Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). "( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
2.06
"Linezolid is an oxazolidinone antibiotic that has been associated with myelosuppression, including leukopenia and thrombocytopenia. "( Clinical experience of linezolid in bone marrow transplantation patients.
Coyle, E; Hachem, RY; Hogan, HL; Neuhauser, M; Raad, II, 2010
)
2.11
"Linezolid is a treatment option for methicillin-resistant Staphylococcus aureus (MRSA) infections in cystic fibrosis (CF) patients. "( Pharmacokinetics of intravenous and oral linezolid in adults with cystic fibrosis.
Keel, RA; Kloft, C; Knauft, RF; Kuti, JL; Muhlebach, M; Nicolau, DP; Pope, JS; Schaeftlein, A, 2011
)
2.08
"Linezolid is a bacteriostatic antibiotic with good cerebrospinal fluid penetration. "( Linezolid in the treatment of methicillin-resistant staphylococcal post-neurosurgical meningitis: a series of 17 cases.
Arda, B; Aydemir, S; Bardak, S; Dalbasti, T; Pullukcu, H; Ruksen, M; Sipahi, OR; Turhan, T; Ulusoy, S; Yurtseven, T; Zileli, M, 2011
)
3.25
"Linezolid plus rifampin is an alternative salvage therapy when the implant is not removed."( Linezolid plus rifampin as a salvage therapy in prosthetic joint infections treated without removing the implant.
Baños, V; Canovas, A; Canovas, E; Canteras, M; Clavel, M; García, E; Gómez, J; Hernández-Torres, A; Martínez, L; Martínez, P; Medina, M; Ruiz, J; Soriano, A, 2011
)
2.53
"Linezolid is an oxazolidinone antibiotic that inhibits the initiation of translation. "( Proteomic and transcriptomic analysis of linezolid resistance in Streptococcus pneumoniae.
Billal, DS; Feng, J; Légaré, D; Leprohon, P; Lupien, A; Ouellette, M; Racine, G; Winstall, E, 2011
)
2.08
"Linezolid is an oxazolidinone antibiotic that has been reported to induce lactic acidosis, especially after prolonged administration, through inhibition of the mitochondrially synthesised components of oxidative phosphorylation."( Rapid-onset, linezolid-induced lactic acidosis in MELAS.
Cope, TE; McFarland, R; Schaefer, A, 2011
)
1.46
"Linezolid is an effective, cheap and relatively safe drug for patients failing MDR-TB treatment, including those with confirmed XDR-TB."( Linezolid: an effective, safe and cheap drug for patients failing multidrug-resistant tuberculosis treatment in India.
Bali, RK; Behera, D; Caminero, JA; Gupta, S; Jaiswal, A; Singla, N; Singla, R, 2012
)
2.54
"Linezolid seems to be a possible therapeutic strategy in case of multiresistant bacteria and/or complex clinical situations. "( Good practice in antibiotic use: what about linezolid in a French university hospital?
Aubin, G; Caillon, J; Corvec, S; Lebland, C; Navas, D; Potel, G; Thomaré, P, 2011
)
2.07
"Linezolid is a protein synthesis inhibitor, while ciprofloxacin is not."( Differential effects of linezolid and ciprofloxacin on toxin production by Bacillus anthracis in an in vitro pharmacodynamic system.
Abshire, T; Brown, DL; Drusano, GL; Heine, HS; Holman, K; Kulawy, R; Liu, W; Louie, A; Vanscoy, BD, 2012
)
1.41
"Linezolid appears to be a safe and effective ALS, preventing CRBSI and prolonging the survival of the catheter in HD patients."( Linezolid versus vancomycin antibiotic lock solution for the prevention of nontunneled catheter-related blood stream infections in hemodialysis patients: a prospective randomized study.
Iatrou, C; Kouloubinis, A; Makriniotou, I; Revela, I; Samonis, G; Smirloglou, D; Sofroniadou, S; Zerbala, S, 2012
)
2.54
"Linezolid is a new antibiotic with activity against Mycobacterium tuberculosis in vitro and in vivo. "( Efficacy and safety of linezolid in the treatment of extensively drug-resistant tuberculosis.
Gu, J; Hao, XH; Liu, YD; Sun, H; Tangg, SJ; Xiao, HP; Yao, L; Zhang, Q; Zheng, LH, 2011
)
2.12
"Linezolid is an oxazolidinone antibiotic in clinical use for the treatment of serious infections of resistant Gram-positive bacteria. "( Resistance to linezolid caused by modifications at its binding site on the ribosome.
Long, KS; Vester, B, 2012
)
2.18
"Linezolid is an important therapeutic option for infections from multi-drug resistant Gram-positive pathogens. "( Immediate hematological toxicity of linezolid in healthy volunteers with different body weight: a phase I clinical trial.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Guo, D; Liang, B; Liu, Y; Vouloumanou, EK; Wang, R, 2012
)
2.1
"Linezolid is an oxazolidinone with an effect on Gram-positive cocci."( Linezolid as rescue treatment for left-sided infective endocarditis: an observational, retrospective, multicenter study.
Arpi, M; Bruun, LE; Bruun, NE; Bundgaard, H; Hassager, C; Johansen, HK; Lauridsen, TK; Moser, C; Rasmussen, RV; Risum, N, 2012
)
2.54
"Linezolid is a new drug from the oxazolidinone class of antibiotics used against mycobacteria and multi-drug resistant (MDR) Gram-positive bacterial infections, which may are also glycopeptide-resistant. "( Rapid and sensitive LC-MS/MS method for the analysis of antibiotic linezolid on dried blood spot.
Cassetta, MI; Chiappini, E; De Gaudio, M; de Martino, M; Fallani, S; Funghini, S; Galli, L; la Marca, G; Malvagia, S; Novelli, A; Ombrone, D; Villanelli, F,
)
1.81
"Linezolid is an effective treatment for patients with and without vascular disease who have a lower-extremity cSSSI caused by MRSA. "( Linezolid and vancomycin in treatment of lower-extremity complicated skin and skin structure infections caused by methicillin-resistant Staphylococcus aureus in patients with and without vascular disease.
Duane, TM; Huang, DB; Puzniak, LA; Weigelt, JA, 2012
)
3.26
"Linezolid is an attractive agent for SSI prophylaxis, particularly for the prevention of SSI due to MRSA."( Surgical site infection prophylaxis strategies for cardiothoracic surgery: a decision-analytic model.
Anderson, DJ; Devine, ST; Ford, KD; Kaye, KS, 2012
)
1.1
"Linezolid is a promising antimicrobial agent for the treatment of multidrug-resistant tuberculosis (MDR-TB), but its use is limited by toxicity. "( Dried blood spot analysis for therapeutic drug monitoring of linezolid in patients with multidrug-resistant tuberculosis.
Alffenaar, JW; Bolhuis, MS; Brouwers, JR; de Lange, WC; Greijdanus, B; Koster, RA; Uges, DR; van Altena, R; Vu, DH, 2012
)
2.06
"Linezolid which is an oxazolidinone and dalbavancin which is a second-generation, semi-synthetic lipoglycopeptid are important therapeutic options for infections caused by antimicrobial-resistant gram-positive pathogens."( [In vitro activity of linezolid and dalbavancin against vancomycin-resistant enterococci].
Aktaş, G; Bozdoğan, B; Derbentli, S, 2012
)
1.41
"Linezolid is an important agent for the treatment of infections because of vancomycin-resistant Enterococcus (VRE). "( Predictors and outcomes of linezolid-resistant vancomycin-resistant Enterococcus: a case-case-control study.
Bommarito, S; Chaudhry, A; Farhat, M; Hayakawa, K; Ho, K; Jagadeesh, KK; Kaye, KS; Lephart, PR; Marchaim, D; Martin, ET; Moshos, JA; Mroue, R; Nanjireddy, P; Obeid, T; Parveen, S; Pogue, JM; Rybak, MJ; Singla, M; Sunkara, B; Vadlamudi, G, 2012
)
2.12
"Linezolid is a reasonable alternative for patients with treatment failure while receiving vancomycin, isolates with vancomycin minimum inhibitory concentrations over 2 μg/mL, allergic reactions, or vancomycin-induced nephrotoxicity."( Pharmacotherapy for methicillin-resistant Staphylococcus aureus nosocomial pneumonia.
Church, TJ; Segarra-Newnham, M, 2012
)
1.1
"Linezolid is a novel oxazolidinone antibacterial agent with a broad clinical application, especially in methicillin-resistant Staphylococcus aureus skin and soft-tissue infections and skin and skin-structure infections. "( Cost-effectiveness of linezolid in methicillin-resistant Staphylococcus aureus skin and skin structure infections.
Bounthavong, M; Hsu, DI, 2012
)
2.14
"Linezolid (LZD) is an option for treating infections caused by multi-resistant Gram-positive bacteria. "( Pharmacokinetics and elimination efficiency of linezolid during dialysis.
Hiraike, M; Hiraki, Y; Kamimura, H; Karube, Y; Matsumoto, K; Misumi, N; Morita, K; Tsuji, Y, 2013
)
2.09
"Linezolid is a new oxazolidinone with activity against gram-positive cocci. "( In vivo pharmacodynamics of a new oxazolidinone (linezolid).
Andes, D; Craig, WA; Peng, J; van Ogtrop, ML, 2002
)
2.01
"Linezolid is a new oxazolidinone with potent antibacterial activity against Gram-positive cocci; it uniquely inhibits bacterial translation through inhibition of 70S initiation complex formation. "( Virulence factor expression by Gram-positive cocci exposed to subinhibitory concentrations of linezolid.
Ford, CW; Gemmell, CG, 2002
)
1.98
"Linezolid is an important therapeutic option for treatment of infections caused by glycopeptide- and beta-lactam-resistant gram-positive organisms. "( Linezolid resistance in Staphylococcus aureus: characterization and stability of resistant phenotype.
Eliopoulos, GM; Ferraro, MJ; Gold, HS; Moellering, RC; Pillai, SK; Sakoulas, G; Wennersten, C, 2002
)
3.2
"Linezolid is an oxazolidinone that has activity against most gram-positive bacteria, including in vitro activity against all Nocardia species and strains. "( Clinical experience with linezolid for the treatment of nocardia infection.
Apodaca, A; Birmingham, MC; Brown-Elliott, BA; Buescher, ES; Gimbel, JF; Moylett, EH; Pacheco, SE; Perry, TR; Rakita, RM; Schentag, JJ; Schwartz, MA; Wallace, RJ, 2003
)
2.07
"Linezolid is an oxazolidinone, which has been shown to be effective against methicillin- and vancomycin-resistant Gram-positive pathogens."( Linezolid: implications for neurosurgical infections.
Larive, LL; Nguyen, CM; Rhoney, DH, 2003
)
2.48
"Linezolid is a recently approved oxazalidinone with extended activity against Gram-positive bacteria. "( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
2.03
"Linezolid is an oxazolidinone antibiotic with a novel mechanism of action that works by inhibiting bacterial protein synthesis by blocking formation of the initiation complex."( Efficacy of linezolid versus comparator therapies in Gram-positive infections.
Wilcox, MH, 2003
)
1.42
"Linezolid is a weak, reversible monoamine oxidase inhibitor: foods containing high concentrations of tyramine should be avoided, and linezolid should be used with caution in patients taking adrenergic or serotonergic agents or in those with uncontrolled hypertension."( Safety and tolerability of linezolid.
French, G, 2003
)
1.34
"Linezolid is an oxazolidinone antibacterial agent that has inhibitory activity against a broad range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, and penicillin-resistant Streptococcus pneumoniae. "( Linezolid: in infants and children with severe Gram-positive infections.
Goa, KL; Lyseng-Williamson, KA, 2003
)
3.2
"Linezolid has proven to be a first-line therapeutic option for vancomycin-resistant strains."( Linezolid resistance since 2001: SENTRY Antimicrobial Surveillance Program.
Enne, V; Jones, RN; Mutnick, AH, 2003
)
2.48
"Linezolid is a novel oxazolidinone antibiotic that is effective for the treatment of gram-positive bacterial infections. "( Hospital resource use and cost of treatment with linezolid versus teicoplanin for treatment of serious gram-positive bacterial infections among hospitalized patients from South America and Mexico: results from a multicenter trial.
Balan, DA; Li, JZ; López, H; Mozaffari, E; Rittenhouse, BE; Tang, T; Vidal, G; Willke, RJ; Zitto, T, 2003
)
2.02
"Linezolid is a member of a new, unique class of synthetic antibacterial agents called oxazolidinones that are effective against gram-positive bacteria, including vancomycin-resistant organisms. "( Pharmacokinetics of linezolid in subjects with renal dysfunction.
Aronoff, GR; Batts, DH; Brier, ME; Hopkins, NK; Jungbluth, GL; O'Grady, M; Ryan, KK; Stalker, DJ, 2003
)
2.09
"Linezolid is an effective and well-tolerated antibiotic for the treatment of Gram-positive infections, including hospital and community-acquired pneumonia and complicated and uncomplicated skin and skin structure infections. "( Hematologic effects of linezolid in young children.
Bruss, JB; Edge-Padbury, B; Kaplan, SL; Meissner, HC; Morfin, MR; Naberhuis-Stehouwer, S; Townsend, T; Wenman, W, 2003
)
2.07
"Linezolid is a mild, reversible, inhibitor of monoamine oxidases A and B."( Clinical pharmacokinetics of linezolid, a novel oxazolidinone antibacterial.
Jungbluth, GL; Stalker, DJ, 2003
)
1.33
"Linezolid is a new, promising antibacterial agent to treat severe infections. "( Development of a liquid chromatography method for the determination of linezolid and its application to in vitro and human microdialysis samples.
Buerger, C; Joukhadar, C; Kloft, C; Muller, M, 2003
)
1.99
"Linezolid is a new antibiotic that belongs to the class of oxazolidinones approved by the FDA for the treatment of VRE infections, including those with bacteremia."( Linezolid in the treatment of vancomycin-resistant Enterococcus faecium in solid organ transplant recipients: report of a multicenter compassionate-use trial.
El-Khoury, J; Fishman, JA, 2003
)
2.48
"Linezolid is a cost-effective alternative to vancomycin for the treatment of ventilator-associated pneumonia."( Linezolid for treatment of ventilator-associated pneumonia: a cost-effective alternative to vancomycin.
Kollef, MH; Shorr, AF; Susla, GM, 2004
)
3.21
"Linezolid is a new oxazolidinone antibiotic with efficacy against a broad range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). "( Serum and sputum concentrations following the oral administration of linezolid in adult patients with cystic fibrosis.
Conway, S; Denton, M; Etherington, C; Hulme, B; Peckham, DG; Saralaya, D; Tobin, CM, 2004
)
2
"Linezolid is a synthetic antimicrobial agent which was introduced into clinical therapy in the early 2001. "( [Sensitivity of methicillin resistant staphylococci to linezolid and some other antimicrobial agents].
Aktaş, E; Ayyildiz, A; Ertek, M; Parlak, M; Yazgi, H, 2003
)
2.01
"Linezolid is a novel antibiotic administrable by the intravenous as well as the oral route. "( [Linezolid (Zyvoxid)].
Sternon, J; Van Laethem, Y, 2004
)
2.68
"Linezolid is a member of the new class of antibacterial agents called oxazolidinones that are active against Gram positive organisms and exert their action by protein synthesis inhibition. "( In vitro susceptibility of staphylococci to linezolid and other antimicrobial agents.
Bădicuţ, I; Buiuc, D; Grigore, L; Poiată, A; Tuchiluş, C,
)
1.84
"Linezolid is an alternative to vancomycin for the long-term treatment of gram-positive bacterial orthopedic infections because of its antibacterial spectrum and oral bioavailability, but duration-related myelosuppression could offset its advantages. "( Similar hematologic effects of long-term linezolid and vancomycin therapy in a prospective observational study of patients with orthopedic infections.
Rao, N; Santa, ER; Wagener, MM; Yu, VL; Ziran, BH, 2004
)
2.03
"Oral linezolid appears to be an effective and well-tolerated treatment option for hip prosthesis infections due to MRSE."( Successful treatment of Staphylococcus epidermidis hip prosthesis infection with oral linezolid.
Archambaud, M; Bonnet, E; Canonge, JM; Mogenet, I; Raetz-Dillon, S, 2004
)
1.06
"Linezolid is an important therapeutic option for infections caused by resistant gram-positive bacteria. "( Linezolid resistance in sequential Staphylococcus aureus isolates associated with a T2500A mutation in the 23S rRNA gene and loss of a single copy of rRNA.
DeGirolami, PC; Eliopoulos, GM; Gold, HS; Meka, VG; Moellering, RC; Pillai, SK; Sakoulas, G; Venkataraman, L; Wennersten, C, 2004
)
3.21
"Linezolid is a drug with well-recognised activity against S."( Successful treatment of methicillin-resistant Staphylococcus aureus endocarditis with linezolid.
Bassetti, D; Bassetti, M; Cenderello, G; Del Bono, V; Di Biagio, A, 2004
)
1.27
"Linezolid is an oxazolidinone antibiotic with activity against important grampositive aerobic bacteria, including nosocomial pathogens. "( Elimination of linezolid by an in vitro extracorporeal circuit model.
Hansen, M; Hoffmann, E; Krueger, WA; Schroeder, TH; Stephan, M; Unertl, K, 2004
)
2.12
"So, linezolid is an important therapeutic option in the treatment of infections caused by multiresistant enterococcal and staphylococcal strains."( [The role of linezolid in the therapy of infections caused by multiresistant gram-positive cocci].
Corti, G; Paradisi, F, 2004
)
1.17
"Linezolid is a new agent recently developed for Gram-positive infections, including MRSA."( Antibiotic resistance in Staphylococcus aureus: concerns, causes and cures.
Chopra, I, 2003
)
1.04
"Linezolid is an excellent and promising new antibiotic for the treatment of resistant Gram-positive pathogens."( A review of linezolid: the first oxazolidinone antibiotic.
Dotter, B; Madaras-Kelly, K; Stevens, DL, 2004
)
1.42
"Linezolid is an attractive alternative for the treatment of chronic bone and joint infections because it is active against common pathogens including methicillin-resistant staphylococci and vancomycin-resistant enterococci and because its oral formulation is convenient for long-term administration. "( Successful treatment of chronic bone and joint infections with oral linezolid.
Hall, RA; Rao, N; Santa, ER; Ziran, BH, 2004
)
2
"Linezolid is a new oxazolidinone antibiotic active against most Gram-positive microorganisms the renal elimination of which accounts for about 30% to 35% of all the clearance. "( Linezolid disposition after standard dosages in critically ill patients undergoing continuous venovenous hemofiltration: a report of 2 cases.
Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Scudeller, L; Viale, P, 2004
)
3.21
"Linezolid is an oxazolidinone antibacterial agent that acts by inhibiting the initiation of bacterial protein synthesis. "( Linezolid.
Gomber, S; Narang, M, 2004
)
3.21
"Linezolid is an oxazolidinone antimicrobial with excellent oral bioavailability and tissue penetration and is active against multidrug-resistant skin/soft tissue pathogens."( Pharmacokinetics and pharmacodynamics of linezolid in obese patients with cellulitis.
Citron, DM; Goldstein, EJ; Havlichek, DH; Kak, V; Peloquin, CA; Schooley, SL; Stein, GE; Tyrrell, KL, 2005
)
2.04
"Linezolid is a new synthetic antibiotic with a broad spectrum of activity against virtually all important Gram-positive infections. "( Linezolid use associated with lactic acidosis.
Armaganidis, A; Kopterides, P; Papadomichelakis, E, 2005
)
3.21
"Linezolid is a new antibacterial agent with a broad spectrum of activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus spp., and penicillin-resistant Streptococcus pneumoniae. "( Multiple-dose pharmacokinetics of linezolid during continuous venovenous haemofiltration.
Heinz, G; Jaeger, W; Karth, GD; Kornek, GV; Locker, GJ; Meyer, B; Nikfardjam, M; Thalhammer, F, 2005
)
2.05
"Linezolid appears to be a safe alternative to vancomycin for therapy-resistant CNS infections because of its good CSF penetration and few side-effects."( Clinical experience with linezolid for the treatment of central nervous system infections.
Pfister, HW; Rupprecht, TA, 2005
)
1.35
"Linezolid is an important oxazolidinone antimicrobial for the treatment of infections caused by Gram-positive cocci, especially vancomycin-resistant enterococci and oxacillin-resistant Staphylococcus aureus (ORSA). "( Trends in linezolid susceptibility patterns: report from the 2002-2003 worldwide Zyvox Annual Appraisal of Potency and Spectrum (ZAAPS) Program.
Anderegg, TR; Fritsche, TR; Jones, RN; Ross, JE; Sader, HS, 2005
)
2.17
"Linezolid is a new antimicrobial agent effective against drug-resistant gram-positive pathogens which are common causes of infections in hospitalized patients. "( Absolute bioavailability and pharmacokinetics of linezolid in hospitalized patients given enteral feedings.
Beringer, P; Gill, M; Gurevitch, M; Hoem, N; Louie, S; Nguyen, M; Wong-Beringer, A, 2005
)
2.03
"Linezolid is an oxazolidinone antibiotic used in the treatment of infections caused by vancomycin-resistant enterococci. "( Varying linezolid susceptibility of vancomycin-resistant Enterococcus faecium isolates during therapy: a case report.
Buchler, MW; Feldhues, RA; Fritz, S; Geiss, HK; Hoppe-Tichy, T; Martignoni, ME; Swoboda, S, 2005
)
2.21
"Linezolid is a pararental drug that also possesses near-complete oral bioavailability and a favourable pharmacokinetic profile."( Oxazolidinones--a new class of broad-spectrum chemotherapeutics.
Pasternak, K; Sztanke, K; Sztanke, M, 2004
)
1.04
"Linezolid proved to be a highly effective agent in the prophylaxis and treatment of infectious complications due to polyresistant grampositive pathogens."( [Problems of prophylaxis and treatment of infectious complications in reconstructive surgery].
Bogomolova, NS; Bolshakov, LV; Oreshkina, TD, 2005
)
1.05
"Linezolid is a more efficient option than teicoplanin because it presents higher rate of effectiveness with lower consumption of resources, thus being a dominant alternative in the treatment of Gram-positive infection with bacteremia."( Pharmacoeconomic evaluation of linezolid versus teicoplanin in bacteremia by Gram-positive microorganisms.
Grau, S; Marín-Casino, M; Mateu-de Antonio, J; Salas, E; Soto, J, 2005
)
2.06
"Linezolid is a weak monoamine oxidase inhibitor and has been reported to interact with selective serotonin reuptake inhibitors (SSRIs)."( Drug interactions between linezolid and selective serotonin reuptake inhibitors: case report involving sertraline and review of the literature.
Andrus, MR; Byrd, DC; Clark, DB, 2006
)
1.36
"Linezolid is a good option mainly in infections of skin and soft tissues, and it has an evincible advantage over vancomycin in the treatment of nosocomial pneumonia and surgical-site infections."( Role of linezolid in the treatment of resistant gram-positive infections.
Benes, J; Cetkovský, P; Dlouhý, P; Dolezel, T; Herold, I; Jahoda, D; Kolár, M; Kouba, M; Novák, I; Nyc, O; Pilnácek, J; Rácil, Z; Sechser, T; Sevcík, P; Svihovec, P, 2006
)
1.49
"Linezolid is an oxazolidinone antibiotic that is increasingly used to treat drug-resistant, gram-positive pathogens. "( Linezolid-induced inhibition of mitochondrial protein synthesis.
Boelaert, JR; Coster, RV; De Vriese, AS; Groote, CC; Lovering, A; Martin, JJ; Seneca, S; Smet, J; Van Haute, LL; Vandecasteele, S; Vanopdenbosch, LJ, 2006
)
3.22
"Linezolid is a new antibiotic with high bioavailability and an outstanding safety profile, synergistic with imipenem, which may deserve a place in the armamentarium for severe pneumonia in children."( Effectiveness of linezolid and imipenem association in the treatment of severe community-acquired pneumonia in children: two case reports.
Caillon, J; Christophe Roze, J; Denizot, S; Godon, N; Gras-Le Guen, C; Podevin, G; Potel, G, 2006
)
1.39
"Linezolid is a bacteriostatic oxazolidinone antibiotic that has been proven to be effective for the treatment of patients with pneumonia, skin and soft tissue infections, and possibly bacteraemia, due to Gram-positive cocci. "( Linezolid for the treatment of patients with endocarditis: a systematic review of the published evidence.
Falagas, ME; Manta, KG; Ntziora, F; Vardakas, KZ, 2006
)
3.22
"Linezolid is a reversible, nonselective monoamine oxidase inhibitor. "( Linezolid and serotonergic drug interactions: a retrospective survey.
Estes, LL; Taylor, JJ; Wilson, JW, 2006
)
3.22
"Linezolid is an oxazolidinone agent which is apparently well designed for treating chronic osteomyelitis, but data on effectiveness and tolerability as prolonged therapy is currently lacking."( Effectiveness and tolerability of prolonged linezolid treatment for chronic osteomyelitis: a retrospective study.
Beltrand, E; Caillaux, M; Legout, L; Migaud, H; Mouton, Y; Senneville, E; Valette, M; Yazdanpanah, Y, 2006
)
2.04
"Linezolid is a new antimicrobial agent effective against drug-resistant gram-positive pathogens commonly responsible for central nervous system (CNS) infections in neurosurgical patients hospitalized in intensive care units. "( Serum and cerebrospinal fluid concentrations of linezolid in neurosurgical patients.
Anagnostaki, M; Baltopoulos, G; Boutzouka, E; Markantonis, SL; Myrianthefs, P; Panidis, D; Vlachos, K, 2006
)
2.03
"Linezolid is a relatively new drug that has been approved for treatment of MRSA infections, but currently there is no research demonstrating its efficacy at treating infections of the disc space."( Efficacy of linezolid versus vancomycin in the treatment of methicillin-resistant Staphylococcus aureus discitis: a controlled animal model.
Brookfield, KF; Chen, J; Chiappetta, G; Conaughty, JM; Eismont, FJ; Martinez, OV, 2006
)
1.43
"Linezolid is a clinically attractive alternative to vancomycin due to its mild side effect profile and oral bioavailability. "( Efficacy of linezolid versus vancomycin in the treatment of methicillin-resistant Staphylococcus aureus discitis: a controlled animal model.
Brookfield, KF; Chen, J; Chiappetta, G; Conaughty, JM; Eismont, FJ; Martinez, OV, 2006
)
2.16
"Linezolid is a treatment option for joint infections following arthroplasty that are caused by resistant bacterial strains, such as MRSA, MRSE or VRE. "( [Linezolid in the treatment of antibiotic-resistant gram-positive infections of the musculoskeletal system].
Jahoda, D; Landor, I; Nyc, O; Pokorný, D; Sosna, A, 2006
)
2.69
"Linezolid is a synthetic antibiotic, the first available agent in a new class of antibiotic called the oxazolidinones, whose particular mechanism of action consists in inhibiting the initiation of protein synthesis. "( [Linezolid: antibacterial activity, clinical efficacy and resistance].
Bourgeois-Nicolaos, N; Butel, MJ; Doucet-Populaire, F; Piriou, O,
)
2.48
"Linezolid is a member of a new class of synthetic antibiotics called oxazolidinones, introduced into therapy due to the increasing resistance of Gram-positive pathogens to traditional antibiotics."( Linezolid: a new antibiotic for newborns and children?
Cuzzolin, L; Fanos, V, 2006
)
2.5
"Linezolid is a new synthetic antibiotic belonging to the oxazolidinone class, available for the therapy of gram-positive infections, caused by methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant pneumococci. "( Correlation between linezolid zone diameter and minimum inhibitory concentration values determined by regression analysis.
Buiuc, D; Dimitriu, G; Poiata, A; Tuchiluş, C,
)
1.9
"Linezolid is a reasonable alternative for treating chronic implant-related osteomyelitis."( Linezolid in the treatment of implant-related chronic osteomyelitis.
Holtom, P; Patzakis, MJ; Vercillo, M; Zalavras, CG, 2007
)
2.5
"Linezolid is an attractive alternative for orthopedic infections because of oral bioavailability and activity against methicillin-resistant staphylococci and vancomycin-resistant enterococci. "( Efficacy and safety of linezolid for Gram-positive orthopedic infections: a prospective case series.
Hamilton, CW; Rao, N, 2007
)
2.09
"Linezolid is a new antibiotic with activity against Gram-positive cocci, including MRSA, and has good penetration into the cerebrospinal fluid."( Treatment of meningitis caused by methicillin-resistant Staphylococcus aureus with linezolid.
Kessler, AT; Kourtis, AP, 2007
)
1.29
"Linezolid is a recent oral antibiotic used in drug-resistant Gram-positive cocci infection. "( Linezolid-related pancytopenia in organ-transplant patients: report of two cases.
Faguer, S; Fillola, G; Guitard, J; Kamar, N; Rostaing, L, 2007
)
3.23
"Linezolid is an oxazolidinone antibacterial agent indicated for serious gram-positive infections. "( Linezolid-associated peripheral and optic neuropathy, lactic acidosis, and serotonin syndrome.
Narita, M; Tsuji, BT; Yu, VL, 2007
)
3.23
"Linezolid is an important therapeutic option for the treatment of infections caused by multiresistant Gram-positive bacteria such as vancomycin-resistant Enterococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). "( A simple isocratic HPLC assay to determine linezolid concentrations in different biomatrices for in vivo and in vitro studies.
Anagnostakos, K; Geiss, HK; Hoppe-Tichy, T; Ober, M; Swoboda, S; Weigand, MA, 2007
)
2.05
"Linezolid seems to be a promising choice."( Linezolid: effectiveness and safety for approved and off-label indications.
Falagas, ME; Ntziora, F; Vardakas, KZ, 2007
)
2.5
"Linezolid is a recent oral antibiotic used in drug-resistant Gram-positive cocci infections. "( Linezolid-induced interstitial nephritis in a kidney-transplant patient.
Esposito, L; Guilbeau-Frugier, C; Kamar, N; Mehrenberger, M; Modesto, A; Rostaing, L, 2007
)
3.23
"Linezolid is an antibacterial agent of oxazolidinone group."( In vitro activities of linezolid and tigecycline against methicillin-resistant Staphylococcus aureus strains.
Akcam, FZ; Kaya, O; Temel, EN, 2008
)
1.38
"Linezolid is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens."( In vitro activities of linezolid against important gram-positive bacterial pathogens including vancomycin-resistant enterococci.
Hacek, D; Noskin, GA; Peterson, LR; Siddiqui, F; Stosor, V, 1999
)
1.34
"Linezolid appears to be a potentially useful drug for infections caused by gram-positive cocci."( Activity of linezolid against multi-resistant gram-positive bacteria from diverse hospitals in the United Kingdom.
Johnson, AP; Livermore, DM; Warner, M, 2000
)
1.41
"Linezolid is an oxazolidinone antibacterial agent that acts by inhibiting the initiation of bacterial protein synthesis. "( Linezolid.
Clemett, D; Markham, A, 2000
)
3.19
"Linezolid is an oxazolidinone antibiotic with excellent in vitro activity against a number of Gram-positive organisms including antibiotic-resistant isolates. "( Single dose pharmacokinetics of linezolid in infants and children.
Abdel-Rahman, SM; Blumer, JL; Bradley, JA; Jacobs, RF; James, LP; Jungbluth, GL; Kearns, GL; Reed, MD; Stalker, DJ; Welshman, IR, 2000
)
2.03
"Linezolid is a well-tolerated, effective treatment for adults with gram-positive nosocomial pneumonia."( Linezolid (PNU-100766) versus vancomycin in the treatment of hospitalized patients with nosocomial pneumonia: a randomized, double-blind, multicenter study.
Cammarata, S; Oliphant, T; Rubinstein, E; Wunderink, R, 2001
)
2.47
"Linezolid is an oxazolidinone available as an oral drug which has activity against most gram-positive bacteria. "( Activities of linezolid against rapidly growing mycobacteria.
Brown-Elliott, BA; Crist, CJ; Mann, LB; Wallace, RJ; Ward, SC; Wilson, RW, 2001
)
2.11
"Linezolid is a synthetic agent which is active against all the clinically important Gram-positive bacteria, including multiply resistant strains."( Linezolid.
French, G,
)
2.3
"Linezolid is an oxazolidinone developed by Pharmacia (formerly Pharmacia & Upjohn) for the treatment of multi-resistant Gram-positive infections [187765,317456]. "( Linezolid Pharmacia Corp.
Barrett, JF, 2000
)
3.19
"Linezolid is a member of the oxazolidinones."( [Antibiotics--TAZ/PIPC, synercid, linezolid, everninomicin].
Hidai, H, 2001
)
1.31
"Linezolid is a new oxazolidinone antibiotic used to treat infections caused by vancomycin-resistant enterococci (VRE). "( Infections due to vancomycin-resistant Enterococcus faecium resistant to linezolid.
DenBesten, K; Gonzales, RD; Graham, MB; Kelkar, S; Quinn, JP; Schreckenberger, PC, 2001
)
1.98
"Linezolid is a generally well tolerated drug."( Linezolid: a review of its use in the management of serious gram-positive infections.
Jarvis, B; Perry, CM, 2001
)
2.47
"Linezolid (PNU-100766) is a new gram-positive oxazolidinone antibiotic that is effective at in vitro concentrations < or =4 microg/ml and in vivo doses < or =10 mg/kg. "( Cardiovascular sympathomimetic amine interactions in rats treated with monoamine oxidase inhibitors and the novel oxazolidinone antibiotic linezolid.
Curry, JT; Humphrey, SJ; Stryd, RP; Turman, CN, 2001
)
1.96
"Linezolid is a weak and reversible monoamine oxidase (MAO) inhibitor and although no increased frequency of adrenergic or serotonergic adverse events has been reported, it is recommended that linezolid is used with caution in patients treated with other MAO inhibitors."( Linezolid--a review of the first oxazolidinone.
Norrby, R, 2001
)
2.47
"Linezolid is a novel oxazolidinone antibiotic with mild reversible monoamine oxidase inhibitor (MAOI) activity. "( Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr.
Antal, EJ; Batts, DH; Hendershot, PE; Hopkins, NK; Welshman, IR, 2001
)
3.2
"Linezolid is a new synthetic antimicrobial agent with activity against multidrug-resistant Gram-positive cocci."( [In vitro activity of linezolid against clinical isolates of methicillin-resistant Staphylococcus aureus].
Alarcón, T; de Las Cuevas, MC; Jiménez, S; López-Brea, S; Pérez, L, 2001
)
1.35
"Linezolid is an oxazolidinone derivative which is active mostly against Gram-positive bacteria. "( Systemic and intracerebral infections of mice with Listeria monocytogenes successfully treated with linezolid.
Callapina, M; Dietz, A; Hof, H; Kretschmar, M; Mosbach, C; Nichterlein, T, 2001
)
1.97
"Linezolid is a promising drug in the treatment of infections caused by Gram-positive cocci. "( The DUEL study: a multi-center in vitro evaluation of linezolid compared with other antibiotics in the Netherlands.
Jansz, AR; Mouton, JW, 2001
)
2
"Linezolid is an oxazolidinone indicated in the treatment of nosocomial and community-acquired pneumonia, complicated and uncomplicated skin and skin structure infections and vancomycin-resistant Enterococcus infections. "( Linezolid: pharmacokinetic characteristics and clinical studies.
Bouza, E; Muñoz, P, 2001
)
3.2
"Linezolid is a novel oxazolidinone antibiotic that has a spectrum of activity encompassing a variety of Gram-positive bacteria. "( Linezolid absolute bioavailability and the effect of food on oral bioavailability.
Hopkins, NK; Jungbluth, GL; Sisson, TA; Stalker, DJ; Welshman, IR, 2001
)
3.2
"Linezolid is a parenteral agent that also possesses near-complete oral bioavailability plus favourable pharmacokinetic and toxic effect profiles."( Oxazolidinone antibiotics.
Diekema, DJ; Jones, RN, 2001
)
1.03
"Linezolid is a new antibiotic that can treat multiresistant gram-positive infections and can be given parenterally or by mouth. "( Linezolid: a new antibiotic for gram-positive infections.
Wilson, P, 2001
)
3.2
"Linezolid is a synthetic antibiotic belonging to a new class of antimicrobials called the oxazolidinones."( Linezolid: its role in the treatment of gram-positive, drug-resistant bacterial infections.
Ament, PW; Horne, JP; Jamshed, N, 2002
)
2.48
"Linezolid is a new antibiotic that is effective in the treatment of both antibiotic-susceptible and antibiotic-resistant Gram-positive bacterial infections, including those resistant to other available antibiotics."( Economic evaluation of linezolid, flucloxacillin and vancomycin in the empirical treatment of cellulitis in UK hospitals: a decision analytical model.
Balan, D; Li, Z; Nathwani, D; Rittenhouse, B; Vinken, A; Wilike, R, 2001
)
1.34
"Linezolid is an oxazolidinone compound that has been shown to have impressive antimicrobial activity against a number of Gram-positive bacteria. "( Linezolid is a specific inhibitor of 50S ribosomal subunit formation in Staphylococcus aureus cells.
Champney, WS; Miller, M, 2002
)
3.2
"Linezolid is a new oxazolidinone antibiotic with potent activity against gram-positive bacteria, including Streptococcus pneumoniae. "( Pharmacodynamic activity and efficacy of linezolid in a rat model of pneumococcal pneumonia.
Gentry-Nielsen, MJ; Olsen, KM; Preheim, LC, 2002
)
2.02

Effects

Linezolid has a unique structure and mechanism of action, which targets protein synthesis at an exceedingly early stage. It is amenable to oral or parenteral administration and potentially useful for continuing outpatient therapy that was initiated for inpatients.

Linezolid has a wide spectrum of activity against gram-positive organisms. Blood count monitoring is recommended in patients receiving this drug for long-term therapy. Linezolid also provided improved outcomes in the treatment of serious vancomycin-resistant entrococci and methicillin-resistant Staphylococcus aureus.

ExcerptReferenceRelevance
"Linezolid has a high distribution in the liver. "( Linezolid-induced thrombocytopenia in a child with a liver transplant: A case report.
Chen, L; Liu, Y; Lu, X; Qi, F; Zhang, B; Zhu, L, 2021
)
3.51
"Linezolid has a favorable pharmacokinetic profile."( Association of pharmacokinetic and pharmacodynamic aspects of linezolid with infection outcome.
Falagas, ME; Kioumis, I; Vardakas, KZ, 2009
)
1.31
"Linezolid has a 100% absorption and can be administered orally or intravenously; it is cleared by renal and hepatic routes, thus dose adjustments are not needed in moderate renal or hepatic failure."( [Oxazolidinones and glycopeptides].
Pigrau, C, 2003
)
1.04
"Linezolid has a unique mechanism of action in its inhibition of bacterial protein synthesis in Gram-positive and a number of anaerobic bacteria."( [Linezolid, an agent from a new class of antibiotics].
Bernards, AT; Kuijper, EJ; Schippers, EF, 2004
)
1.96
"Linezolid has a wide spectrum of activity against gram-positive organisms including methicillin resistant staphylococci, penicillin resistant pneumococci and vancomycin resistant enterococcus faecalis and E."( Linezolid.
Gomber, S; Narang, M, 2004
)
2.49
"Linezolid has an oral and parenteral formulation, which are equivalent."( Role of linezolid in the treatment of complicated skin and soft tissue infections.
Peppard, WJ; Weigelt, JA, 2006
)
1.49
"Linezolid has a wide spectrum of activity against gram-positive organisms including methicillin-resistant staphylococci, penicillin-resistant pneumococci and vancomycin-resistant Enterococcus faecalis and E."( Linezolid.
Clemett, D; Markham, A, 2000
)
2.47
"Linezolid has a wide gram-positive spectrum of activity and is amenable to oral or parenteral administration These attributes make it potentially useful for continuing outpatient therapy that was initiated for inpatients."( Linezolid--a new option for treating gram-positive infections.
Batts, DH, 2000
)
2.47
"Linezolid has a unique structure and mechanism of action, which targets protein synthesis at an exceedingly early stage. "( Linezolid: an oxazolidinone antimicrobial agent.
Fung, HB; Kirschenbaum, HL; Ojofeitimi, BO, 2001
)
3.2
"Linezolid has a spectrum of activity against Gram-positive micro-organisms including methicillin-resistant Staphylococcus aureus (MRSA) and VRE, and can provide a useful treatment alternative to the glycopeptides."( The use of linezolid in the treatment of vancomycin-resistant enterococcal septicaemia in two patients with burn injuries.
Atkins, JL; Dziewulski, P; Hidvegi, N; Teare, L, 2002
)
1.43
"Linezolid resistance has dominantly been mediated by mutations in 23S rRNA or ribosomal protein L4 genes. "( First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
Castanheira, M; Deshpande, LM; DiPersio, J; Jones, RN; Mendes, RE; Saubolle, MA, 2008
)
2.05
"Linezolid has been one of the key anti-tuberculosis agents for the treatment of multidrug-resistant tuberculosis (MDR-TB)/extensively drug-resistant tuberculosis (XDR-TB). "( Linezolid for patients with multidrug-resistant tuberculosis/extensively drug-resistant tuberculosis in China.
Chen, X; Deng, G; Lin, Y; Tan, J; Zhang, H; Zhang, P, 2022
)
3.61
"Linezolid has the potential to interact with some antidepressants, leading to serotonin syndrome. "( Association of Linezolid With Risk of Serotonin Syndrome in Patients Receiving Antidepressants.
Bai, AD; Gill, SS; Loeb, M; McKenna, S; Wise, H, 2022
)
2.52
"Linezolid has been reported to restore erythromycin susceptibility in erythromycin-resistant "( Loss of
Chen, W; Huang, Y; Jiao, X; Lin, Y; Yao, F; Ye, J, 2023
)
2.35
"Linezolid use has increased in frequency and duration, especially in the treatment of drug-resistant tuberculosis, and data indicate that these patients experience lower rates of complete vision recovery compared with patients taking linezolid for other indications."( Linezolid optic neuropathy.
Cao, AA; Lee, MS; McClelland, CM; Miller, HV, 2023
)
3.07
"Linezolid has been the common antimicrobial treatment for Gram-positive infection even in neonates and infants. "( Relationship between cytopenia and gestational age in infants and neonates treated with linezolid therapy.
Asai, N; Hagihara, M; Kato, H; Koizumi, Y; Mikamo, H; Shibata, Y; Suematsu, H; Watarai, M; Yamagishi, Y, 2020
)
2.22
"Linezolid has shown strong antimicrobial activity against multidrug-resistant (MDR)/rifampin-resistant strains of Mycobacterium tuberculosis. "( Penetration of linezolid into bone tissue 24 h after administration in patients with multidrug-resistant spinal tuberculosis.
Dong, W; Fan, J; Guo, A; Huang, H; Lan, T; Li, Y; Qin, S; Wen, S; Zhang, T, 2019
)
2.31
"Linezolid has previously been reported to cause a toxic optic neuropathy. "( Linezolid-induced photoreceptor dysfunction masquerading as autoimmune retinopathy.
Berman, A; Grassi, MA; Grohmann, SM, 2020
)
3.44
"Linezolid (LNZ) has recently been listed by the World Health Organization (WHO) as a Group A agent for the treatment of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) in longer regimens (18-20 months). "( Safety of longer linezolid regimen in children with drug-resistant tuberculosis and extensive tuberculosis in Southwest China.
Chen, J; Cheng, Z; Fu, Z; Jiang, L; Liu, Q; Shang, T; Wang, X; Xu, H; Zhang, Z; Zhu, K, 2020
)
2.34
"Linezolid has potential adverse effects like bone marrow suppression, peripheral neuropathy and hyponatremia."( Linezolid-induced rare triad of hypoglycaemia, bone marrow suppression and hyponatraemia in elderly.
Kapoor, D; Shenoy, S; Singhania, SVK, 2020
)
2.72
"Linezolid resistance has increasingly been described in coagulase negative staphylococci (CoNS) in recent years. "( First Draft Genome Sequence of Linezolid and Rifampicin Resistant Staphylococcus haemolyticus.
Bakthavatchalam, YD; Neeravi, A; Perumal, R; Vasudevan, K; Veeraraghavan, B, 2020
)
2.29
"Linezolid has good penetration into cerebrospinal fluid and brain tissue."( Linezolid as salvage therapy for central nervous system infections due to methicillin-resistant Staphylococcus aureus at two medical centers in Taiwan.
Chen, HA; Lee, CH; Liao, CH; Tsai, MS; Yang, CJ, 2020
)
2.72
"Linezolid has been increasingly used in tertiary NICUs. "( Increasing use of linezolid in a tertiary NICU during a 10-year period: reasons and concerns for the future.
Barreto, C; Butin, M; Claris, O; Matrat, L; Plaisant, F, 2020
)
2.33
"Linezolid has coverage against non-tuberculous mycobacteria and is an effective therapeutic option for cutaneous NTM cases in which identification to the species level is not possible or when adverse effects limit therapeutic options."( Linezolid as a treatment option for cutaneous non-tuberculous mycobacterial infections.
Farooq, S; Koshelev, MV; McNally, MA; Tschen, J, 2020
)
2.72
"Linezolid has a high distribution in the liver. "( Linezolid-induced thrombocytopenia in a child with a liver transplant: A case report.
Chen, L; Liu, Y; Lu, X; Qi, F; Zhang, B; Zhu, L, 2021
)
3.51
"Linezolid resistance has since emerged, yet its global prevalence remains low."( Prevalence and mechanisms of linezolid resistance among staphylococcal clinical isolates from Egypt.
Abouelfetouh, A; El-Nakeeb, M; Maarouf, L; Omar, H, 2021
)
1.63
"Linezolid has previously been reported to cause toxic optic neuropathy and retinopathy."( Linezolid-Induced Toxic Optic Neuropathy.
Aljebreen, MA; Alotaibi, AK; Alrobaian, M,
)
2.3
"Linezolid has excellent antibiotic activity against gram-positive organisms and is expected to be an alternative to vancomycin for the treatment of bacterial meningitis. "( Different intra-cerebrospinal distribution of linezolid in patients with inflammatory meningitis.
Enoki, Y; Fukao, E; Ichinose, N; Ichisawa, M; Matsumoto, K; Oda, T; Taguchi, K; Takahata, T; Tsutsumi, K; Yoshikawa, G, 2021
)
2.32
"Linezolid has been approved for the treatment of infections caused by vancomycin-resistant"( Linezolid: a review of its properties, function, and use in critical care.
Farhadi, T; Ganjparvar, M; Hashemian, SMR, 2018
)
2.64
"Linezolid has been widely used in serious infections for its effective inhibiting effect against multidrug-resistant gram-positive pathogens. "( Linezolid Inhibited Synthesis of ATP in Mitochondria: Based on GC-MS Metabolomics and HPLC Method.
Hu, L; Huang, A; Lin, G; Wang, X; Wen, C; Ye, X, 2018
)
3.37
"Linezolid has been successfully used for treatment of multidrug-resistant tuberculosis (MDR-TB). "( Linezolid-based Regimens for Multidrug-resistant Tuberculosis (TB): A Systematic Review to Establish or Revise the Current Recommended Dose for TB Treatment.
Akkerman, OW; Alffenaar, JC; Bolhuis, MS; Ghimire, S; Gumbo, T; Srivastava, S; Sturkenboom, MGG, 2018
)
3.37
"Linezolid has immunomodulatory properties."( Effect of linezolid on clinical severity and pulmonary cytokines in a murine model of influenza A and Staphylococcus aureus coinfection.
Fusco, DN; He, Y; Liu, X; Papanicolaou, GA; White, JR; Xiao, K, 2013
)
1.51
"Linezolid has emerged as an important therapeutic option for the treatment of Staphylococcus aureus in patients with cystic fibrosis. "( Rapid emergence of resistance to linezolid and mutator phenotypes in Staphylococcus aureus isolates from an adult cystic fibrosis patient.
Chapron, J; Collobert, G; Dusser, D; Hubert, D; Longo, M; Morand, PC; Poyart, C; Tazi, A; Touak, G, 2013
)
2.11
"Linezolid has antibacterial activity against aerobic Gram-positive cocci, including methicillin-resistant Staphylococcus aureus (MRSA). "( Population pharmacokinetic analysis of linezolid in low body weight patients with renal dysfunction.
Hiraki, Y; Kamimura, H; Karube, Y; Matsumoto, K; Mizoguchi, A; Morita, K; To, H; Tsuji, Y; Yukawa, E, 2013
)
2.1
"Linezolid has been off-label used in treatment of MDR/XDR-TB with major adverse effects."( Outcomes of MDR/XDR-TB patients treated with linezolid: experience in Thailand.
Chuchottaworn, C; Roongruangpitayakul, C, 2013
)
1.37
"Linezolid has good efficacy in treatment of MDR/XDR-TB with major adverse effect and should be used with caution. "( Outcomes of MDR/XDR-TB patients treated with linezolid: experience in Thailand.
Chuchottaworn, C; Roongruangpitayakul, C, 2013
)
2.09
"Linezolid has demonstrated clinical efficacy and favourable outcomes in patients for the treatment of MRSA cSSTIs including the treatment of lower extremity infections."( European perspective and update on the management of complicated skin and soft tissue infections due to methicillin-resistant Staphylococcus aureus after more than 10 years of experience with linezolid.
Baguneid, M; Bassetti, M; Bouza, E; Dryden, M; Nathwani, D; Wilcox, M, 2014
)
1.31
"Linezolid has demonstrated high penetration into the epithelial lining fluid of patients with ventilator-associated pneumonia and shown statistically superior clinical efficacy versus vancomycin in the treatment of MRSA NP in a phase IV, randomized, controlled study."( European perspective and update on the management of nosocomial pneumonia due to methicillin-resistant Staphylococcus aureus after more than 10 years of experience with linezolid.
Blasi, F; Chastre, J; Masterton, RG; Rello, J; Torres, A; Welte, T, 2014
)
1.32
"Linezolid has shown promise as an alternative in the empiric therapy of nocardiosis, but little is known about its effectiveness and safety in this setting."( Experience with linezolid for the treatment of nocardiosis in organ transplant recipients.
De La Cruz, O; Minces, LR; Silveira, FP, 2015
)
1.48
"Linezolid has been reported to remain active against 98% of staphylococci with resistance identified in 0.05% of Staphylococcus aureus and 1.4% of CoNS. "( Molecular characterization of linezolid-resistant CoNS isolates in Japan.
Ishiwada, N; Kimura, A; Matsui, M; Sato, Y; Shibayama, K; Takaya, A; Watanabe, M; Yamamoto, T, 2015
)
2.15
"Linezolid, which has bacteriostatic activity, is approved for the treatment of vancomycin-resistant enterococci (VRE) infections. "( Daptomycin versus linezolid for treatment of vancomycin-resistant enterococcal bacteremia: systematic review and meta-analysis.
Chang, SC; Chuang, YC; Lin, HY; Wang, JT, 2014
)
2.18
"Linezolid has unique immunomodulatory effects on host inflammatory response and lung injury in a murine model of post-viral cMRSA pneumonia."( Linezolid has unique immunomodulatory effects in post-influenza community acquired MRSA pneumonia.
Ballinger, MN; Bhan, U; Keshamouni, V; Kovach, MA; Podsiad, AB; Standiford, TJ, 2015
)
3.3
"Linezolid has been directly compared to vancomycin in pneumonia; however, most clinical trials have not compared outcomes specifically in the healthcare-associated pneumonia (HCAP) population. "( Comparative-effectiveness of vancomycin and linezolid as part of guideline-recommended empiric therapy for healthcare-associated pneumonia.
Attridge, RT; Frei, CR; Mortensen, EM; Reveles, KR, 2015
)
2.12
"Linezolid has been increasingly used for several severe infections including multidrug-resistant tuberculosis. "( Linezolid Induced Reversible Peripheral Neuropathy.
Goyal, MK; Lal, V; Modi, M; Vishnu, VY,
)
3.02
"Linezolid (LZD) has become increasingly important for the treatment of multidrug-resistant tuberculosis (MDR-TB), but its mechanisms of resistance are not well characterized. "( Mycobacterium tuberculosis Mutations Associated with Reduced Susceptibility to Linezolid.
Chan, D; Chen, J; Cui, P; Niu, H; Shi, W; Shi, X; Yew, WW; Zhang, S; Zhang, W; Zhang, Y, 2016
)
2.1
"Linezolid has been recommended for treatment of patients with multidrug-resistant (MDR) or extensively-drug-resistant (XDR) tuberculosis, although uncertainties remain regarding its safety and tolerability in these circumstances."( Efficacy and safety profile of linezolid in the treatment of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis: a systematic review and meta-analysis.
Agyeman, AA; Ofori-Asenso, R, 2016
)
1.44
"Linezolid (LZD) has arisen as an alternative treatment in diabetic foot osteitis due to staphylococci. "( Mutation in the L3 Ribosomal Protein Could Be Associated with Risk of Selection of High-Level Linezolid-Resistant Staphylococcus epidermidis Strains.
Aslangul, E; Bourgeois-Nicolaos, N; Butel, MJ; Deback, C; Doucet-Populaire, F; Rivière, A; Rouard, C, 2017
)
2.12
"Linezolid has been studied in several randomized controlled trials for the treatment of patients with community-acquired and nosocomial pneumonia, skin and soft tissue infections (SSTIs), urinary tract infections and bacteraemia."( Benefit-risk assessment of linezolid for serious gram-positive bacterial infections.
Falagas, ME; Vardakas, KZ, 2008
)
1.36
"Linezolid has modest early bactericidal activity against rapidly dividing tubercle bacilli in patients with cavitary pulmonary tuberculosis during the first 2 days of administration, but little extended early bactericidal activity. "( Early and extended early bactericidal activity of linezolid in pulmonary tuberculosis.
Boom, WH; Debanne, SM; Dietze, R; Eisenach, K; Hadad, DJ; Johnson, DF; Johnson, JL; Maciel, EL; McGee, B; Molino, LP; Palaci, M; Peloquin, CA, 2008
)
2.04
"Linezolid has a favorable pharmacokinetic profile."( Association of pharmacokinetic and pharmacodynamic aspects of linezolid with infection outcome.
Falagas, ME; Kioumis, I; Vardakas, KZ, 2009
)
1.31
"Linezolid has demonstrated activity against antibiotic-susceptible and antibiotic-resistant aerobic Gram-positive cocci. "( Linezolid: a review of safety and tolerability.
Rubinstein, E; Vinh, DC, 2009
)
3.24
"Linezolid therapy has shown high rates of clinical success in patients with osteomyelitis and prosthetic joint infections caused by Gram-positive cocci. "( Tolerability of prolonged linezolid therapy in bone and joint infection: protective effect of rifampicin on the occurrence of anaemia?
Beltrand, E; Caillaux, M; Dezeque, H; Dubreuil, L; Legout, L; Lemaire, X; Loïez, C; Migaud, H; Nguyen, S; Senneville, E; Valette, M; Yazdanpanah, Y, 2010
)
2.1
"Linezolid has been used in the treatment of multidrug-resistant/extensively drug-resistant tuberculosis in adults with encouraging results, however experience in children is scarce. "( Linezolid in the treatment of multidrug-resistant/extensively drug-resistant tuberculosis in paediatric patients: experience of a paediatric infectious diseases unit.
Brito, MJ; Ferreira, G; Gouveia, C; Kjöllerström, P; Varandas, L, 2011
)
3.25
"Linezolid has monoamine oxidase (MAO) inhibitory properties, and MAO inhibitors have been reported to contribute to hypoglycemia. "( Linezolid-associated hypoglycemia in a 64-year-old man with type 2 diabetes.
Bodnar, T; Halter, JB; Starr, K, 2011
)
3.25
"Linezolid has been in general use in the UK since 2000. "( Linezolid: safety and efficacy in special populations.
Gould, FK, 2011
)
3.25
"Linezolid has been widely used in the treatment of Gram-positive infections for more than a decade. "( Linezolid pharmacokinetics and pharmacodynamics in clinical treatment.
Dryden, MS, 2011
)
3.25
"Linezolid has proven valuable in musculoskeletal infections, however, failure and resistance have been described and toxicity is worrisome when more than 28 days are necessary. "( Usefulness of monitoring linezolid trough serum concentration in prolonged treatments.
Bori, G; Cervera, C; García-Ramiro, S; López, R; Martínez-Pastor, JC; Mensa, J; Soriano, A; Sousa, R, 2011
)
2.12
"Linezolid has activity against resistant staphylococci and a high oral bioavailability; therefore, it could be a good option for combining with rifampicin."( Decreased serum linezolid concentrations in two patients receiving linezolid and rifampicin due to bone infections.
Brunet, M; Climent, C; Cuesta, M; Garcia-Ramiro, S; Hoyo, I; Martínez-Pastor, J; Mensa, J; Soriano, A, 2012
)
1.45
"Linezolid has been successfully used to treat DR-TB in adults, but there are few case reports of its use in children for TB."( Linezolid-containing regimens for the treatment of drug-resistant tuberculosis in South African children.
Hallbauer, UM; Hesseling, AC; Rose, PC; Schaaf, HS; Seddon, JA, 2012
)
2.54
"Linezolid has antimycobacterial activity in vitro and is increasingly used for patients with highly drug-resistant tuberculosis."( Linezolid for treatment of chronic extensively drug-resistant tuberculosis.
Barry, CE; Carroll, MW; Chen, RY; Cho, SN; Choi, H; Dartois, V; Follmann, D; Goldfeder, LC; Jeon, HS; Jeong, I; Jin, B; Joh, JS; Kang, E; Kim, CT; Kim, H; Kwak, H; Lee, D; Lee, J; Lee, JK; Lee, M; Min, S; Olivier, KN; Park, H; Park, SK; Shaw, PA; Song, SD; Song, T; Via, LE, 2012
)
3.26
"Linezolid has demonstrated similar efficacy to vancomycin in randomized clinical trials and recent data have suggested that it may be superior in some cases, although there are limitations to this conclusion."( Pharmacotherapy for methicillin-resistant Staphylococcus aureus nosocomial pneumonia.
Church, TJ; Segarra-Newnham, M, 2012
)
1.1
"Linezolid has been associated with reversible myelosuppression. "( Hematologic effects of linezolid: summary of clinical experience.
Arellano, FM; Bruss, JB; Gerson, SL; Hafkin, B; Kaplan, SL; Kuter, DJ; Le, V, 2002
)
2.07
"Linezolid has gram-positive activity comparable to that of vancomycin, is effective in a variety of infections, and is well tolerated, with diarrhea, headache, and nausea being the most frequently reported adverse effects."( Linezolid: an oxazolidinone antimicrobial agent.
Paladino, JA, 2002
)
2.48
"Linezolid has approved indications for skin and soft tissue infections; lower respiratory tract infections; and vancomycin-resistant Enterococcus faecium infections, including cases with concurrent bacteremia."( Linezolid: the first oxazolidinone antimicrobial.
Moellering, RC, 2003
)
2.48
"Linezolid has a 100% absorption and can be administered orally or intravenously; it is cleared by renal and hepatic routes, thus dose adjustments are not needed in moderate renal or hepatic failure."( [Oxazolidinones and glycopeptides].
Pigrau, C, 2003
)
1.04
"Linezolid has been associated with anemia and thrombocytopenia. "( Mechanisms for linezolid-induced anemia and thrombocytopenia.
Barile, AJ; Bernstein, WB; Rector, JT; Tjaden, JA; Trotta, RF, 2003
)
2.11
"Linezolid has excellent therapeutic potential against most species of NTM."( In vitro activity of linezolid against slowly growing nontuberculous Mycobacteria.
Brown-Elliott, BA; Crist, CJ; Mann, LB; Wallace, RJ; Wilson, RW, 2003
)
1.36
"Linezolid has proven to be a first-line therapeutic option for vancomycin-resistant strains."( Linezolid resistance since 2001: SENTRY Antimicrobial Surveillance Program.
Enne, V; Jones, RN; Mutnick, AH, 2003
)
2.48
"Linezolid therapy has the potential to reduce the total cost of treatment."( Hospital resource use and cost of treatment with linezolid versus teicoplanin for treatment of serious gram-positive bacterial infections among hospitalized patients from South America and Mexico: results from a multicenter trial.
Balan, DA; Li, JZ; López, H; Mozaffari, E; Rittenhouse, BE; Tang, T; Vidal, G; Willke, RJ; Zitto, T, 2003
)
1.29
"Linezolid has complete bioavailability in parenteral and oral administration, is well tolerated and shows little toxicity, thus favoring a shortened hospital stay, improving the patient's quality of life and reducing social costs."( Treatment of gram-positive surgical sepsis: role of the oxazolidinones.
Carnuccio, P; Colizza, S; Cucchiara, G; Rodio, F; Rossi, S, 2003
)
1.04
"Linezolid has been proven to have high efficacy against MRSA by some trials abroad."( [Successful treatment with linezolid in two cases of methicillin-resistant Staphylococcus aureus infections in the orthopedic field].
Fukuda, Y; Hirakata, Y; Kaneko, Y; Kohno, S; Miyazaki, Y; Nakamura, S; Otsu, Y; Shindo, H; Tashiro, T; Tomono, K; Yanagihara, K, 2003
)
1.34
"Oral linezolid has excellent bioavailability and activity against MRSA and MR-CoNS and offers the potential for outpatient treatment of MRSA and MR-CoNS infections."( Early switch and early discharge opportunities in intravenous vancomycin treatment of suspected methicillin-resistant staphylococcal species infections.
Goetz, MB; Parodi, S; Rhew, DC,
)
0.59
"Linezolid has similar safety and efficacy to teicoplanin in treating Gram-positive infections in the critically ill. "( Linezolid versus teicoplanin in the treatment of Gram-positive infections in the critically ill: a randomized, double-blind, multicentre study.
Cepeda, JA; Cooper, B; Hails, J; Hayman, S; Jones, K; Kibbler, C; Kwaku, F; Shaw, S; Shulman, R; Singer, M; Taylor, L; Whitehouse, T; Wilson, AP, 2004
)
3.21
"Linezolid has dopaminergic properties that may enhance the central nervous system effects of anticholinergics."( Acute delirium associated with combined diphenhydramine and linezolid use.
Serio, RN, 2004
)
1.29
"Linezolid has promising in vitro anti-adhesion activity that merits further studies to determine its role in the management of foreign-body infections."( Effects of linezolid on staphylococcal adherence versus time of treatment.
Buchanan, LV; Dailey, CF; Gibson, JK; Haas, JV; Pagano, PJ; Van Enk, RA, 2004
)
1.43
"Linezolid has a unique mechanism of action in its inhibition of bacterial protein synthesis in Gram-positive and a number of anaerobic bacteria."( [Linezolid, an agent from a new class of antibiotics].
Bernards, AT; Kuijper, EJ; Schippers, EF, 2004
)
1.96
"As linezolid has been shown to have hematologic side effects, blood count monitoring is recommended in patients receiving this drug for long-term therapy."( Sideroblastic anemia due to linezolid in a patient with a left ventricular assist device.
Dunlap, S; Heroux, A; Loew, J; Montpetit, MC; Pamboukian, SV; Shammo, JL, 2004
)
1.13
"Linezolid has a wide spectrum of activity against gram-positive organisms including methicillin resistant staphylococci, penicillin resistant pneumococci and vancomycin resistant enterococcus faecalis and E."( Linezolid.
Gomber, S; Narang, M, 2004
)
2.49
"Linezolid has both intravenous and oral formulations and the latter is 100% bioavailable."( Update on linezolid: the first oxazolidinone antibiotic.
Wilcox, MH, 2005
)
1.45
"Linezolid has an oral and parenteral formulation, which are equivalent."( Role of linezolid in the treatment of complicated skin and soft tissue infections.
Peppard, WJ; Weigelt, JA, 2006
)
1.49
"Linezolid has also provided improved outcomes in the treatment of serious vancomycin-resistant entrococci (VRE) and methicillin-resistant Staphylococcus aureus (MRSA) infections."( [Linezolid--novel antibiotic for the treatment of gram-positive bacterial infections].
Jankowski, A; Stefanik, W, 2006
)
1.97
"Linezolid has very good in vitro activity against staphylococci, with an MIC 90 of 2 mcg/ml and only 0.8% resistance."( Antimicrobial susceptibility of Staphylococcus aureus isolated from colonized hospital personnel.
Ambăruş, A; Buiuc, D; Luca, V; Poiată, A; Teodor, A; Teodorescu, I; Tuchiluş, C,
)
0.85
"Linezolid has been approved for the treatment of patients with infections caused by Gram-positive cocci that are resistant to traditionally used antibiotics, including glycopeptides. "( Linezolid versus glycopeptide or beta-lactam for treatment of Gram-positive bacterial infections: meta-analysis of randomised controlled trials.
Falagas, ME; Siempos, II; Vardakas, KZ, 2008
)
3.23
"Linezolid has a wide spectrum of activity against gram-positive organisms including methicillin-resistant staphylococci, penicillin-resistant pneumococci and vancomycin-resistant Enterococcus faecalis and E."( Linezolid.
Clemett, D; Markham, A, 2000
)
2.47
"Linezolid has been shown to be effective against key gram-positive pathogens in vitro, without evidence of resistance development or cross-resistance to other antibiotics."( Linezolid--a new option for treating gram-positive infections.
Batts, DH, 2000
)
2.47
"Linezolid has excellent antibacterial activity against a wide range of Gram-positive organisms. "( In vitro activity of linezolid (U-100766) against Haemophilus influenzae measured by three different susceptibility testing methods.
Biedenbach, DJ; Jones, RN, 2001
)
2.07
"Linezolid has a unique structure and mechanism of action, which targets protein synthesis at an exceedingly early stage. "( Linezolid: an oxazolidinone antimicrobial agent.
Fung, HB; Kirschenbaum, HL; Ojofeitimi, BO, 2001
)
3.2
"Linezolid has good activity against gram-positive bacteria, particularly multidrug resistant strains of S. "( Linezolid: a review of its use in the management of serious gram-positive infections.
Jarvis, B; Perry, CM, 2001
)
3.2
"Linezolid has almost 100% bioavailability and the area under the plasma concentration curve is identical after oral and iv."( Linezolid--a review of the first oxazolidinone.
Norrby, R, 2001
)
2.47
"Linezolid has been proved to be useful in severe infections sustained by multiresistant Gram-positive micro-organisms."( The oxazolidinones as a new family of antimicrobial agent.
Marchese, A; Schito, GC, 2001
)
1.03
"Linezolid has a spectrum of activity against Gram-positive micro-organisms including methicillin-resistant Staphylococcus aureus (MRSA) and VRE, and can provide a useful treatment alternative to the glycopeptides."( The use of linezolid in the treatment of vancomycin-resistant enterococcal septicaemia in two patients with burn injuries.
Atkins, JL; Dziewulski, P; Hidvegi, N; Teare, L, 2002
)
1.43
"Linezolid has been compared to vancomycin for treatment of Gram-positive nosocomial pneumonia, and the clinical cure rates were 66.4 % and 68.1 %, respectively. "( [New treatment option for gram-positive infections in critically ill patients - overview over linezolid].
Krueger, WA; Unertl, KE, 2002
)
1.98

Actions

Linezolid did not inhibit the independent binding of either mRNA or N-formylmethionyl-tRNA to E. Linezolid may cause reversible optic neuropathy and irreversible peripheral neuropathy after months of treatment. LineZolid can cause serious adverse effects including thrombocytopenia and anemia.

ExcerptReferenceRelevance
"Linezolid (LZD) may cause thrombocytopenia, which can result in discontinuation of treatment. "( Pharmacokinetic and pharmacodynamic simulation for the quantitative risk assessment of linezolid-associated thrombocytopenia.
Ikawa, K; Ikebuchi, A; Ishihara, N; Morikawa, N; Naora, K; Nishimura, N; Onita, T; Tamaki, H; Yano, T, 2022
)
2.39
"Linezolid can cause serious adverse effects including thrombocytopenia and anemia. "( Hematological toxicities associated with linezolid therapy in adults: key findings and clinical considerations.
Cattaneo, D; Gervasoni, C; Marriott, DJ, 2023
)
2.62
"Linezolid may cause adverse effects such as thrombocytopenia, which were found to be dependent on receiving linezolid for longer than 2 weeks. "( Linezolid-related adverse effects in clinical practice in children.
Bayram, N; Devrim, İ; Düzgöl, M; Kara, A; Özdemir, FM, 2017
)
3.34
"Linezolid plays an increasingly important role in the treatment of multidrug-resistant tuberculosis (MDR-TB). "( Clinical validation of the analysis of linezolid and clarithromycin in oral fluid of patients with multidrug-resistant tuberculosis.
Alffenaar, JW; Bolhuis, MS; de Lange, WC; Greijdanus, B; Kosterink, JG; Uges, DR; van Altena, R; van der Werf, TS; van Hateren, K, 2013
)
2.1
"Linezolid was noted to cause time and dose-dependent reversible myelosuppression in preclinical studies. "( Pancytopenia and lactic acidosis associated with linezolid use in a patient with empyema.
Kraleti, S; Soultanova, I, 2013
)
2.09
"Linezolid can cause trombocytopenia when treatment lasted longer than two weeks."( [Oxazolidinones and glycopeptides].
Pigrau, C, 2003
)
1.04
"Linezolid may cause reversible optic neuropathy and irreversible peripheral neuropathy after months of treatment."( Linezolid-associated toxic optic neuropathy.
Bardenstein, D; Hamilton, SR; Isada, CM; Lee, MS; Rucker, JC, 2006
)
2.5
"Linezolid yielded a lower average cost-effectiveness ratio, euro 8,444.78 (8,195.90 - 8,709.25) than teicoplanin, euro 9,962.74 (9,465.68 - 10,502.23), with a slight reduction in average cost per successfully treated patient of 15.2% ( euro 1,517.96)."( Economic evaluation of linezolid versus teicoplanin for the treatment of infections caused by gram-positive microorganisms in Spain.
Aguado, JM; Del Castillo, A; Gonzalez, P; Grau, S; Mateu-de Antonio, J, 2007
)
1.37
"Linezolid did not inhibit the independent binding of either mRNA or N-formylmethionyl-tRNA to E."( The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria.
Aoki, H; Ganoza, MC; Shinabarger, DL; Swaney, SM, 1998
)
1.36

Treatment

Linezolid improves the treatment outcomes of multidrug-resistant tuberculosis substantially. Linezolid-related treatment interruption is common, is strongly associated with HIV co-infection, and system-specific toxicity occurs within predictable time frames.

ExcerptReferenceRelevance
"In linezolid-treated animals, dark-field microscopy and qPCR assessment showed no presence of treponemes after day 3 post-treatment start, serologic test did not convert to positive, CSF had no abnormalities, and RIT was negative."( Efficacy of linezolid on Treponema pallidum, the syphilis agent: A preclinical study.
Giacani, L; Haynes, AM; Mayans, MV; Mitjà, O; Nieto, C; Pérez-Mañá, C; Quintó, L; Romeis, E; Ubals, M, 2021
)
1.51
"Linezolid or daptomycin treatment for at least 10 days and higher Pitt bacteremia scores were independently associated with 14-day and 28-day mortality."( Clinical characteristics and treatment outcomes of vancomycin-resistant Enterococcus faecium bacteremia.
Cheng, CW; Huang, CT; Huang, PY; Lee, MH; Shie, SS; Wu, TS; Yang, JH; Ye, JJ, 2018
)
1.2
"Linezolid with other treatments for skin and soft tissue infections (SSTIs) has been evaluated in several studies. "( Efficacy and safety of linezolid compared with other treatments for skin and soft tissue infections: a meta-analysis.
Li, Y; Xu, W, 2018
)
2.23
"Linezolid improves the treatment outcomes of multidrug-resistant tuberculosis substantially. "( Substitution of ethambutol with linezolid during the intensive phase of treatment of pulmonary tuberculosis: a prospective, multicentre, randomised, open-label, phase 2 trial.
Ahn, H; Cho, YJ; Choi, HS; Choi, SM; Hahn, S; Han, J; Heo, EY; Hwang, YR; Jeong, I; Jo, YS; Joh, JS; Ki, J; Kim, DK; Kim, H; Kim, HS; Kim, J; Kim, SJ; Kwak, N; Lee, CH; Lee, J; Lee, JH; Lee, JK; Lee, JY; Lee, M; Lee, SH; Lee, SM; Lee, YJ; Lim, JN; Park, JH; Park, JS; Park, SS; Park, YS; Song, T; Yim, JJ; Yoon, HI, 2019
)
2.24
"Linezolid-related treatment interruption is common, is strongly associated with HIV co-infection, and system-specific toxicity occurs within predictable time frames. "( Linezolid interruption in patients with fluoroquinolone-resistant tuberculosis receiving a bedaquiline-based treatment regimen.
Dheda, K; Esmail, A; Gina, P; Limberis, J; Olayanju, O, 2019
)
3.4
"Linezolid-treated mice had less weight loss on days 4-6 after influenza infection compared to placebo (all P<0.05)."( Effect of linezolid on clinical severity and pulmonary cytokines in a murine model of influenza A and Staphylococcus aureus coinfection.
Fusco, DN; He, Y; Liu, X; Papanicolaou, GA; White, JR; Xiao, K, 2013
)
1.51
"Linezolid is a valuable treatment option for central nervous system (CNS) infections caused by multidrug-resistant Gram-positive micro-organisms. "( Plasma and cerebrospinal fluid concentrations of linezolid in neurosurgical critically ill patients with proven or suspected central nervous system infections.
Alvarez-Lerma, F; Basas, M; Campillo, N; Ferrández, O; Grau, S; Horcajada, JP; Lipman, J; Luque, S; Roberts, JA, 2014
)
2.1
"Linezolid treatment was also associated with greater 30-day all-cause mortality and microbiologic failure in this cohort."( Comparison of the Effectiveness and Safety of Linezolid and Daptomycin in Vancomycin-Resistant Enterococcal Bloodstream Infection: A National Cohort Study of Veterans Affairs Patients.
Britt, NS; Patel, N; Potter, EM; Steed, ME, 2015
)
1.4
"Linezolid is a valuable treatment option for treating infections caused by multi-resistant gram-positive pathogens. "( Decreased Linezolid Serum Concentrations in Three Critically Ill Patients: Clinical Case Studies of a Potential Drug Interaction between Linezolid and Rifampicin.
Blassmann, U; Briegel, J; Frey, OR; Huge, V; Koeberer, A; Roehr, AC; Vetter-Kerkhoff, C, 2016
)
2.28
"Linezolid is a treatment option for methicillin-resistant Staphylococcus aureus (MRSA) infections in cystic fibrosis (CF) patients. "( Pharmacokinetics of intravenous and oral linezolid in adults with cystic fibrosis.
Keel, RA; Kloft, C; Knauft, RF; Kuti, JL; Muhlebach, M; Nicolau, DP; Pope, JS; Schaeftlein, A, 2011
)
2.08
"The linezolid treatment for methicillin-resistant Staphylococcus aureus (MRSA) infection was sporadically reported in children. "( Successful treatment of pediatric endocarditis and pericarditis due to MRSA with linezolid.
Miyaji, K; Miyamoto, T; Tomoyasu, T, 2011
)
1.15
"Linezolid iv treatment was started after intensive pre-treatment (up to 11 other antibiotics for a median duration of 14 days) and changed to enteral administration in only 4% of all iv courses."( Use of linezolid in neonatal and pediatric inpatient facilities--results of a retrospective multicenter survey.
Ammann, RA; Beutel, K; Dirkwinkel, E; Dohna-Schwake, C; Ebinger, F; Faber, J; Groll, AH; Holzapfel, J; Klabunde-Cherwon, A; Lehrnbecher, T; Masjosthusmann, K; Müllenborn, E; Müller, A; Prelog, M; Schenk, W; Simon, A, 2012
)
1.56
"Linezolid is one of few treatment options available for vancomycin-resistant enterococci. "( Risk factors associated with linezolid-nonsusceptible enterococcal infections.
Allen, GP; Bearden, DT; Hartung, DM; McGregor, JC; Taplitz, RA; Tong, T; Traver, R, 2012
)
2.11
"Linezolid-treated patients had fewer IV catheter-site complications and less kidney impairment but more frequent thrombocytopenia than those who received vancomycin, regardless of the presence or absence of vascular disease."( Linezolid and vancomycin in treatment of lower-extremity complicated skin and skin structure infections caused by methicillin-resistant Staphylococcus aureus in patients with and without vascular disease.
Duane, TM; Huang, DB; Puzniak, LA; Weigelt, JA, 2012
)
2.54
"Linezolid treatment significantly reduced the bacterial counts in the wounds."( Treatment with an oxazolidinone antibiotic inhibits toxic shock syndrome toxin-1 production in MRSA-infected burn wounds.
Amundsen, B; Jo, DY; Jordan, MH; Mauskar, NA; Mino, MJ; Moffatt, LT; Njimoluh, KL; Ortiz, RT; Randad, PR; Shupp, JW,
)
0.85
"Linezolid effectively treated infections caused by S."( Linezolid versus cefadroxil in the treatment of skin and skin structure infections in children.
Bruss, J; Fleishaker, D; Hilty, M; Naberhuis-Stehouwer, S; Tregnaghi, M; Wible, K, 2003
)
2.48
"linezolid in the treatment of MRSS-infected patients."( Cost analysis of switching from i.v. vancomycin to p.o. linezolid for the management of methicillin-resistant Staphylococcus species.
McCollum, M; Parodi, S; Rhew, DC, 2003
)
1.29
"Linezolid treatment with 600 mg orally twice daily was instituted for MRSA cellulitis."( Serotonin toxicity associated with concomitant use of linezolid.
Bergeron, L; Boulé, M; Perreault, S, 2005
)
1.3
"Linezolid is a treatment option for joint infections following arthroplasty that are caused by resistant bacterial strains, such as MRSA, MRSE or VRE. "( [Linezolid in the treatment of antibiotic-resistant gram-positive infections of the musculoskeletal system].
Jahoda, D; Landor, I; Nyc, O; Pokorný, D; Sosna, A, 2006
)
2.69
"The linezolid treatment for meningitis was sporadically reported in adults but there was no report in children."( Successful treatment with linezolid of meningitis complicated with subdural empyema in a 6-month-old boy.
Dinleyici, EC; Dinleyici, M; Yakut, A; Yarar, C, 2007
)
1.12
"Linezolid treatment was more active (P < 0.05) than vancomycin treatment or no treatment."( Linezolid therapy of vancomycin-resistant Enterococcus faecium experimental endocarditis.
Patel, R; Piper, KE; Rouse, MS; Steckelberg, JM, 2001
)
2.47
"Linezolid-treated patients had significant LOS reductions that otherwise would be masked without the use of more appropriate, but less commonly used, methods."( Approaches to analysis of length of hospital stay related to antibiotic therapy in a randomized clinical trial: linezolid versus vancomycin for treatment of known or suspected methicillin-resistant Staphylococcus species infections.
Glick, HA; Li, JZ; Rittenhouse, BE; Willke, RJ, 2002
)
1.25
"Treatment with linezolid was an alternative to catheter removal in these patients."( Successful port-a-cath salvage using linezolid in children with acute leukemia.
Català, A; Estella, J; Justicia, A; Moreno, RB; Rives, S; Ruiz-Llobet, A; Toll, T, 2013
)
1
"Treatment with linezolid was not associated with more adverse effects in general (OR = 0.61, 95 % CI 0.25-1.48)."( Efficacy and safety of linezolid for the treatment of infections in children: a meta-analysis.
Apostolidou-Kiouti, F; Haidich, AB; Ioannidou, M; Niopas, I; Roilides, E, 2014
)
1.05
"Treatment with linezolid for VRE-BSI resulted in significantly higher treatment failure in comparison to daptomycin. "( Comparison of the Effectiveness and Safety of Linezolid and Daptomycin in Vancomycin-Resistant Enterococcal Bloodstream Infection: A National Cohort Study of Veterans Affairs Patients.
Britt, NS; Patel, N; Potter, EM; Steed, ME, 2015
)
1.03
"Treatment with linezolid in critically ill patients with Gram-positive infections was equivalent to vancomycin in terms of efficacy and safety, but linezolid was associated to a higher rate of microbiologic eradication of the infecting organism at the seventh day of treatment."( Linezolid more efficacious than vancomycin to eradicate infecting organism in critically ill patients with Gram-positive infections.
Bonet, A; de Batlle, J; de la Torre, M; Motjé, M; Piñeiro, L; Sirvent, JM, 2010
)
2.16
"Treatment with linezolid was not associated with more adverse effects in general in comparison with vancomycin (OR=1.06, 95%CI 0.68-1.64, P>0.05)."( [Linezolid versus vancomycin in the treatment of pneumonia caused by Gram-positive cocci: meta-analysis of randomised controlled trials].
Chen, Q; Huang, P; Huang, YL; Lin, ZQ, 2010
)
1.61
"Treatment with linezolid combined with TMP-SMZ resulted in a clear clinical improvement and bacterial clearance."( Linezolid combined with trimethoprim-sulfamethoxazole therapy for the treatment of disseminated nocardiosis.
Li, H; Shen, Q; Zhou, H; Zhou, J, 2011
)
2.15
"Treatment with linezolid was continued for a total therapy duration of three weeks, after which the patient was discharged in a good condition. "( Enterococcus gallinarum meningitis: a case report and literature review.
Elshafi, SS; Khan, FY, 2011
)
0.71
"Treatment with linezolid at a dosage of 10 mg/kg every 8 h intravenously for a duration of 16 days and 14 days, respectively, was well tolerated and led to complete clinical recovery and clearance of the organism from all body sites."( Linezolid treatment of glycopeptide-resistant Enterococcus faecium in very low birth weight premature neonates.
Bauer, K; Groll, AH; Hoehn, R; Schaefer, V; Schloesser, RL, 2006
)
2.12
"Treatment with linezolid, which penetrates well into the lung, is associated with higher cure and survival rates."( Methicillin-Resistant S. aureus Ventilator-Associated Pneumonia: Strategies to Prevent and Treat.
Lam, AP; Wunderink, RG, 2006
)
0.67
"Treatment with linezolid was not associated with more adverse effects in general (OR 1.40 [0.95-2.06]); however, thrombocytopenia was recorded more commonly in patients receiving linezolid (OR 11.72 [3.66-37.57])."( Linezolid versus glycopeptide or beta-lactam for treatment of Gram-positive bacterial infections: meta-analysis of randomised controlled trials.
Falagas, ME; Siempos, II; Vardakas, KZ, 2008
)
2.13
"The treatment with LINEZOLID initialized immediately after the identification of the microbiological agent or when was suspect the resistant of initial antibiotics gram-positive infection."( [Our experience with linesolid usage in newborn children].
Atanasova, V; Rosmanova, R; Slavkova, N, 2007
)
0.66

Toxicity

Linezolid was significantly related to higher adverse events than ampicillin/sulbactam. Among children with MDR-TB there are no linezolid pharmacokinetic data, and its adverse effects have not yet been prospectively described.

ExcerptReferenceRelevance
" Linezolid is well tolerated: the most common adverse events (gastrointestinal effects, headache) are reported in frequencies similar to those reported for comparator agents."( Efficacy and safety of linezolid in the treatment of skin and soft tissue infections.
Hau, T, 2002
)
1.54
"8%) of the 191 episodes of infection, patients experienced one or more adverse events or exhibited one or more abnormal laboratory results; in 35 (18."( The efficacy and safety of linezolid as treatment for Staphylococcus aureus infections in compassionate use patients who are intolerant of, or who have failed to respond to, vancomycin.
Birmingham, MC; Forrest, A; Moise, PA; Schentag, JJ, 2002
)
0.61
" Linezolid was well-tolerated in this patient population, with an overall adverse event rate of 17."( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
1.5
"Linezolid was safe and effective in treating resistant Gram-positive infections in neutropenic cancer patients."( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
2.03
"Clinical trials have shown that linezolid (600 mg twice daily in adults) is safe and generally well tolerated for up to 28 days."( Safety and tolerability of linezolid.
French, G, 2003
)
0.9
" Drug-related adverse events were primarily transient."( Worldwide assessment of linezolid's clinical safety and tolerability: comparator-controlled phase III studies.
Cammarata, S; Hafkin, B; Isturiz, R; Le, V; Oliphant, TH; Remington, J; Rubinstein, E; Smith, LG; Standiford, HC, 2003
)
0.63
" Because of the increasing use of linezolid, it is important to review the common adverse events (AEs) associated with its use in children with the use of data from clinical trials."( Safety and tolerability of linezolid in children.
Bruss, JB; Edge-Padbury, B; Goldfarb, J; Kaplan, SA; Naberhuis-Stehouwer, S; Saiman, L; Wible, K, 2003
)
0.89
"Linezolid was safe and well-tolerated in pediatric patients with community-acquired pneumonia, otitis media, SSSIs and infections caused by Gram-positive resistant pathogens."( Safety and tolerability of linezolid in children.
Bruss, JB; Edge-Padbury, B; Goldfarb, J; Kaplan, SA; Naberhuis-Stehouwer, S; Saiman, L; Wible, K, 2003
)
2.06
" However, the apparent increase in observed adverse events, particularly bone marrow suppression, seen with prolonged administration, means that treatment of such patients must be undertaken with careful surveillance, at least until these complications are better understood."( The safety and efficacy of linezolid in orthopaedic practice for the treatment of infection due to antibiotic-resistant organisms.
Giannoudis, PV; Harwood, PJ, 2004
)
0.62
" Seven of 10 patients experienced serious adverse events, which led to withdrawal of linezolid in all seven."( Efficacy and safety of linezolid in multidrug resistant tuberculosis (MDR-TB)--a report of ten cases.
Brubakk, O; Sandven, P; von der Lippe, B, 2006
)
0.87
" Adverse hematological events have been reported."( Possibly linezolid-induced peripheral and central neurotoxicity: report of four cases.
Biron, F; Boibieux, A; Chidiac, C; Ferry, T; Issartel, B; Petiot, P; Peyramond, D; Ponceau, B; Simon, M, 2005
)
0.75
"Two de novo peripheral neuropathies and one worsening of a preexisting toxic neuropathy have been observed."( Possibly linezolid-induced peripheral and central neurotoxicity: report of four cases.
Biron, F; Boibieux, A; Chidiac, C; Ferry, T; Issartel, B; Petiot, P; Peyramond, D; Ponceau, B; Simon, M, 2005
)
0.75
" Close neurological monitoring should be recommended in prolonged linezolid therapy and coadministration of a serotonin reuptake inhibitor or antihistamine should be avoided to limit neurological adverse events."( Possibly linezolid-induced peripheral and central neurotoxicity: report of four cases.
Biron, F; Boibieux, A; Chidiac, C; Ferry, T; Issartel, B; Petiot, P; Peyramond, D; Ponceau, B; Simon, M, 2005
)
0.98
" Patients were also evaluated for adverse drug reactions due to linezolid."( The effectiveness and safety of oral linezolid for the primary and secondary treatment of osteomyelitis.
Aneziokoro, CO; Cannon, JP; Lentino, JR; Pachucki, CT, 2005
)
0.84
" Distribution of adverse events, including reported hematologic events, was similar between groups, except that linezolid was associated with fewer drug-related adverse events (52 [17."( Efficacy and safety of linezolid compared with vancomycin in a randomized, double-blind study of febrile neutropenic patients with cancer.
Hartman, CS; Jaksic, B; Leonard, LB; Martinelli, G; Perez-Oteyza, J; Tack, KJ, 2006
)
0.86
"We requested from the US Food and Drug Administration all postmarketing adverse event reports regarding linezolid that included serotonin toxicity or any report describing cognitive or behavioral symptoms and autonomic and neuromuscular excitability."( Serotonin toxicity associated with the use of linezolid: a review of postmarketing data.
Adra, M; Gillman, PK; Lawrence, KR, 2006
)
0.81
" Thirteen patients required an intervention to prevent permanent impairment or required hospitalization for the adverse event."( Serotonin toxicity associated with the use of linezolid: a review of postmarketing data.
Adra, M; Gillman, PK; Lawrence, KR, 2006
)
0.59
" Assessment of causality using the Naranjo adverse drug reaction probability scale revealed a probable relationship between this adverse drug event and linezolid therapy."( Bell's palsy associated with linezolid therapy: case report and review of neuropathic adverse events.
Bruno-Murtha, LA; Thai, XC, 2006
)
0.82
" New rare adverse events are likely to follow."( Tongue discoloration in an elderly kidney transplant recipient: Treatment-related adverse event?
Amir, KA; Arsura, EL; Balogun, SA; Bobba, RK; Clarke, B; Evans, JM; Nagy-Agren, S, 2006
)
0.33
" Based on the Naranjo probability scale, the calculated score for tongue discoloration as a drug-related adverse event was 7 out of a maximum score of 13 points, designating it as a probable cause."( Tongue discoloration in an elderly kidney transplant recipient: Treatment-related adverse event?
Amir, KA; Arsura, EL; Balogun, SA; Bobba, RK; Clarke, B; Evans, JM; Nagy-Agren, S, 2006
)
0.33
" We present this case to increase clinicians' awareness of the potential adverse event."( Tongue discoloration in an elderly kidney transplant recipient: Treatment-related adverse event?
Amir, KA; Arsura, EL; Balogun, SA; Bobba, RK; Clarke, B; Evans, JM; Nagy-Agren, S, 2006
)
0.33
" The aim of this study was to evaluate the influences of pyridoxine, rifampin, and renal function on hematological adverse events."( Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
Bové, A; García, S; Marcos, M; Martínez, JA; Martínez, JC; Mensa, J; Ortega, M; Peñarroja, G; Soriano, A, 2007
)
0.55
" The most common adverse events were thrombocytopenia (n = 5) and anemia (n = 5), necessitating treatment discontinuation in 3 patients."( Efficacy and safety of linezolid for Gram-positive orthopedic infections: a prospective case series.
Hamilton, CW; Rao, N, 2007
)
0.65
"The optic nerve is quite vulnerable to the toxic effect of drugs."( [Toxicity of recent and less recent drugs on the optic nerve. Does Viagra cause blindness?].
Cordonnier, M, 2007
)
0.34
" However, haematological toxic effects of linezolid frequently limit its prolonged use, especially in patients with poor marrow reserves such as those with cancer receiving chemotherapy."( The role of vitamin B6 in the prevention of haematological toxic effects of linezolid in patients with cancer.
Adachi, J; Chemaly, RF; Hachem, R; Raad, I; Rolston, K; Ying, J; Youssef, S, 2008
)
0.84
" We found no significant differences in the rate of haematological toxic effects between the two patient groups."( The role of vitamin B6 in the prevention of haematological toxic effects of linezolid in patients with cancer.
Adachi, J; Chemaly, RF; Hachem, R; Raad, I; Rolston, K; Ying, J; Youssef, S, 2008
)
0.58
"Damage of the optic nerve (optic neuropathy) may be caused, apart from other reasons, by an adverse drug effect."( [Adverse effect optic neuropathy].
Martini, BC, 2008
)
0.35
"Tigecycline is safe and effective in hospitalized patients with serious infection caused by MRSA."( Efficacy and safety of tigecycline compared with vancomycin or linezolid for treatment of serious infections with methicillin-resistant Staphylococcus aureus or vancomycin-resistant enterococci: a Phase 3, multicentre, double-blind, randomized study.
Babinchak, T; Beuran, M; Bochan, M; Cooper, CA; Dartois, N; Dimov, R; Dukart, G; Ellis-Grosse, EJ; Fichev, G; Florescu, I; Gandjini, H; Razbadauskas, A, 2008
)
0.59
"Since linezolid was licensed, rare-but-serious adverse events caused by inhibition of mitochondrial protein synthesis have been identified."( Toxicity of extended courses of linezolid: results of an Infectious Diseases Society of America Emerging Infections Network survey.
Beekmann, SE; Gilbert, DN; Polgreen, PM, 2008
)
1.11
"To review the literature (including latest publications) about the adverse events of linezolid and its overall safety."( Update on the safety of linezolid.
Falagas, ME; Metaxas, EI, 2009
)
0.88
"The range of adverse events of linezolid is growing; new ones, such as nephro-toxicity and Bell's palsy, have been reported."( Update on the safety of linezolid.
Falagas, ME; Metaxas, EI, 2009
)
0.95
" Our findings demonstrate no adverse effect on the times to neutrophil or platelet engraftment with linezolid use."( Hematologic safety profile of linezolid in the early periengraftment period after allogeneic stem cell transplantation.
Chou, J; Chung, D; Cohen, N; Heller, G; Mihu, CN; Papanicolaou, GA; Seo, SK, 2009
)
0.86
" The main adverse events were thrombocytopenia grade 1-3 and anemia grade 2-3 (four and two patients, respectively)."( Efficacy and safety of linezolid in immunocompromised children with cancer.
Chatzi, F; Chrousos, G; Karamolegou, K; Moschovi, M; Santou, A; Tourkantoni, N; Trimis, G; Tsotra, M, 2010
)
0.67
"Linezolid may be another effective and safe therapy to treat infections from resistant Gram-positive bacteria in immunocompromised children, even in young ages."( Efficacy and safety of linezolid in immunocompromised children with cancer.
Chatzi, F; Chrousos, G; Karamolegou, K; Moschovi, M; Santou, A; Tourkantoni, N; Trimis, G; Tsotra, M, 2010
)
2.11
" Adverse events were similar to each drug's established safety profile."( Efficacy and safety of linezolid versus vancomycin for the treatment of complicated skin and soft-tissue infections proven to be caused by methicillin-resistant Staphylococcus aureus.
Baruch, AM; Bhattacharyya, H; Dryden, MS; Itani, KM; Kunkel, MJ; Weigelt, JA, 2010
)
0.67
" All doses were safe and well tolerated."( Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis.
Bedarida, G; Campbell, S; Jakubiec, W; Kumar, V; Ladutko, L; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, A; Wallis, RS; Zhu, T, 2011
)
0.37
" We did not observe any further adverse events, especially no severe neurological complications (e."( Efficacy and safety of linezolid in liver transplant patients.
Juntermanns, B; Kaiser, GM; Mathe, Z; Paul, A; Radunz, S; Saner, FH; Treckmann, J, 2011
)
0.68
" However, little is known about the mechanism of this side effect and the exposure-response relationship."( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
0.61
"Spontaneous reports in the United States Food and Drug Administration Adverse Event Reporting System (AERS) database generated between November 1, 1997, and December 21, 2008."( Potential for linezolid-related blindness: a review of spontaneous adverse event reports.
Aitken, SL; Brown, J; van Manen, RP, 2011
)
0.73
" A limitation of AERS is the lack of a quantitative exposure estimate to put rare adverse events of the AERS, such as linezolid-related blindness, into perspective."( Potential for linezolid-related blindness: a review of spontaneous adverse event reports.
Aitken, SL; Brown, J; van Manen, RP, 2011
)
0.94
" Nausea and vomiting were the most common adverse events."( Randomized, double-blind, phase II, multicenter study evaluating the safety/tolerability and efficacy of JNJ-Q2, a novel fluoroquinolone, compared with linezolid for treatment of acute bacterial skin and skin structure infection.
Almenoff, J; Andrae, D; Covington, P; Davenport, JM; Liverman, L; McIntyre, G; O'Riordan, W, 2011
)
0.57
"3%) patients due to adverse reactions."( Linezolid: an effective, safe and cheap drug for patients failing multidrug-resistant tuberculosis treatment in India.
Bali, RK; Behera, D; Caminero, JA; Gupta, S; Jaiswal, A; Singla, N; Singla, R, 2012
)
1.82
" The exact proportions of serious and minor adverse events determined by linezolid were 21."( Efficacy and safety of linezolid in the treatment of extensively drug-resistant tuberculosis.
Gu, J; Hao, XH; Liu, YD; Sun, H; Tangg, SJ; Xiao, HP; Yao, L; Zhang, Q; Zheng, LH, 2011
)
0.91
" All reported adverse events were evaluated for serotonin toxicity using exact and surrogate terms consistent with Sternbach Criteria and Hunter Serotonin Toxicity Criteria."( Comparison of serotonin toxicity with concomitant use of either linezolid or comparators and serotonergic agents: an analysis of Phase III and IV randomized clinical trial data.
Butterfield, JM; Huang, DB; Lawrence, KR; Lodise, TP; Reisman, A; Thompson, CA, 2012
)
0.62
" No patients in either group were reported to have adverse events identified as serotonin toxicity."( Comparison of serotonin toxicity with concomitant use of either linezolid or comparators and serotonergic agents: an analysis of Phase III and IV randomized clinical trial data.
Butterfield, JM; Huang, DB; Lawrence, KR; Lodise, TP; Reisman, A; Thompson, CA, 2012
)
0.62
" However, prolonged linezolid treatment (>14 days) is considered to increase the risk of hematological adverse events."( Immediate hematological toxicity of linezolid in healthy volunteers with different body weight: a phase I clinical trial.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Guo, D; Liang, B; Liu, Y; Vouloumanou, EK; Wang, R, 2012
)
0.98
" Only two patients (both teen-aged) encountered linezolid-related adverse effects (13 %, 2/16)."( Safety and efficacy of linezolid in 16 infants and children in Japan.
Hasegawa, N; Iketani, O; Iwata, S; Kudo, M; Mori, T; Shimada, H; Shimojima, N; Shinjoh, M; Sugita, K; Takahashi, T; Watanabe, K; Yamagishi, H, 2012
)
0.95
" Adverse events were observed in 63 (58."( Efficacy, safety and tolerability of linezolid containing regimens in treating MDR-TB and XDR-TB: systematic review and meta-analysis.
Alffenaar, JW; Anger, HA; Caminero, JA; Castiglia, P; Centis, R; D'Ambrosio, L; De Lorenzo, S; Ferrara, G; Koh, WJ; Migliori, GB; Schecter, GF; Shim, TS; Singla, R; Skrahina, A; Sotgiu, G; Spanevello, A; Udwadia, ZF; Villar, M; Zampogna, E; Zellweger, JP; Zumla, A, 2012
)
0.65
" Adverse events were reported in 46 (41."( A randomized, evaluator-blind, phase 2 study comparing the safety and efficacy of omadacycline to those of linezolid for treatment of complicated skin and skin structure infections.
Arbeit, RD; Draper, MP; Hait, H; Noel, GJ; Tanaka, SK, 2012
)
0.59
"Literature was accessed via MEDLINE/PubMed and Google Scholar (both through February 2013) using the search terms linezolid, serotonin syndrome, serotonin toxicity, and adverse reaction."( Clinical relevance of linezolid-associated serotonin toxicity.
Maynor, LM; Woytowish, MR, 2013
)
0.91
" However, the safe upper threshold level for LNZ plasma trough concentrations (Cmin values) has not been defined with certainty."( Linezolid plasma concentrations and occurrence of drug-related haematological toxicity in patients with gram-positive infections.
Baldelli, S; Cattaneo, D; Clementi, E; Cordier, L; Cozzi, V; Fucile, S; Gulisano, C; Merli, S; Orlando, G; Rizzardini, G, 2013
)
1.83
" Clinical success, microbiologic success, and adverse events (AEs) were evaluated."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
" This study of hospitalized patients revealed comparably low frequencies of adverse events potentially related to ST among patients who received linezolid or vancomycin."( Comparative evaluation of serotonin toxicity among veterans affairs patients receiving linezolid and vancomycin.
Lazariu, V; Lodise, TP; McNutt, LA; Patel, N; Rivera, A; Tristani, L; Vandewall, H, 2013
)
0.81
" Myelosuppression and monoamine oxidase inhibition (MAOI) are key independent causes for limiting adverse effects in therapy with the sole approved drug of this class, linezolid."( New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
Gordeev, MF; Yuan, ZY, 2014
)
0.6
" Treatment with linezolid was not associated with more adverse effects in general (OR = 0."( Efficacy and safety of linezolid for the treatment of infections in children: a meta-analysis.
Apostolidou-Kiouti, F; Haidich, AB; Ioannidou, M; Niopas, I; Roilides, E, 2014
)
1.06
" GSK1322322 administration was associated with mild-to-moderate drug-related adverse events, most commonly, nausea, vomiting, diarrhea, and headache."( Safety, tolerability, and efficacy of GSK1322322 in the treatment of acute bacterial skin and skin structure infections.
Corey, R; Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; O'Riordan, WD; Zhu, JZ, 2014
)
0.4
"8%) patients had clinically significant adverse events in the linezolid group, of whom 25 (93%) patients had events that were possibly or probably related to linezolid."( Efficacy, safety and tolerability of linezolid for the treatment of XDR-TB: a study in China.
Gu, J; Hao, X; Lin, F; Liu, G; Liu, X; Liu, Y; Sun, H; Tang, S; Wang, X; Wu, M; Yao, L; Zen, L; Zhang, X; Zhang, Z, 2015
)
0.93
"Linezolid induced black hairy tongue is a rare benign reversible side effect of linezolid therapy."( Linezolid induced black hairy tongue: a rare side effect.
Abdulla, FM; Aijazi, I,
)
3.02
"Oxazolidinone pharmacology including structure-activity relationships, mode of action, pharmacokinetics, drug-drug interactions, and adverse drug reactions is reviewed."( Drug-drug interactions and safety of linezolid, tedizolid, and other oxazolidinones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.69
"Peripheral neuropathy is a common side effect of prolonged treatment with linezolid."( Toxicity to sensory neurons and Schwann cells in experimental linezolid-induced peripheral neuropathy.
Bobylev, I; Joshi, AR; Lehmann, HC; Maru, H, 2016
)
0.91
"0120) and lower incidence of gastrointestinal adverse events (tedizolid: 16."( Efficacy, safety, tolerability and population pharmacokinetics of tedizolid, a novel antibiotic, in Latino patients with acute bacterial skin and skin structure infections.
Cabré-Márquez, JF; Fang, E; Fiedler-Kelly, J; Flanagan, SD; Nannini, EC; Ortiz-Covarrubias, A; Passarell, J; Prokocimer, PG; Tanaka, T; Zhu, X,
)
0.13
"Long-term linezolid use is limited by mitochondrial toxicity-associated adverse events (AEs)."( Linezolid Trough Concentrations Correlate with Mitochondrial Toxicity-Related Adverse Events in the Treatment of Chronic Extensively Drug-Resistant Tuberculosis.
Barry, CE; Cai, Y; Chen, RY; Cho, SN; Dartois, V; Dodd, LE; Follman, D; Goldfeder, LC; Jeon, HS; Lee, M; Olivier, KN; Park, Y; Song, T; Via, LE; Wang, J; Xie, Y, 2015
)
2.26
" The incidence of adverse reactions was similar in the two groups[50."( [A comparison of efficacy and safety of linezolid versus vancomycin for the treatment of infections in patients after allogeneic hematopoietic stem cell transplantation].
Chen, H; Chen, Y; Han, W; Huang, X; Liu, D; Liu, K; Tian, J; Wang, F; Wang, Y; Xu, L; Xu, Z; Yan, C; Zhang, X; Zhang, Y, 2016
)
0.7
" We evaluated the occurrence of outcomes including culture conversion, treatment success and incidence of adverse events such as myelosuppression and neuropathy."( Efficacy and safety profile of linezolid in the treatment of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis: a systematic review and meta-analysis.
Agyeman, AA; Ofori-Asenso, R, 2016
)
0.72
" The incidence of neuropathy and other adverse events leading to permanent discontinuation of linezolid also showed no significance upon dose comparisons (p = 0."( Efficacy and safety profile of linezolid in the treatment of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis: a systematic review and meta-analysis.
Agyeman, AA; Ofori-Asenso, R, 2016
)
0.94
"Available evidence presents Linezolid as a viable option in the treatment of MDR/XDR TB although patients ought to be monitored closely for the incidence of major adverse events such as myelosuppression and neuropathy."( Efficacy and safety profile of linezolid in the treatment of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis: a systematic review and meta-analysis.
Agyeman, AA; Ofori-Asenso, R, 2016
)
1.01
" Adverse event rates were not significantly different between the two groups."( Similar efficacy and safety of daptomycin versus linezolid for treatment of vancomycin-resistant enterococcal bloodstream infections: a meta-analysis.
Chen, D; Ji, L; Liang, L; Patel, K; Zhang, Y; Zhao, M; Zhu, Y, 2016
)
0.69
" While no adverse events were reported for IC, 2 minor side effects, only, were attributed to linezolid (17%); in both cases the drug was re-started without further problems."( Effectiveness and safety of imipenem/clavulanate and linezolid to treat multidrug and extensively drug-resistant tuberculosis at a referral hospital in Brazil.
Arbex, MA; Bonini, EH; Centis, R; D'Ambrosio, L; Kawakame Pirolla, G; Migliori, GB,
)
0.6
" The SAT was interrupted in five cases due to adverse events."( Sequential antimicrobial treatment with linezolid for neurosurgical infections: efficacy, safety and cost study.
Castillo-Ojeda, E; Gil-Navarro, MV; Gómez-Gómez, MJ; Jiménez-Mejías, ME; Márquez-Rivas, FJ; Martín-Gandul, C; Mayorga-Buiza, MJ; Rivero-Garvía, M, 2016
)
0.7
"SAT with linezolid was safe and effective for the treatment of NSI."( Sequential antimicrobial treatment with linezolid for neurosurgical infections: efficacy, safety and cost study.
Castillo-Ojeda, E; Gil-Navarro, MV; Gómez-Gómez, MJ; Jiménez-Mejías, ME; Márquez-Rivas, FJ; Martín-Gandul, C; Mayorga-Buiza, MJ; Rivero-Garvía, M, 2016
)
1.12
" Oral MRX-I was well tolerated at single doses of up to 1,200 and 800 mg q12h for up to 28 days; all adverse events were mild to moderate in severity, and there was no drug discontinuation due to adverse events."( Single- and Multiple-Dose Study To Determine the Safety, Tolerability, Pharmacokinetics, and Food Effect of Oral MRX-I versus Linezolid in Healthy Adult Subjects.
Eckburg, PB; Ge, Y; Hafkin, B, 2017
)
0.66
" Therefore, the objective of this study was to gain an understanding of clinical heterogeneity in response to identical linezolid exposures through exhaustive examination of the molecular basis of tissue-dependent mitotoxicity, consequent cell dysfunction, and the association of mitochondrial genetics with adverse effects of linezolid administered for the recommended period."( Influence of Mitochondrial Genetics on the Mitochondrial Toxicity of Linezolid in Blood Cells and Skin Nerve Fibers.
Andreu, AL; Cardellach, F; Casanova-Mollà, J; Catalán-Garcia, M; García-Arumí, E; Garrabou, G; Lozano, E; Mensa, J; Milisenda, JC; Montoya, J; Morales, M; Morén, C; Pacheu-Grau, D; Pinós, T; Ruiz-Pesini, E; Soriano, À, 2017
)
0.9
"Linezolid may cause adverse effects such as thrombocytopenia, which were found to be dependent on receiving linezolid for longer than 2 weeks."( Linezolid-related adverse effects in clinical practice in children.
Bayram, N; Devrim, İ; Düzgöl, M; Kara, A; Özdemir, FM, 2017
)
3.34
" Adverse effects attributed to linezolid and time of occurrence of side effects was evaluated."( Linezolid-related adverse effects in clinical practice in children.
Bayram, N; Devrim, İ; Düzgöl, M; Kara, A; Özdemir, FM, 2017
)
2.18
"1%) patients experienced adverse effects."( Linezolid-related adverse effects in clinical practice in children.
Bayram, N; Devrim, İ; Düzgöl, M; Kara, A; Özdemir, FM, 2017
)
1.9
"Transient adverse effects were detected in 20."( Linezolid-related adverse effects in clinical practice in children.
Bayram, N; Devrim, İ; Düzgöl, M; Kara, A; Özdemir, FM, 2017
)
1.9
"Clinical adverse event (AE) and laboratory data were pooled across completed clinical studies (13 phase 1, two phase 2, and two phase 3), for all participants who received ≥1 dose of tedizolid 200 mg, linezolid 600 mg (phase 3 only), or placebo (phase 1 only)."( Clinical safety and tolerability of tedizolid phosphate in the treatment of acute bacterial skin and skin structure infections.
Anuskiewicz, S; Bidell, M; De Anda, C; Flanagan, S; Hardalo, C; Lodise, TP; Prokocimer, P, 2018
)
0.67
" Both treatments were well tolerated; overall treatment-emergent adverse events (TEAEs) in tedizolid phosphate (79."( Efficacy, safety and pharmacokinetics of tedizolid versus linezolid in patients with skin and soft tissue infections in Japan - Results of a randomised, multicentre phase 3 study.
Iwamoto, Y; Kato, M; Kohno, S; Mikamo, H; Takesue, Y; Tanigawa, T; Tanimura, Y, 2018
)
0.73
" Investigation items were as follows; sex, age, gestational age, birth weight, body weight, duration of treatment, Apgar score, laboratory data, rate of patients with blood transfusion, serum levels of vancomycin, disease type, concomitant medications, clinical isolates, adverse effects during antimicrobial treatment, antimicrobial susceptibility of isolated Gram-positive bacteria."( Comparative study on safety of linezolid and vancomycin in the treatment of infants and neonates for Gram-positive bacterial infections.
Asai, N; Hagihara, M; Kato, H; Koizumi, Y; Matsuura, K; Mikamo, H; Nishiyama, N; Shibata, Y; Suematsu, H; Yamagishi, Y, 2018
)
0.77
" Any adverse events during antimicrobial treatment were admitted in linezolid 46."( Comparative study on safety of linezolid and vancomycin in the treatment of infants and neonates for Gram-positive bacterial infections.
Asai, N; Hagihara, M; Kato, H; Koizumi, Y; Matsuura, K; Mikamo, H; Nishiyama, N; Shibata, Y; Suematsu, H; Yamagishi, Y, 2018
)
1
" If patients present with this triad of symptoms secondary to linezolid therapy, adverse effects should be treated with dextrose and intravenous thiamine while reserving hemodialysis for those with metabolic acidosis refractory to thiamine."( A Case of Linezolid Induced Toxicity.
Gurnani, PK; Hanson, AP; Tobias, PE; Varughese, CA, 2020
)
1.2
"Lefamulin was noninferior to moxifloxacin for the primary efficacy endpoints and was generally safe and well tolerated."( Efficacy and Safety of Intravenous-to-oral Lefamulin, a Pleuromutilin Antibiotic, for the Treatment of Community-acquired Bacterial Pneumonia: The Phase III Lefamulin Evaluation Against Pneumonia (LEAP 1) Trial.
Das, A; File, TM; Gasink, LB; Gelone, SP; Goldberg, L; Paukner, S; Saviski, J; Seltzer, E; Sweeney, C; Talbot, GH; Wicha, WW, 2019
)
0.51
" However, among children with MDR-TB, there are no linezolid pharmacokinetic data, and its adverse effects have not yet been prospectively described."( Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies.
Draper, HR; Garcia-Cremades, M; Garcia-Prats, AJ; Hesseling, AC; Savic, RM; Schaaf, HS; Wiesner, L; Winckler, J, 2019
)
1.02
" Adverse events were assessed for severity and attribution to linezolid."( Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies.
Draper, HR; Garcia-Cremades, M; Garcia-Prats, AJ; Hesseling, AC; Savic, RM; Schaaf, HS; Wiesner, L; Winckler, J, 2019
)
1.01
"Linezolid-related adverse effects were frequent and occasionally severe."( Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies.
Draper, HR; Garcia-Cremades, M; Garcia-Prats, AJ; Hesseling, AC; Savic, RM; Schaaf, HS; Wiesner, L; Winckler, J, 2019
)
2.21
"Identify the incidence of haematological adverse effects associated with linezolid."( Haematological adverse effects associated with linezolid in patients with drug-resistant tuberculosis: an exploratory study.
Gaida, R; Kamau, H; Letswee, G; Truter, I, 2019
)
1
"Approximately a quarter (n = 7) of patients experienced haematological adverse effects."( Haematological adverse effects associated with linezolid in patients with drug-resistant tuberculosis: an exploratory study.
Gaida, R; Kamau, H; Letswee, G; Truter, I, 2019
)
0.77
" Haematological monitoring should be done monthly in order to detect adverse effects timeously and intervene as appropriate."( Haematological adverse effects associated with linezolid in patients with drug-resistant tuberculosis: an exploratory study.
Gaida, R; Kamau, H; Letswee, G; Truter, I, 2019
)
0.77
"Drug adverse events (AEs), or called adverse drug events (ADEs), are ranked one of the leading causes of mortality."( ODAE: Ontology-based systematic representation and analysis of drug adverse events and its usage in study of adverse events given different patient age and disease conditions.
Garg, N; He, Y; Nysak, S; Ong, E; Ye, X; Yu, H; Zhang, X, 2019
)
0.51
" To logically represent the complex relations among drug, drug ingredient and mechanism of action, AE, age, disease, and other related factors, an ontology design pattern was developed and applied to generate a community-driven open-source Ontology of Drug Adverse Events (ODAE)."( ODAE: Ontology-based systematic representation and analysis of drug adverse events and its usage in study of adverse events given different patient age and disease conditions.
Garg, N; He, Y; Nysak, S; Ong, E; Ye, X; Yu, H; Zhang, X, 2019
)
0.51
" In addition, potentially toxic concentrations and treatment discontinuation due to overexposure and hematological toxicity were also more frequently seen in cirrhotic patients."( Linezolid Dosing in Patients With Liver Cirrhosis: Standard Dosing Risk Toxicity.
Álvarez-Lerma, F; Campillo, N; Echeverría-Esnal, D; González-Colominas, E; Grau, S; Horcajada, JP; Luque, S; Martínez-Casanova, J; Muñoz-Bermudez, R; Roberts, JA; Sorli, L, 2019
)
1.96
"Thrombocytopenia may be a dose-dependent adverse effect of linezolid therapy."( Proactive therapeutic drug monitoring (TDM) may be helpful in managing long-term treatment with linezolid safely: findings from a monocentric, prospective, open-label, interventional study.
Bassetti, M; Cojutti, PG; Merelli, M; Pea, F, 2019
)
0.98
"Of the 31 patients, 13 (42%) had suspected or confirmed adverse events (AEs) related to LNZ treatment, including digestive symptoms, haematological toxicity, neuropathy and lactic acidosis."( Safety of longer linezolid regimen in children with drug-resistant tuberculosis and extensive tuberculosis in Southwest China.
Chen, J; Cheng, Z; Fu, Z; Jiang, L; Liu, Q; Shang, T; Wang, X; Xu, H; Zhang, Z; Zhu, K, 2020
)
0.9
" These drugs are associated with numerous adverse events that can cause severe morbidity, such as deafness, and in some instances can lead to death."( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis.
Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020
)
0.56
"We did a meta-analysis using individual-level patient data that were obtained from studies that reported adverse events that resulted in permanent discontinuation of anti-tuberculosis medications."( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis.
Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020
)
0.56
" Using meta-analysis of proportions, drugs with low risks of adverse event occurrence leading to permanent discontinuation included levofloxacin (1·3% [95% CI 0·3-5·0]), moxifloxacin (2·9% [1·6-5·0]), bedaquiline (1·7% [0·7-4·2]), and clofazimine (1·6% [0·5-5·3])."( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis.
Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020
)
0.56
"Fluoroquinolones, clofazimine, and bedaquiline had the lowest incidence of adverse events leading to permanent drug discontinuation, whereas second-line injectable drugs, aminosalicylic acid, and linezolid had the highest incidence."( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis.
Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020
)
0.75
" Adverse events such as hematological toxicity of linezolid, neurotoxicity of metronidazole, nitrofurantoin pulmonary toxicity or even risk of aortic aneurysm from fluoroquinolones require cautious use and an individualized assessment of the risk-benefit."( [Side effects of selected antibiotics, not to be missed !]
Boillat-Blanco, N; Huttner, B; Kritikos, A; Zanella, MC, 2020
)
0.81
" An important side effect of linezolid is linezolid-induced thrombocytopenia; so, the safety of linezolid for AML patients in myelosuppression is of concern."( Linezolid is safe on platelet count for AML patients during myelosuppression after consolidation chemotherapy.
Shi, T; Xie, W; Yang, X; Ye, X; Zhao, S; Zhu, J; Zhu, L, 2020
)
2.29
"This retrospective clinical study suggests that it is safe to manage AML patients in complete remission during myelosuppression after standard consolidation chemotherapy with idarubicin and cytarabine, with about 7 days of linezolid therapy."( Linezolid is safe on platelet count for AML patients during myelosuppression after consolidation chemotherapy.
Shi, T; Xie, W; Yang, X; Ye, X; Zhao, S; Zhu, J; Zhu, L, 2020
)
2.19
" To rule out toxic levels during the therapy, plasma and cerebro-spinal fluid concentrations of linezolid were measured and reported."( Staphylococcal meningitis therapy with linezolid in a young infant: efficacy, CSF levels and side effects.
Amante, PG; Auriti, C; Bersani, I; Cairoli, S; Goffredo, BM; Longo, D; Piersigilli, F, 2020
)
1.05
"Linezolid is one of the most effective drugs for treating multidrug-resistant tuberculosis (MDR TB), but adverse effects remain problematic."( Linezolid-Associated Neurologic Adverse Events in Patients with Multidrug-Resistant Tuberculosis, France.
Bodaghi, B; Butel, N; Caumes, E; El Helali, N; Flandre, P; Guillot, H; Jaspard, M; Marigot-Outtandy, D; Petitjean, G; Peytavin, G; Pourcher, V; Veziris, N, 2020
)
3.44
" Incidences of treatment-emergent adverse events (TEAEs) were similar between treatment groups and between IV (20."( Efficacy and Safety of a Novel Broad-Spectrum Anti-MRSA Agent Levonadifloxacin Compared with Linezolid for Acute Bacterial Skin and Skin Structure Infections: A Phase 3, Openlabel, Randomized Study.
Bhagwat, S; Bhatia, A; Chavan, R; Friedland, HD; Gutte, R; Joshi, P; Kumbhar, D; Llorens, L; Mastim, M; Palwe, SR; Patel, M; Periasamy, H; Shah, M, 2020
)
0.78
" Levonadifloxacin is safe and well tolerated in the treatment of ABSSSI caused by Gram -positive pathogens including MRSA as well as non-inferior to IV and oral linezolid, respectively."( Efficacy and Safety of a Novel Broad-Spectrum Anti-MRSA Agent Levonadifloxacin Compared with Linezolid for Acute Bacterial Skin and Skin Structure Infections: A Phase 3, Openlabel, Randomized Study.
Bhagwat, S; Bhatia, A; Chavan, R; Friedland, HD; Gutte, R; Joshi, P; Kumbhar, D; Llorens, L; Mastim, M; Palwe, SR; Patel, M; Periasamy, H; Shah, M, 2020
)
0.97
"Lactic acidosis (LA) is a rare but potentially lethal side effect of linezolid (LZD)."( Linezolid and the risk of lactic acidosis: Data mining and analysis of the FDA Adverse Event Reporting System.
Dai, Y; Shi, D; Wang, Y; Zeng, Y; Zhang, C; Zhou, Z, 2020
)
2.24
"We evaluated the association between LZD and LA using the reporting odd ratio (ROR) for mining the adverse event report signals in the FDA Adverse Event Reporting System database from January 2013 to December 2019."( Linezolid and the risk of lactic acidosis: Data mining and analysis of the FDA Adverse Event Reporting System.
Dai, Y; Shi, D; Wang, Y; Zeng, Y; Zhang, C; Zhou, Z, 2020
)
2
" While no adverse effect of LZ was seen in the control corneas, 66-100% of rabbits showed reaction to AZ and TG."( Linezolid shows high safety and efficacy in the treatment of Pythium insidiosum keratitis in a rabbit model.
Ahirwar, LK; Bagga, B; Das, S; Kalra, P; Mittal, R; Mohamed, A; Sharma, S, 2021
)
2.06
" Three patients (12%) experienced serious adverse events, of which in two cases were possibly related to TB drugs in the regimen."( Effectiveness and safety of fully oral modified shorter treatment regimen for multidrug-resistant tuberculosis in Georgia, 2019-2020.
Ahmedov, S; Avaliani, T; Davtyan, H; Denisiuk, O; Gozalov, O; Hovhannesyan, A; Kiria, N; Sereda, Y; Togonidze, T; Tukvadze, N, 2021
)
0.62
"BackgroundTo investigate the adverse event (AE) profile of tedizolid and linezolid in post-marketing surveillance."( Serious adverse events with tedizolid and linezolid: pharmacovigilance insights through the FDA adverse event reporting system.
De Ponti, F; Fusaroli, M; Gatti, M; Moretti, U; Poluzzi, E; Raschi, E, 2021
)
1.12
"67%) patients had at least one serious adverse event."( Early safety and efficacy of linezolid-based combination therapy among patients with drug-resistant tuberculosis in North-western Nigeria.
Ahmad, BG; Dayyab, FM; Habib, AG; Iliyasu, G,
)
0.42
" Severe anemia and thrombocytopenia were defined as ≥ grade 3 adverse events according to the NIAID Division of Microbiology and Infectious Disease Adult Toxicity table."( Proposed Linezolid Dosing Strategies to Minimize Adverse Events for Treatment of Extensively Drug-Resistant Tuberculosis.
Conradie, F; Imperial, MZ; Nedelman, JR; Savic, RM, 2022
)
1.14
"Multicentre (16 countries), prospective, observational study reporting incidence and frequency of clinically relevant adverse events of special interest (AESIs) among patients who received MDR/RR-TB treatment containing bedaquiline and/or delamanid."( Safety of Treatment Regimens Containing Bedaquiline and Delamanid in the endTB Cohort.
Adenov, M; Adnan, S; Ahmed, S; Bastard, M; Coutisson, S; Danielyan, N; Franke, MF; Hewison, C; Huerga, H; Islam, S; Janmohamed, A; Kamene Kimenye, M; Karakozian, H; Khan, P; Khan, U; Kholikulov, B; Kirakosyan, O; Krisnanda, A; Kumsa, A; Lachenal, N; Leblanc, G; Lecca, L; Mamsa, S; Melikyan, N; Mitnick, CD; Nkuebe, M; Osso, E; Padayachee, S; Rich, ML; Seung, KJ; Thit, P; Varaine, F, 2022
)
0.72
" Adverse events are a concern to prescribers but have not been systematically studied at the standard dose, and the relationship between linezolid exposure and clinical toxicity is not completely elucidated."( Linezolid toxicity in patients with drug-resistant tuberculosis: a prospective cohort study.
Abdelwahab, MT; Brust, JCM; Denti, P; Gandhi, NR; Little, F; Maartens, G; Meintjes, G; Wasserman, S; Wiesner, L, 2022
)
2.37
" Grade 3 or 4 linezolid-associated adverse events occurred in 21 (14%) participants."( Linezolid toxicity in patients with drug-resistant tuberculosis: a prospective cohort study.
Abdelwahab, MT; Brust, JCM; Denti, P; Gandhi, NR; Little, F; Maartens, G; Meintjes, G; Wasserman, S; Wiesner, L, 2022
)
2.52
" All serious adverse events and adverse events of special interest (AESI), leading to a treatment change, or judged significant by a clinician, were systematically monitored and documented."( Safety and Effectiveness Outcomes From a 14-Country Cohort of Patients With Multi-Drug Resistant Tuberculosis Treated Concomitantly With Bedaquiline, Delamanid, and Other Second-Line Drugs.
Ahmed, S; Bastard, M; Franke, MF; Grium Tefera, D; Hewison, C; Holtzman, D; Huerga, H; Islam, S; Jacques Leblanc, G; Khan, PY; Khan, U; Kumsa, A; Lachenal, N; Leonovich, O; Mamsa, S; Manzur-Ul-Alam, M; Melikyan, N; Mitnick, CD; Myint, Z; Osso, E; Padayachee, S; Rafi Siddiqui, M; Rashitov, M; Rich, ML; Salahuddin, N; Salia, G; Sánchez, E; Serobyan, A; Seung, KJ; Varaine, F; Vetushko, D; Yeghiazaryan, L, 2022
)
0.72
"Concomitant use of Bdq and Dlm, along with linezolid and clofazimine, is safe and effective for MDR/RR-TB patients with extensive disease."( Safety and Effectiveness Outcomes From a 14-Country Cohort of Patients With Multi-Drug Resistant Tuberculosis Treated Concomitantly With Bedaquiline, Delamanid, and Other Second-Line Drugs.
Ahmed, S; Bastard, M; Franke, MF; Grium Tefera, D; Hewison, C; Holtzman, D; Huerga, H; Islam, S; Jacques Leblanc, G; Khan, PY; Khan, U; Kumsa, A; Lachenal, N; Leonovich, O; Mamsa, S; Manzur-Ul-Alam, M; Melikyan, N; Mitnick, CD; Myint, Z; Osso, E; Padayachee, S; Rafi Siddiqui, M; Rashitov, M; Rich, ML; Salahuddin, N; Salia, G; Sánchez, E; Serobyan, A; Seung, KJ; Varaine, F; Vetushko, D; Yeghiazaryan, L, 2022
)
0.98
" The frequency of treatment-emergent adverse events was comparable between the two groups."( A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections.
Huang, H; Yuan, H; Yuan, Z; Zhang, Y; Zhao, X, 2022
)
0.93
" All patients had normal hepatic and renal function, and no statistical difference of adverse effects between 2 groups were found."( Analysis of efficacy and safety of linezolid-based chemotherapeutic regimens for patients with postoperative multidrug-resistant spinal tuberculosis.
Dai, X; Feng, J; Qiao, J; Xia, P; Xu, F; Yang, L, 2022
)
1
"Linezolid-based chemotherapeutic regimens can effectively treat patients with postoperative multidrug-resistant spinal tuberculosis but have higher rates of adverse reactions."( Analysis of efficacy and safety of linezolid-based chemotherapeutic regimens for patients with postoperative multidrug-resistant spinal tuberculosis.
Dai, X; Feng, J; Qiao, J; Xia, P; Xu, F; Yang, L, 2022
)
2.44
" A shorter, less toxic and more efficacious regimen would improve outcomes for people with rifampicin-resistant tuberculosis."( TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tubercul
Berry, C; du Cros, P; Fielding, K; Gajewski, S; Kazounis, E; McHugh, TD; Merle, C; Moore, DAJ; Motta, I; Nyang'wa, BT, 2022
)
0.72
"TB-PRACTECAL is an ambitious trial using adaptive design to accelerate regimen assessment and bring novel treatments that are effective and safe to patients quicker."( TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tubercul
Berry, C; du Cros, P; Fielding, K; Gajewski, S; Kazounis, E; McHugh, TD; Merle, C; Moore, DAJ; Motta, I; Nyang'wa, BT, 2022
)
0.72
"Treatment of multidrug-resistant (MDR) tuberculosis with linezolid is characterized by high rates of adverse events."( Association Between Increased Linezolid Plasma Concentrations and the Development of Severe Toxicity in Multidrug-Resistant Tuberculosis Treatment.
Caumes, E; Eimer, J; El-Helali, N; Fréchet-Jachym, M; Guglielmetti, L; Le Dû, D; Marigot-Outtandy, D; Mechai, F; Peytavin, G; Pourcher, V; Rioux, C; Robert, J; Yazdanpanah, Y, 2023
)
1.44
" Safety outcomes included assessment of treatment-emergent adverse events."( Efficacy and safety of tedizolid for the treatment of ventilated gram-positive hospital-acquired or ventilator-associated bacterial pneumonia in Japanese patients: Results from a subgroup analysis of a phase 3, randomized, double-blind study comparing ted
De Anda, C; Fujimi, S; Kusachi, S; Mikamo, H; Nagashima, M; Oshima, N; Takase, A, 2022
)
0.72
"We investigated adverse events in patients with prosthetic joint infections receiving combination therapy with linezolid, rifampicin, and clindamycin for ≥ 7 days."( Safety of linezolid, rifampicin, and clindamycin combination therapy in patients with prosthetic joint infection.
Kitaoka, A; Kobayashi, S; Ogura, T; Tagawa, S; Yasu, T, 2022
)
1.34
" The trial results will help establish evidence towards a safe and effective dose of LZD that can be used in a fully, all-oral short course regimen for highly DR-TB patients."( Randomised trial to evaluate the effectiveness and safety of varying doses of linezolid with bedaquiline and pretomanid in adults with pre-extensively drug-resistant or treatment intolerant/non-responsive multidrug-resistant pulmonary tuberculosis: study
Devaleenal, B; Mandal, S; Mattoo, S; Padmapriyadarsini, C; Parmar, M; Ponnuraja, C; Ramraj, B; Singla, R, 2022
)
0.95
" Meanwhile, the types and incidence of adverse effects associated with LZD were evaluated."( Linezolid-related adverse effects in the treatment of rifampicin resistant tuberculosis: a retrospective study.
Chen, G; Cui, D; Hu, X; Shi, L; Wang, D, 2023
)
2.35
"Adverse event reports of QT interval prolongation associated with LZD from the Food and Drug Administration Adverse Event Reporting System from January 2013 to December 2021 were analysed and the reporting odds ratio (ROR) with 95% confidence intervals were calculated."( Linezolid and the risk of QT interval prolongation: A pharmacovigilance study of the Food and Drug Administration Adverse Event Reporting System.
Dai, Y; Shao, H; Shi, D, 2023
)
2.35
"A total of 6738 adverse event reports of LZD as the primary and secondary suspected drug were obtained from the database, including 192 reports with electrocardiogram QT prolonged (QTp), and the ROR value was 26."( Linezolid and the risk of QT interval prolongation: A pharmacovigilance study of the Food and Drug Administration Adverse Event Reporting System.
Dai, Y; Shao, H; Shi, D, 2023
)
2.35
" Of 106 evaluated, 95 (90%) were successfully treated, six (6%) were lost-to-follow-up, one (1%) died, and four (4%) had treatment failure, including three with permanent regimen change owing to adverse events (AE) and one with culture reversion."( Effectiveness and safety of bedaquiline-based, modified all-oral 9-11-month treatment regimen for rifampicin-resistant tuberculosis in Vietnam.
Decroo, T; Hoang, TTT; Le, THM; Merle, CSC; Nguyen, BH; Nguyen, NL; Nguyen, TMP; Nguyen, VN; Pedrazzoli, D, 2023
)
0.91
"4:1:1) to 3 treatment arms (1, standard of care [SOC]; 2, SOC + additional rifampicin [up to 35 mg/kg/d] + linezolid 1200 mg/d reducing after 28 days to 600 mg/d; 3, as per arm 2 + aspirin 1000 mg/d) for 56 days, when the primary outcome of adverse events of special interest (AESI) or death was assessed."( A Phase 2A Trial of the Safety and Tolerability of Increased Dose Rifampicin and Adjunctive Linezolid, With or Without Aspirin, for Human Immunodeficiency Virus-Associated Tuberculous Meningitis: The LASER-TBM Trial.
Aziz, S; Banderker, IA; Black, J; Bremer, M; Candy, S; Crede, T; Daroowala, R; Davis, AG; Denti, P; Goliath, R; Jackson, A; Jason Liang, C; Kadernani, Y; Koekemoer, S; Lai Sai, L; Lai, RPJ; Maartens, G; Maxebengula, M; Meintjes, G; Moosa, MS; Naude, J; Offiah, C; Raubenheimer, P; Sihoyiya, T; Stegmann, S; Stek, C; Szymanski, P; Vallie, Y; Vorster, I; Wahl, G; Wasserman, S; Wilkinson, RJ, 2023
)
1.34
"Rifampicin-resistant tuberculosis (RR-TB) treatment requires combination treatment, which frequently causes serious adverse events and globally results in not much more than 60% treatment success."( Safety, effectiveness, and adherence of a short and all-oral treatment regimen for the treatment of rifampicin-resistant tuberculosis in Niger: a study protocol of a pragmatic randomised clinical trial with stratified block randomisation.
Adehossi, E; Decroo, T; Gagara-Issoufou, A; Halidou-Moussa, S; Mamadou, S; Maman Lawan, I; Ortuño-Gutiérrez, N; Piubello, A; Souleymane, MB; Soumana, A; Van Deun, A, 2022
)
0.72
" The extracted studies were included in a single-rate meta-analysis of adverse events and clinical outcomes using random-effects models."( Safety and clinical efficacy of linezolid in children: a systematic review and meta-analysis.
Cai, K; Huang, HY; Huang, LS; Li, S; Shi, Y; Wu, HL; Wu, YH; Xu, SS; Yu, XB; Zhang, CH; Zhang, J; Zhang, LY, 2023
)
1.19
"Linezolid was well-tolerated in pediatric patients and was associated with a low frequency of adverse events, such as anemia, thrombocytopenia, and neutropenia."( Safety and clinical efficacy of linezolid in children: a systematic review and meta-analysis.
Cai, K; Huang, HY; Huang, LS; Li, S; Shi, Y; Wu, HL; Wu, YH; Xu, SS; Yu, XB; Zhang, CH; Zhang, J; Zhang, LY, 2023
)
2.64
" Hence, before such treatments could advance into clinical usage, it is paramount to identify appropriate levels of topical ozone that are effective in treating bacterial infections and safe for use in topical administration."( Biocompatibility and Safety Assessment of Combined Topical Ozone and Antibiotics for Treatment of Infected Wounds.
Chen, YX; Cox, AD; Hopf Jannasch, AS; Krishnakumar, A; Maruthamuthu, MK; McCain, RR; McIntosh, M; Nguyen, J; Rahimi, R; Roth, A; Seleem, MN, 2023
)
0.91
"Linezolid is an effective, but toxic anti-tuberculosis drug that is currently recommended for the treatment of drug-resistant tuberculosis."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
2.35
"DECODE is an innovative dose-finding trial, designed to support exposure-response modelling for safe and effective dose selection."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91
" Nephrotoxicity is a common side effect of aminoglycosides used in the management of actinomycetoma."( Linezolid: a safer and effective substitute to aminoglycoside in the treatment of actinomycetoma by Nocardia species.
Chhabra, N; Ganguly, S; Sri, P, 2023
)
2.35
" Toxicity relevance was classified according to Common Terminology Criteria for Adverse Events v5."( Influence of augmented renal clearance on the lower incidence of linezolid-related hematological toxicity.
Caro-Teller, JM; Ferrari-Piquero, JM; Gonzalez-Barrios, I; Hernández-Ramos, JA; Rodríguez-Quesada, PP; Sánchez-Sanz, B,
)
0.37
" Toxicity relevance was classified according to Common Terminology Criteria for Adverse Events v5."( [Translated article] Influence of augmented renal clearance in the lower incidence of linezolid-related haematological toxicity.
Caro-Teller, JM; Ferrari-Piquero, JM; González-Barrios, I; Hernández-Ramos, JA; Rodríguez-Quesada, PP; Sánchez-Sanz, B,
)
0.35
" Linezolid may be a good option for treating bone and joint infections, but there is an increased risk of potential serious adverse drug events (ADEs) when used for more than 28 days."( Prolonged use of linezolid in bone and joint infections: a retrospective analysis of adverse effects.
Goosen, J; Heesterbeek, P; Jager, N; Spijkers, K; Telgt, D; Veerman, K, 2023
)
2.16
" Severe cytopenia, according to the Common Terminology Criteria for Adverse events (CTCA), was observed in four patients and was reversible after discontinuation of linezolid."( Prolonged use of linezolid in bone and joint infections: a retrospective analysis of adverse effects.
Goosen, J; Heesterbeek, P; Jager, N; Spijkers, K; Telgt, D; Veerman, K, 2023
)
1.45
" The effectiveness, safety, antibiotic susceptibility profiles, outcomes, culture conversion, cavity closure, and adverse reactions were compared in these two groups."( Effectiveness and safety of regimens containing linezolid for treatment of Mycobacterium abscessus pulmonary Disease.
Cao, J; Cheng, LP; Lou, H; Qu, QR; Sha, W; Shen, XN; Sun, Q; Wei, W; Zhang, Q, 2023
)
1.17

Pharmacokinetics

The aim of the study was to assess the biliary penetration of linezolid and the probabilities of attaining optimal pharmacodynamic exposure against vancomycin-resistant enterococci in the bile of liver transplant (LTx) patients. The purpose was to describe the pharmacokinetic profile and determine the level of penetration oflinezolid into healthy thigh tissue.

ExcerptReferenceRelevance
" Pharmacokinetic data demonstrate that coadministration of linezolid and aztreonam does not alter the disposition of either agent under single-dose conditions."( A pharmacokinetic evaluation of concomitant administration of linezolid and aztreonam.
Hopkins, NK; Jungbluth, GL; Sisson, TL, 1999
)
0.79
" A mean peak concentration in plasma of 18."( Pharmacokinetics and tissue penetration of linezolid following multiple oral doses.
Andrews, J; Ashby, J; Ellis, R; Gee, T; Marshall, G; Wise, R, 2001
)
0.57
" The authors present data evaluating the pharmacokinetic and pharmacodynamic responses to coadministration of oral linezolid with sympathomimetics (pseudoephedrine and phenylpropanolamine) and a serotonin reuptake inhibitor (dextromethorphan)."( Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr.
Antal, EJ; Batts, DH; Hendershot, PE; Hopkins, NK; Welshman, IR, 2001
)
1.96
" Pharmacokinetic parameters were assessed using noncompartmental methods."( Age and sex effects on the pharmacokinetics of linezolid.
Hopkins, NK; Jungbluth, GL; Sisson, TL, 2002
)
0.57
" The pharmacodynamic activity and in vivo efficacy of linezolid were compared to those of ceftriaxone in an immunocompetent rat model of pneumococcal pneumonia."( Pharmacodynamic activity and efficacy of linezolid in a rat model of pneumococcal pneumonia.
Gentry-Nielsen, MJ; Olsen, KM; Preheim, LC, 2002
)
0.83
"In this study, our objective was to determine the steady-state intrapulmonary concentrations and pharmacokinetic parameters of orally administered linezolid in healthy volunteers."( Intrapulmonary pharmacokinetics of linezolid.
Conte, JE; Golden, JA; Kipps, J; Zurlinden, E, 2002
)
0.79
" There were no significant differences in terminal elimination half-life between days 1 and 7 (9."( Single- and multiple-dose pharmacokinetics of linezolid and co-amoxiclav in healthy human volunteers.
Borner, K; Burkhardt, O; Köppe, P; Lode, H; Nord, CE; Pletz, MW; von der Höh, N, 2002
)
0.57
" Of the patient covariates considered (age, sex, ideal body weight, baseline serum albumin, hepatic or renal dysfunction, underlying malignancy, organ transplantation, surgical status, global severity of illness, site of infection, route of administration, and location of care [intensive-care unit, general floor, or outpatient]), only normalized creatinine clearance (CL(CR)) and body weight explained significant portions of the variance and were incorporated into the pharmacokinetic model."( Population pharmacokinetics of linezolid in patients treated in a compassionate-use program.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.6
" The plasma-ear fluid pharmacodynamic profile associated with linezolid efficacy was a T>MIC of >/=42%, a C(max)/MIC ratio of >/=3."( Pharmacokinetics and efficacy of linezolid in a gerbil model of Streptococcus pneumoniae-induced acute otitis media.
Biermacher, JJ; Humphrey, WR; Jensen, JL; Kuo, MS; Richards, IM; Schaadt, RD; Shattuck, MH; Smith, DP; Zielinski, RJ; Zurenko, GE, 2003
)
0.84
" Non-compartmental pharmacokinetic analyses were used to describe the disposition of linezolid."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.77
" Mean clearance, half-life and volume of distribution were similar irrespective of dose for both the oral and intravenous routes."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.55
" Plasma samples for population pharmacokinetic analysis were collected."( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
0.58
"Potential alternatives, including linezolid, adjunctive rifampin, and moxifloxacin, were evaluated against vancomycin-tolerant (P9802-020) and vancomycin-susceptible clinical isolates of Streptococcus pneumoniae in an in vitro pharmacodynamic model."( Linezolid and vancomycin, alone and in combination with rifampin, compared with moxifloxacin against a multidrug-resistant and a vancomycin-tolerant Streptococcus pneumoniae strain in an in vitro pharmacodynamic model.
Cha, R; Rybak, MJ, 2003
)
2.04
" Serial blood samples for assessment of the pharmacokinetic parameters of linezolid and its two inactive metabolites were collected on days 1 and 8, whereas vitamin concentrations were measured prior to and after the vitamin intake on these days."( The pharmacokinetics of linezolid are not affected by concomitant intake of the antioxidant vitamins C and E.
Antal, EJ; Francom, SF; Gordi, T; Hong, C; Hopkins, NJ; Slatter, JG; Tan, LH, 2003
)
0.86
" Therefore it is important to determine the specific pharmacokinetic characteristics for individual drugs in pediatric patients so that appropriate age-specific dosage regimens can be developed and evaluated in clinical trials."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
1.76
" Children younger than 12 years of age have a smaller area under the drug concentration-time curve, a faster clearance and a shorter elimination half-life than adults."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
1.76
" The elimination half-life of linezolid is 5-7 hours, and twice-daily administration of 400-600 mg provides steady-state concentrations in the therapeutic range."( Clinical pharmacokinetics of linezolid, a novel oxazolidinone antibacterial.
Jungbluth, GL; Stalker, DJ, 2003
)
0.9
" aureus (VRSA), an in vitro pharmacodynamic model with simulated endocardial vegetations incorporating protein and a high inoculum was used to simulate daptomycin, linezolid, quinupristin-dalfopristin, and vancomycin against the Michigan VRSA strain."( Bactericidal activities of daptomycin, quinupristin-dalfopristin, and linezolid against vancomycin-resistant Staphylococcus aureus in an in vitro pharmacodynamic model with simulated endocardial vegetations.
Brown, WJ; Cha, R; Rybak, MJ, 2003
)
0.75
" Plasma concentrations were obtained and a multicompartmental pharmacokinetic model was fitted."( Clinical pharmacodynamics of linezolid in seriously ill patients treated in a compassionate use programme.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.61
"Modelled pharmacodynamic outcomes of efficacy included probabilities of eradication and clinical cure (multifactorial logistic regression, nonparametric tree-based modelling, nonlinear regression) and time to bacterial eradication (Kaplan-Meier and Cox proportional hazards regression)."( Clinical pharmacodynamics of linezolid in seriously ill patients treated in a compassionate use programme.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.61
" Pharmacokinetic parameters were estimated using standard noncompartmental methods."( Linezolid pharmacokinetics in adult patients with cystic fibrosis.
Bosso, JA; Flume, PA; Gray, SL, 2004
)
1.77
"To compare the pharmacodynamic profiles of linezolid, levofloxacin, and vancomycin against clinical strains of Streptococcus pneumoniae, including vancomycin-tolerant and fluoroquinolone-resistant isolates."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
2.02
"In vitro pharmacodynamic model."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
1.76
"An in vitro pharmacodynamic model was used to simulate standard dosing regimens of linezolid, levofloxacin, and vancomycin against the isolates 79, R921, and P9802-020."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
1.99
" Allometric scaling has previously been used as an effective tool for the prediction of human pharmacokinetic data."( Prediction of clinical pharmacokinetic parameters of linezolid using animal data by allometric scaling: applicability for the development of novel oxazolidinones.
Bhamidipati, RK; Dravid, PV; Mullangi, R; Srinivas, NR, 2004
)
0.57
"To determine the pharmacokinetic characteristics of linezolid and teicoplanin in critically ill patients."( Pharmacokinetic studies of linezolid and teicoplanin in the critically ill.
Aarons, L; Cepeda, JA; Kibbler, C; MacGowan, A; Nalda-Molina, R; Shaw, S; Shulman, R; Singer, M; Tobin, C; Whitehouse, T; Wilson, AP, 2005
)
0.88
"The aim of this study was to compare the activity of linezolid and vancomycin in an in vitro pharmacodynamic model to assess potential differences in activity against biofilm-embedded organisms."( Antibacterial activity of linezolid and vancomycin in an in vitro pharmacodynamic model of gram-positive catheter-related bacteraemia.
Coyle, EA; Lewis, RE; Prince, RA; Raad, II; Wiederhold, NP, 2005
)
0.88
"Single-lumen central venous catheters colonized with biofilm-embedded Staphylococcus aureus, Staphylococcus epidermidis or vancomycin-resistant Enterococcus faecium (VRE) were treated with simulated clinical dosing regimens of linezolid 600 mg every 12 h or vancomycin 1 g every 12 h in a one-compartment in vitro pharmacodynamic model."( Antibacterial activity of linezolid and vancomycin in an in vitro pharmacodynamic model of gram-positive catheter-related bacteraemia.
Coyle, EA; Lewis, RE; Prince, RA; Raad, II; Wiederhold, NP, 2005
)
0.81
"To determine the steady-state plasma pharmacokinetic variables and epithelial lining fluid concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia."( Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC; Toutain, J, 2005
)
0.79
" After 2 days of therapy, the steady-state plasma pharmacokinetic variables and epithelial lining fluid concentrations of linezolid were determined by high-performance liquid chromatography."( Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC; Toutain, J, 2005
)
0.78
" Pharmacokinetic parameters derived from noncompartmental and compartmental analysis incorporating linear and nonlinear elimination pathways were compared between groups: F, Ka, Vs, K23, K32, Vmax, Km, and K20 (bioavailability, absorption rate constant, volume of central compartment normalized to body weight, intercompartmental rate constants, maximum velocity, Michaelis-Menten constant, and elimination rate constant, respectively)."( Absolute bioavailability and pharmacokinetics of linezolid in hospitalized patients given enteral feedings.
Beringer, P; Gill, M; Gurevitch, M; Hoem, N; Louie, S; Nguyen, M; Wong-Beringer, A, 2005
)
0.58
" Aqueous and serum levels of linezolid were assayed by high performance liquid chromatography, and a pharmacokinetic curve constructed from the pooled results."( The pharmacokinetics of linezolid in the non-inflamed human eye.
Jenkins, DR; Lovering, A; Prydal, JI; Watts, A, 2005
)
0.93
"Several antibiotics show significant pharmacokinetic interactions when they are given orally concomitantly with antacids."( Lack of pharmacokinetic interaction between linezolid and antacid in healthy volunteers.
Drewe, J; Grunder, G; Krähenbühl, S; Maier, T; Vollenweider, F; Zysset-Aschmann, Y, 2006
)
0.59
"We inoculated an in vitro pharmacodynamic model simultaneously with clinical isolates of methicillin-resistant Staphylococcus aureus and an enterocin-producing enterococcus (vancomycin-resistant Enterococcus faecalis, ampicillin susceptible) at 7 log10 CFU/ml to examine enterocin effects and antimicrobial activity on staphylococci."( Impact of Enterococcus faecalis on the bactericidal activities of arbekacin, daptomycin, linezolid, and tigecycline against methicillin-resistant Staphylococcus aureus in a mixed-pathogen pharmacodynamic model.
Chin, JN; LaPlante, KL; Leuthner, KD; Rybak, MJ, 2006
)
0.56
" Individual compartmental pharmacokinetic (PK) analysis was performed using WinNonlin."( Pharmacokinetics of unbound linezolid in plasma and tissue interstitium of critically ill patients after multiple dosing using microdialysis.
Buerger, C; Dehghanyar, P; Joukhadar, C; Kloft, C; Plock, N, 2006
)
0.63
"The pharmacokinetic profile of linezolid in cerebrospinal fluid (CSF) in five neurointensive care patients with staphylococcal ventriculitis was studied."( Pharmacokinetics of intravenous linezolid in cerebrospinal fluid and plasma in neurointensive care patients with staphylococcal ventriculitis associated with external ventricular drains.
Beer, R; Brenneis, C; Broessner, G; Engelhardt, KW; Georgopoulos, A; Helbok, R; Kaehler, ST; Lackner, P; Pfausler, B; Schmutzhard, E, 2007
)
0.91
" Optimal pharmacokinetic (PK)/pharmacodynamic (PD) indices have been described for the antimicrobial efficacy of linezolid (area under the concentration-time curve over 24 h at steady state divided by the MIC, >100; the cumulative percentage of a 24-h period that the drug concentration exceeds the MIC under steady-state PK conditions, >85)."( Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
Boak, LM; Li, J; Nation, RL; Rayner, CR, 2007
)
0.78
"To compare pharmacodynamic indices and minimal inhibitory concentrations for vancomycin, gatifloxacin, moxifloxacin, linezolid, and combined quinupristin and dalfopristin for historic and current human coagulase-negative staphylococcus (CoNS) endophthalmitis isolates."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.55
" Peak concentration (C(max)) was defined as the maximum attainable aqueous concentration using topical or oral therapy, or both."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
"The objective of this study was to evaluate a physiologically based pharmacokinetic (PBPK) approach for predicting the plasma concentration-time curves expected after intravenous administration of candidate drugs to rodents."( Evaluation of a basic physiologically based pharmacokinetic model for simulating the first-time-in-animal study.
Burton, PS; Crivori, P; Germani, M; Poggesi, I; Rocchetti, M; Smith, ME; Wilson, AG, 2007
)
0.34
" Therefore, a population pharmacokinetic analysis using NONMEM was performed to thoroughly understand the pharmacokinetics of unbound linezolid in plasma."( Does linezolid inhibit its own metabolism? Population pharmacokinetics as a tool to explain the observed nonlinearity in both healthy volunteers and septic patients.
Buerger, C; Joukhadar, C; Kljucar, S; Kloft, C; Plock, N, 2007
)
1.06
" Pharmacodynamic targets included an AUC/MIC >82."( Pharmacodynamic comparison of linezolid, teicoplanin and vancomycin against clinical isolates of Staphylococcus aureus and coagulase-negative staphylococci collected from hospitals in Brazil.
Kiffer, CR; Kuti, JL; Mendes, CM; Nicolau, DP, 2008
)
0.63
" The aim of this study was to assess the feasibility of the microdialysis technique to cancellous bone for single dose pharmacokinetic investigations of the anti-infective linezolid."( Pharmacokinetics of linezolid in bone tissue investigated by in vivo microdialysis.
Arpi, M; Buerger, C; Emmertsen, KJ; Joukhadar, C; Kloft, C; Plock, N; Riegels-Nielsen, P; Stolle, LB, 2008
)
0.86
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"Simulating the average non-protein-bound (free) human serum drug concentration-time profiles for linezolid in an in vitro pharmacodynamic model, we characterized the pharmacodynamic parameter(s) of linezolid predictive of kill and for prevention of resistance in Bacillus anthracis."( Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
Brown, DL; Drusano, GL; Heine, HS; Kim, K; Kinzig-Schippers, M; Liu, W; Louie, A; Sörgel, F; VanScoy, B, 2008
)
0.81
"The aim of this study was to develop an integrated system for in vitro pharmacodynamic modelling of antimicrobials with greater flexibility, easier control and better accuracy than existing in vitro models."( Development of an integrated semi-automated system for in vitro pharmacodynamic modelling.
Berejnaia, O; Conway, D; Giacobbe, RA; Kath, GS; Racine, F; Wang, L; Wismer, MK, 2008
)
0.35
" The system was validated by pharmacokinetic simulations of linezolid 600 mg infusion."( Development of an integrated semi-automated system for in vitro pharmacodynamic modelling.
Berejnaia, O; Conway, D; Giacobbe, RA; Kath, GS; Racine, F; Wang, L; Wismer, MK, 2008
)
0.59
"The aim of the study was to assess the biliary penetration of linezolid and the probabilities of attaining optimal pharmacodynamic exposure against vancomycin-resistant enterococci (VRE) in the bile of liver transplant (LTx) patients who received linezolid for the treatment of multidrug-resistant Gram-positive hospital infections."( Biliary penetration and pharmacodynamic exposure of linezolid in liver transplant patients.
Adani, GL; Baccarani, U; Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Tavio, M; Viale, P, 2009
)
0.84
" Biliary penetration of linezolid was calculated as the ratio between Cmin in bile and in plasma."( Biliary penetration and pharmacodynamic exposure of linezolid in liver transplant patients.
Adani, GL; Baccarani, U; Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Tavio, M; Viale, P, 2009
)
0.91
"83) enabled achievement of optimal theoretical pharmacodynamic exposure against VRE in bile (Cmin>2 mg/L) on all of the occasions."( Biliary penetration and pharmacodynamic exposure of linezolid in liver transplant patients.
Adani, GL; Baccarani, U; Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Tavio, M; Viale, P, 2009
)
0.6
" There are no published pharmacokinetic (PK) and pharmacodynamic (PD) data for linezolid in children with CF."( Pharmacokinetics and pharmacodynamics of linezolid in children with cystic fibrosis.
Ahmad, N; Brown, ME; Jafri, HS; McCracken, GH; Murphey, DK; Prestidge, CB; Salvatore, CM; Sanchez, PJ; Santos, RP; Siegel, JD; Urbancyzk, B, 2009
)
0.85
" Linezolid has a favorable pharmacokinetic profile."( Association of pharmacokinetic and pharmacodynamic aspects of linezolid with infection outcome.
Falagas, ME; Kioumis, I; Vardakas, KZ, 2009
)
1.5
" Non-compartmental analyses were used to describe the pharmacokinetic disposition of linezolid."( Pharmacokinetic evaluation of linezolid in patients with major thermal injuries.
Birraux, G; Bret, P; Hovsepian, L; Le Floch, R; Lovering, AM; Stephanazzi, J; Vinsonneau, C, 2009
)
0.87
"The rational selection of antibiotics for the treatment of meningitis must take into account several criteria, among which their intrinsic activity against the causative bacteria, and their pharmacokinetic and pharmacodynamic properties."( [Pharmacodynamics of antibiotics in CSF: principles and consequences (predictive factors of efficacy)].
Tulkens, PM; Van Bambeke, F,
)
0.13
" Although linezolid has been approved worldwide, the Japanese pharmacokinetic (PK) profile has not been characterized in detail."( Population pharmacokinetic analysis of linezolid in patients with infectious disease: application to lower body weight and elderly patients.
Abe, S; Chiba, K; Cirincione, B; Grasela, TH; Ito, K; Suwa, T, 2009
)
1.02
"In an in vitro pharmacodynamic model, linezolid attenuated the activity of aztreonam and ceftazidime against Escherichia coli."( Evaluating aztreonam and ceftazidime pharmacodynamics with Escherichia coli in combination with daptomycin, linezolid, or vancomycin in an in vitro pharmacodynamic model.
LaPlante, KL; Sakoulas, G, 2009
)
0.84
" TGC displayed linear PK and had a mean half-life of 10."( Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
Banevicius, MA; Crandon, JL; Koomanachai, P; Nicolau, DP; Peng, L, 2009
)
0.35
" The goal of the present study was to develop a general pharmacokinetic (PK)-pharmacodynamic (PD) model that allows the characterization and comparison of the in vitro activities of oxazolidinones, determined in time-kill curve experiments, against MRSA."( Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
Abbanat, D; Barbour, A; Derendorf, H; Manitpisitkul, P; Sabarinath, SN; Schmidt, S; Sha, S, 2009
)
0.35
" The pharmacokinetic parameters, their variability, and possible covariates were analyzed using NONMEM."( Pharmacokinetics of linezolid in septic patients with and without extended dialysis.
Haefeli, WE; Hempel, G; Hoppe-Tichy, T; Lichtenstern, C; Ober, MC; Saleh, S; Schwenger, V; Sonntag, HG; Swoboda, S; Weigand, MA, 2010
)
0.68
" The mean half-life and apparent oral clearance were decreased for the combination treatment compared with linezolid alone."( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism.
Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011
)
0.83
" Pharmacokinetic indices (Cmax, Cmin, Tmax, AUC) were determined for plasma and ventricular fluid (VF) after the first and last doses."( Pharmacokinetics and distribution of linezolid in cerebrospinal fluid in children and adolescents.
Damle, B; Levy, G; Nachman, S; Yogev, R, 2010
)
0.63
"In study 1, after the last dose, the mean Cmax values for plasma and VF were 10."( Pharmacokinetics and distribution of linezolid in cerebrospinal fluid in children and adolescents.
Damle, B; Levy, G; Nachman, S; Yogev, R, 2010
)
0.63
"This open-label, prospective pharmacokinetic study evaluated two doses (300 and 600 mg) of linezolid in MDR-TB patients, who received linezolid as part of their treatment."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
0.82
" The present article reviews the pharmacokinetic properties of vancomycin, linezolid, tigecycline and daptomycin."( Comparison of the pharmacokinetic properties of vancomycin, linezolid, tigecyclin, and daptomycin.
Derendorf, H; Estes, KS, 2010
)
0.83
" Using 603 platelet counts from 45 patients, a PPK/PD analysis with a semimechanistic pharmacodynamic model described the relationship between linezolid exposure and platelet counts quantitatively, and the newly constructed model was validated using external data (776 platelet counts from 60 patients)."( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
0.81
" Single-dose pharmacokinetic studies were conducted in mice for TR-701/700."( In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model.
Drusano, GL; Kulawy, R; Liu, W; Louie, A, 2011
)
0.37
" Population pharmacokinetic analyses were performed by nonlinear mixed-effects modeling using a previously described 2-compartment model with time-dependent clearance inhibition."( Pharmacokinetics of intravenous and oral linezolid in adults with cystic fibrosis.
Keel, RA; Kloft, C; Knauft, RF; Kuti, JL; Muhlebach, M; Nicolau, DP; Pope, JS; Schaeftlein, A, 2011
)
0.64
" This review examines pharmacokinetic data relating to linezolid use in different patient groups (obesity, enteral feeding, renal failure, neonates, and paediatrics) and in different clinical conditions (sepsis syndrome, skin and soft tissue infection, diabetic foot infection, pneumonia, bone and joint infection, infection of the central nervous system, eye infection, and neutropenic sepsis)."( Linezolid pharmacokinetics and pharmacodynamics in clinical treatment.
Dryden, MS, 2011
)
2.06
" The purpose of the current study was to describe the pharmacokinetic profile and determine the level of penetration of linezolid into healthy thigh tissue and infected wound tissue of the same extremity in 9 diabetic patients with chronic lower limb infections by use of in vivo microdialysis."( Determination of tissue penetration and pharmacokinetics of linezolid in patients with diabetic foot infections using in vivo microdialysis.
Kuti, JL; Nicolau, DP; Shepard, A; Wiskirchen, DE, 2011
)
0.82
" The results showed increased clearance of linezolid and a reduced serum concentration compared to population pharmacokinetic parameters, with trough levels below the 90% minimum inhibitory concentration."( Evaluation of the pharmacokinetics of linezolid in an obese Japanese patient.
Hiraki, Y; Kamimura, H; Karube, Y; Kobayashi, T; Matsumoto, K; Mizoguchi, A; Morita, K; Sadoh, S; Sakamoto, S; Tsuji, Y; Yukawa, E, 2012
)
0.91
"Our study shows that the continuous infusion of 1200 mg of linezolid daily in critically ill patients with VAP provides satisfactory pharmacokinetic results, with a linezolid alveolar diffusion of 100% and concentrations exceeding almost twice the susceptibility breakpoint for Staphylococcus aureus (4 mg/L) in both serum and ELF for 100% of the time."( Alveolar diffusion and pharmacokinetics of linezolid administered in continuous infusion to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Bouvet, L; Breilh, D; Caillault-Sergent, A; Djabarouti, S; Guillaume, C; Rimmelé, T; Saux, MC; Xuereb, F, 2012
)
0.88
"The methodology included the following steps: acquisition of microbiological and pharmacokinetic data, Monte Carlo simulation, estimation of the probability of target attainment (PTA), and calculation of the cumulative fraction of response (CFR)."( Pharmacokinetic-pharmacodynamic evaluation of daptomycin, tigecycline, and linezolid versus vancomycin for the treatment of MRSA infections in four western European countries.
Betriu, C; Canut, A; Gascón, AR; Isla, A, 2012
)
0.61
" These data highlight the importance of pharmacokinetic confirmation in each model."( Pharmacokinetics and pulmonary disposition of tedizolid and linezolid in a murine pneumonia model under variable conditions.
Crandon, JL; Keel, RA; Nicolau, DP, 2012
)
0.62
"A series of tetracyclic nitrofuran isoxazoline anti-tuberculosis agents was designed and synthesized to improve the pharmacokinetic properties of an initial lead compound, which had potent anti-tuberculosis activity but suffered from poor solubility, high protein binding and rapid metabolism."( Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
Bruhn, D; Gilliland, JC; Gruppo, V; Lee, RB; Lee, RE; Lenaerts, AJ; Maddox, M; Madhura, DB; McNeil, MR; Meibohm, B; Scherman, MS; Trivedi, A; Yang, L, 2012
)
0.38
" Pharmacokinetic analyses were conducted using compartmental and noncompartmental methods."( Pharmacokinetics of intravenous linezolid in moderately to morbidly obese adults.
Bhalodi, AA; Kuti, JL; Nicolau, DP; Papasavas, PK; Tishler, DS, 2013
)
0.67
"The objective was to evaluate the pharmacokinetic and pharmacodynamic properties of a single intravenous fixed dose compared with a weight-adjusted dose of linezolid."( Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Karageorgopoulos, DE; Liang, B; Wang, R, 2013
)
0.86
" A Monte Carlo simulation was used to evaluate the probability of pharmacodynamic target attainment (PTA)."( Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Karageorgopoulos, DE; Liang, B; Wang, R, 2013
)
0.66
"From the pharmacodynamic perspective (serum concentrations), vancomycin tolerance should include MBC/MIC ≥8 since strains exhibiting this ratio showed bacteriostatic profiles similar to those obtained with isolates with MBC/MIC ratios of 16 or 32."( Influence of the MBC/MIC ratio on the antibacterial activity of vancomycin versus linezolid against methicillin-resistant Staphylococcus aureus isolates in a pharmacodynamic model simulating serum and soft tissue interstitial fluid concentrations reported
Aguilar, L; Alou, L; Cafini, F; Gimenez, MJ; Gomez-Lus, ML; Gonzalez, N; Prieto, J; Sevillano, D, 2013
)
0.62
" The population pharmacokinetic (PPK) of linezolid was investigated in MRSA infected patients with renal dysfunction."( Population pharmacokinetic analysis of linezolid in low body weight patients with renal dysfunction.
Hiraki, Y; Kamimura, H; Karube, Y; Matsumoto, K; Mizoguchi, A; Morita, K; To, H; Tsuji, Y; Yukawa, E, 2013
)
0.93
" The validated method was applied to assay real plasma samples used for pharmacokinetic studies and therapeutic drug monitoring of the selected drugs."( Simultaneous quantification of linezolid, tinidazole, norfloxacin, moxifloxacin, levofloxacin, and gatifloxacin in human plasma for therapeutic drug monitoring and pharmacokinetic studies in human volunteers.
Helmy, SA, 2013
)
0.68
"This assay method was valid within a wide range of plasma concentrations and may be proposed as a suitable method for pharmacokinetic studies, therapeutic drug monitoring implementation, and routine clinical applications, especially for some populations of patients who receive a combination of these drugs."( Simultaneous quantification of linezolid, tinidazole, norfloxacin, moxifloxacin, levofloxacin, and gatifloxacin in human plasma for therapeutic drug monitoring and pharmacokinetic studies in human volunteers.
Helmy, SA, 2013
)
0.68
"A Monte Carlo simulation involving 10000 subjects was used to analyze the pharmacokinetic parameters and microbiological data of linezolid for an effectiveness evaluation at the corresponding AUC24/MIC values (area under the serum concentration-time curve over 24h/minimum inhibitory concentration)."( Developments in the pharmacokinetic/pharmacodynamic index of linezolid: a step toward dose optimization using Monte Carlo simulation in critically ill patients.
Chen, L; Dong, H; Dong, Y; Sun, J; Wang, T; Xie, J; Zhao, Y, 2014
)
0.85
" Multiple administrations of linezolid led to disappearance of significant differences in Cmax and AUC0-8 between plasma, inflamed, and non-inflamed tissue."( Target site pharmacokinetics of linezolid after single and multiple doses in diabetic patients with soft tissue infection.
Burian, A; Eslam, RB; Frenzel, D; Hammer, A; Kloft, C; Matzneller, P; Minichmayr, IK; Oesterreicher, Z; Sauermann, R; Vila, G; Zeitlinger, M, 2014
)
0.98
" The study aimed to describe the pharmacokinetic properties of linezolid administered intravenously at a dose of 10 mg/kg in severely burned rabbits in comparison to that in non-burns."( Comparison of the pharmacokinetics of linezolid in burn and non-burn rabbits.
Chu, WL; Feng, YQ; Gao, L; Li, X; Ma, JL; Wang, XQ; Zhang, QZ, 2015
)
0.93
"2 × Cmin + 134."( Analysis of thrombocytopenic effects and population pharmacokinetics of linezolid: a dosage strategy according to the trough concentration target and renal function in adult patients.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2014
)
0.63
"We performed a retrospective study of patients whose plasma C(min) and Cmax levels were measured during linezolid treatment."( Pharmacokinetic/pharmacodynamic evaluation of linezolid in hospitalized paediatric patients: a step toward dose optimization by means of therapeutic drug monitoring and Monte Carlo simulation.
Cojutti, P; Crichiutti, G; Isola, M; Maximova, N; Pea, F, 2015
)
0.89
"Linezolid pharmacokinetic profile in pediatric patients has not been fully characterized, and the dose needed to achieve a pharmacokinetic-pharmacodynamic (PK-PD) target has yet to be established because its efficacy is associated with the area under the plasma drug concentration-time curve (AUC24)/minimum inhibitory concentration (MIC) ratio."( Linezolid dosage in pediatric patients based on pharmacokinetics and pharmacodynamics.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2015
)
3.3
" To evaluate the potential of the novel oxazolidinone tedizolid to cause similar side effects, nonclinical and pharmacokinetic assessments were conducted."( Nonclinical and pharmacokinetic assessments to evaluate the potential of tedizolid and linezolid to affect mitochondrial function.
Das, D; Fiedler-Kelly, J; Flanagan, S; Hosako, H; McKee, EE; Passarell, J; Prokocimer, P; Radovsky, A; Tulkens, PM, 2015
)
0.64
" As a continuous, growth-control-normalised pharmacodynamic measure, the relative bacterial reduction (RBR) was introduced and derived."( Concentration-response studies and modelling of the pharmacodynamics of linezolid: Staphylococcus aureus versus Enterococcus faecium.
Derendorf, H; Kloft, C; Michael, J; Scheerans, C; Wicha, SG, 2015
)
0.65
"To systematically assess the impact of pharmacodynamic interactions when adding either linezolid or vancomycin to meropenem on the antibacterial activity against methicillin-susceptible Staphylococcus aureus (MSSA)."( Pharmacodynamic and response surface analysis of linezolid or vancomycin combined with meropenem against Staphylococcus aureus.
Kees, MG; Kloft, C; Kuss, J; Wicha, SG, 2015
)
0.89
" We newly elaborated a response surface analysis (RSA) to quantify the extent of the pharmacodynamic interactions."( Pharmacodynamic and response surface analysis of linezolid or vancomycin combined with meropenem against Staphylococcus aureus.
Kees, MG; Kloft, C; Kuss, J; Wicha, SG, 2015
)
0.67
"Standard doses of linezolid and meropenem will provide inhibitory concentrations and thus pharmacodynamic antagonism throughout the whole dosing interval for MSSA."( Pharmacodynamic and response surface analysis of linezolid or vancomycin combined with meropenem against Staphylococcus aureus.
Kees, MG; Kloft, C; Kuss, J; Wicha, SG, 2015
)
1.01
"The clinical development of FtsZ-targeting benzamide compounds like PC190723 has been limited by poor drug-like and pharmacokinetic properties."( TXA709, an FtsZ-Targeting Benzamide Prodrug with Improved Pharmacokinetics and Enhanced In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus.
Kaul, M; LaVoie, EJ; Lyu, YL; Mark, L; Parhi, AK; Pawlak, J; Pilch, DS; Saravolatz, LD; Saravolatz, S; Weinstein, MP; Zhang, Y, 2015
)
0.42
"To evaluate the pharmacokinetic and pharmacodynamic (PK/PD) results of three different infusion time regimens of single doses of 600 mg linezolid in healthy Han Chinese volunteers."( Pharmacokinetic/pharmacodynamic research on three different infusion time regimens of linezolid in healthy Chinese volunteers.
Bai, N; Cai, Y; Liang, B; Liu, X; Wang, J; Wang, R, 2015
)
0.84
" No significant difference was found in pharmacokinetic parameters among the three different infusion regimens."( Pharmacokinetic/pharmacodynamic research on three different infusion time regimens of linezolid in healthy Chinese volunteers.
Bai, N; Cai, Y; Liang, B; Liu, X; Wang, J; Wang, R, 2015
)
0.64
"Pharmacodynamic activity in antibiotic combinations of daptomycin, vancomycin, and linezolid was investigated in a 48-h in vitro pharmacodynamic model."( Observed Antagonistic Effect of Linezolid on Daptomycin or Vancomycin Activity against Biofilm-Forming Methicillin-Resistant Staphylococcus aureus in an In Vitro Pharmacodynamic Model.
LaPlante, KL; Luther, MK, 2015
)
0.93
" Population pharmacokinetic analysis was undertaken using Pmetrics."( Population pharmacokinetics of linezolid in critically ill patients on renal replacement therapy: comparison of equal doses in continuous venovenous haemofiltration and continuous venovenous haemodiafiltration.
Lefrant, JY; Lipman, J; Louart, B; Muller, L; Roberts, JA; Roger, C; Saissi, G; Wallis, SC, 2016
)
0.72
" Achievement of pharmacodynamic targets was poor for an MIC of 2 mg/L with the studied dose."( Population pharmacokinetics of linezolid in critically ill patients on renal replacement therapy: comparison of equal doses in continuous venovenous haemofiltration and continuous venovenous haemodiafiltration.
Lefrant, JY; Lipman, J; Louart, B; Muller, L; Roberts, JA; Roger, C; Saissi, G; Wallis, SC, 2016
)
0.72
"During CVVHF and CVVHDF, there is profound pharmacokinetic variability of linezolid."( Population pharmacokinetics of linezolid in critically ill patients on renal replacement therapy: comparison of equal doses in continuous venovenous haemofiltration and continuous venovenous haemodiafiltration.
Lefrant, JY; Lipman, J; Louart, B; Muller, L; Roberts, JA; Roger, C; Saissi, G; Wallis, SC, 2016
)
0.95
"Using appropriate oral pharmacokinetic data (single dose and steady state) for linezolid, both maximum plasma drug concentration (Cmax) versus area under the plasma concentration-time curve (AUC) and minimum plasma drug concentration (Cmin) versus AUC relationship was established by linear regression models."( Applicability of a Single Time Point Strategy for the Prediction of Area Under the Concentration Curve of Linezolid in Patients: Superiority of Ctrough- over Cmax-Derived Linear Regression Models.
Srinivas, NR; Syed, M, 2016
)
0.88
"The Cmax versus AUC and trough plasma concentration (Ctrough) versus AUC models displayed excellent correlation, with r values of >0."( Applicability of a Single Time Point Strategy for the Prediction of Area Under the Concentration Curve of Linezolid in Patients: Superiority of Ctrough- over Cmax-Derived Linear Regression Models.
Srinivas, NR; Syed, M, 2016
)
0.65
" Population pharmacokinetic analysis suggested that estimated tedizolid exposure measures in Latino patients vs non-Latino patients were similar."( Efficacy, safety, tolerability and population pharmacokinetics of tedizolid, a novel antibiotic, in Latino patients with acute bacterial skin and skin structure infections.
Cabré-Márquez, JF; Fang, E; Fiedler-Kelly, J; Flanagan, SD; Nannini, EC; Ortiz-Covarrubias, A; Passarell, J; Prokocimer, PG; Tanaka, T; Zhu, X,
)
0.13
" More population pharmacokinetic studies are necessary which will identify and quantify the influence of various factors on clearance and plasma concentrations of linezolid in critically ill patients."( Pharmacokinetics of linezolid in critically ill patients.
Dimitrijevic, A; Jankovic, SM; Kostic, M; Sazdanovic, P; Stefanovic, S, 2016
)
0.95
" The compounds were designed with the objective of improving pharmacokinetic properties."( Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
Abdelghany, TM; Bayoumi, SA; Disouky, AM; El-Morsy, A; Elshafeey, A; Mancy, AS; Mayhoub, AS; Mohammad, H; Seleem, MA; Seleem, MN, 2016
)
0.43
" Physiologically based pharmacokinetic (PBPK) modeling offers an enhanced ability to predict age-related changes in pharmacokinetics in the pediatric population."( Physiologically Based Pharmacokinetic Prediction of Linezolid and Emtricitabine in Neonates and Infants.
Burckart, GJ; Duan, P; Fisher, JW; Wang, J; Yoshida, K; Zhang, L, 2017
)
0.71
" Based on this study, linezolid and emtricitabine pediatric PBPK models incorporating the ontogeny in renal maturation describe the pharmacokinetic differences between adult and pediatric populations, even though the contribution of renal clearance to the total clearance of two drugs was very different (30 % for linezolid vs."( Physiologically Based Pharmacokinetic Prediction of Linezolid and Emtricitabine in Neonates and Infants.
Burckart, GJ; Duan, P; Fisher, JW; Wang, J; Yoshida, K; Zhang, L, 2017
)
1.02
" There are no studies describing the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" We investigated the pharmacodynamic mechanism (myelosuppression or enhanced platelet destruction) and the role of impaired renal function (RF) in the development of thrombocytopenia."( Population pharmacokinetics and pharmacodynamics of linezolid-induced thrombocytopenia in hospitalized patients.
Heo, YA; Higashi, Y; Holford, NHG; Kasai, H; Mizoguchi, A; Ogami, C; To, H; Tsuji, Y; Yamamoto, Y, 2017
)
0.71
" This combined pharmacokinetic, pharmacodynamic and turnover model identified that the most common mechanism of thrombocytopenia associated with linezolid is PDI."( Population pharmacokinetics and pharmacodynamics of linezolid-induced thrombocytopenia in hospitalized patients.
Heo, YA; Higashi, Y; Holford, NHG; Kasai, H; Mizoguchi, A; Ogami, C; To, H; Tsuji, Y; Yamamoto, Y, 2017
)
0.91
" Current strategies are not informed by clinical pharmacokinetic (PK)/pharmacodynamic (PD) data; we aimed to address this gap."( Linezolid pharmacokinetics in MDR-TB: a systematic review, meta-analysis and Monte Carlo simulation.
Alffenaar, JC; Bolhuis, M; Bonnett, L; Caws, M; Dartois, V; Davies, G; Hodel, EM; Johnson, JL; Millard, J; Pertinez, H; Sloan, DJ; Tiberi, S, 2018
)
1.92
"We investigated the pharmacokinetic (PK) and pharmacodynamic (PD) parameters of linezolid in patients who had suffered cerebral hemorrhage after lateral ventricular drainage."( Pharmacokinetics and pharmacodynamics of linezolid in plasma/cerebrospinal fluid in patients with cerebral hemorrhage after lateral ventricular drainage by Monte Carlo simulation.
Kong, L; Tang, Y; Wu, C; Wu, X; Zhang, X, 2018
)
0.97
" The aim of this study was to develop a population pharmacokinetic model for linezolid in children and optimize the dosing strategy in order to improve therapeutic efficacy."( Population Pharmacokinetics and Dosing Optimization of Linezolid in Pediatric Patients.
Li, SC; Wang, Y; Xu, H; Ye, Q; Zhang, L, 2019
)
0.99
" However, among children with MDR-TB, there are no linezolid pharmacokinetic data, and its adverse effects have not yet been prospectively described."( Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies.
Draper, HR; Garcia-Cremades, M; Garcia-Prats, AJ; Hesseling, AC; Savic, RM; Schaaf, HS; Wiesner, L; Winckler, J, 2019
)
1.02
"Children routinely treated for MDR-TB in 2 observational studies (2011-2015, 2016-2018) conducted at a single site in Cape Town, South Africa, underwent intensive pharmacokinetic sampling after either a single dose or multiple doses of linezolid (at steady state)."( Pharmacokinetics, optimal dosing, and safety of linezolid in children with multidrug-resistant tuberculosis: Combined data from two prospective observational studies.
Draper, HR; Garcia-Cremades, M; Garcia-Prats, AJ; Hesseling, AC; Savic, RM; Schaaf, HS; Wiesner, L; Winckler, J, 2019
)
0.95
"We previously investigated the pharmacokinetic and pharmacodynamic (PK/PD) parameters of routine linezolid infusions (1 h) in patients with external ventricular drains (EVD)."( Prolonged infusion of linezolid is associated with improved pharmacokinetic/pharmacodynamic (PK/PD) profiles in patients with external ventricular drains.
Kong, L; Wu, C; Wu, X; Zhao, W, 2021
)
1.15
"The objective of this study was to perform an external evaluation of published linezolid population pharmacokinetic and pharmacodynamic models, to evaluate the predictive performance using an independent data set."( External Evaluation of Population Pharmacokinetics and Pharmacodynamics in Linezolid-Induced Thrombocytopenia: The Transferability of Published Models to Different Hospitalized Patients.
Kawasuji, H; Nishi, Y; Ogami, C; To, H; Tsuji, Y; Yamamoto, Y, 2021
)
1.08
"We performed a systematic literature search in PubMed for all studies evaluating the population pharmacokinetic and pharmacodynamic parameters of linezolid in patients and selected the models to be used for the external validation."( External Evaluation of Population Pharmacokinetics and Pharmacodynamics in Linezolid-Induced Thrombocytopenia: The Transferability of Published Models to Different Hospitalized Patients.
Kawasuji, H; Nishi, Y; Ogami, C; To, H; Tsuji, Y; Yamamoto, Y, 2021
)
1.05
"Three articles (models A, B, and C) provided linezolid-induced platelet dynamic models using population pharmacokinetic and pharmacodynamic modeling approaches."( External Evaluation of Population Pharmacokinetics and Pharmacodynamics in Linezolid-Induced Thrombocytopenia: The Transferability of Published Models to Different Hospitalized Patients.
Kawasuji, H; Nishi, Y; Ogami, C; To, H; Tsuji, Y; Yamamoto, Y, 2021
)
1.11
"We confirmed the transferability of published population pharmacokinetic and pharmacodynamic models and showed that they were suitable for extrapolation to other hospitals and/or patients."( External Evaluation of Population Pharmacokinetics and Pharmacodynamics in Linezolid-Induced Thrombocytopenia: The Transferability of Published Models to Different Hospitalized Patients.
Kawasuji, H; Nishi, Y; Ogami, C; To, H; Tsuji, Y; Yamamoto, Y, 2021
)
0.85
" CF can modify both the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of antibiotics, therefore specific PK/PD endpoints should be determined in the context of CF."( Pharmacokinetic and Pharmacodynamic Optimization of Antibiotic Therapy in Cystic Fibrosis Patients: Current Evidences, Gaps in Knowledge and Future Directions.
Jullien, V; Launay, M; Magréault, S; Roy, C; Sermet-Gaudelus, I, 2021
)
0.62
"The aim of this study is to use a population pharmacokinetic (PK) approach to evaluate the optimal dosing strategy for linezolid (LNZ) in critically ill patients."( Pharmacokinetics of Linezolid Dose Adjustment for Creatinine Clearance in Critically Ill Patients: A Multicenter, Prospective, Open-Label, Observational Study.
Chen, C; Chen, S; Hou, Y; Lan, J; Li, Z; Luo, J; Qiu, B; Wang, X; Wang, Y; Wu, Z; Yao, F; Zheng, Z, 2021
)
1.15
" Data were obtained from pharmacokinetic substudies in a randomized controlled trial and an observational cohort study, both of which enrolled adults with drug-resistant pulmonary tuberculosis."( Linezolid Population Pharmacokinetics in South African Adults with Drug-Resistant Tuberculosis.
Abdelwahab, MT; Brust, JCM; Denti, P; Dheda, K; Gandhi, NR; Maartens, G; Meintjes, G; Sirgel, FA; Warren, RM; Wasserman, S; Wiesner, L, 2021
)
2.06
" This comprehensive review aimed to summarize population pharmacokinetic models of linezolid, by focusing on dosage optimization to maximize the probability of attaining a certain pharmacokinetic-pharmacodynamic parameter in special populations."( A Review of Population Pharmacokinetic Analyses of Linezolid.
Bandín-Vilar, E; Campos-Toimil, M; Castro-Balado, A; Fernández-Ferreiro, A; García-Quintanilla, L; González-Barcia, M; Mangas-Sanjuan, V; Mondelo-García, C; Zarra-Ferro, I, 2022
)
1.2
"Only a few reports are available on the population pharmacokinetic (PK) analysis of linezolid and its main metabolites."( Population pharmacokinetics of linezolid and its major metabolites PNU-142300 and PNU-142586 in adult patients.
Abe, J; Imoto, W; Kakeya, H; Kawaguchi, H; Kuwabara, G; Nakamura, Y; Sakurai, N; Shibata, W; Yamada, K; Yasui, H, 2022
)
1.23
" In this study, the blood LZD trough concentration was estimated based on population pharmacokinetic (PK) parameters derived from two previously published models in the Japanese population to determine the rate of achieving the target trough value when the risk of thrombocytopenia is low and to clarify its relationship with the onset of thrombocytopenia."( Pharmacokinetic and pharmacodynamic simulation for the quantitative risk assessment of linezolid-associated thrombocytopenia.
Ikawa, K; Ikebuchi, A; Ishihara, N; Morikawa, N; Naora, K; Nishimura, N; Onita, T; Tamaki, H; Yano, T, 2022
)
0.94
"Similar ratios of generic/originator (90% CI) Cmax were observed for Cefepime-MIP/Maxipime [93."( Comparison of pharmacokinetics and stability of generics of cefepime, linezolid and piperacillin/tazobactam with their respective originator drugs: an intravenous bioequivalence study in healthy volunteers.
Al Jalali, V; Ballarini, N; Bauer, M; Bergmann, F; Jorda, A; König, F; Lackner, E; Nussbaumer-Pröll, A; Oesterreicher, Z; Reiter, B; Stimpfl, T; Wölfl-Duchek, M; Wulkersdorfer, B; Zeitlinger, M, 2022
)
0.96
" A population pharmacokinetic model was constructed to identify covariates and test potential drug-drug interactions that may account for interpatient variability."( Linezolid Population Pharmacokinetics to Improve Dosing in Cardiosurgical Patients: Factoring a New Drug-Drug Interaction Pathway.
Cojutti, PG; Della Siega, P; Gerussi, V; Pai, MP; Pea, F; Tascini, C, 2023
)
2.35
" The objectives of this study were to establish a population pharmacokinetic model for linezolid in plasma and cerebrospinal fluid, as well as to optimize dosing strategies in this susceptible population."( Population Pharmacokinetics and Dosing Regimen Optimization of Linezolid in Cerebrospinal Fluid and Plasma of Post-operative Neurosurgical Patients.
Cao, P; Dong, H; Li, S; Meng, L; Wang, Y; Zhu, Y, 2023
)
1.37
"This was a prospective pharmacokinetic study in post-operative neurosurgical patients receiving intravenous linezolid."( Population Pharmacokinetics and Dosing Regimen Optimization of Linezolid in Cerebrospinal Fluid and Plasma of Post-operative Neurosurgical Patients.
Cao, P; Dong, H; Li, S; Meng, L; Wang, Y; Zhu, Y, 2023
)
1.36
" Studies involving adults receiving CRRT and treatment with linezolid were considered eligible if the CRRT setting and linezolid's pharmacokinetic parameters were clearly mentioned."( A Systematic Review of Linezolid Pharmacokinetics/Pharmacodynamics in Patients Undergoing Continuous Renal Replacement Therapy: Does One Size Fit All?
Chen, F; Ge, XH; Guo, HL; Ji, X; Liu, Y; Miao, HJ; Xu, J; Zhang, Y, 2023
)
1.46
"Several linezolid population pharmacokinetic (popPK) models have been established to facilitate optimal therapy; however, their extrapolated predictive performance to other clinical sites is unknown."( External evaluation of the predictive performance of published population pharmacokinetic models of linezolid in adult patients.
Chen, YT; Chen, Z; Jiao, Z; Li, XY; Lv, QZ; Qin, Y; Shen, Y; Ye, YR, 2023
)
1.56

Compound-Compound Interactions

Linezolid in combination with ertapenem showed in vitro synergy against methicillin-resistant Staphylococcus aureus strains. When combined with 8 mg/L rifampicin, MBECs for ciprofloxacin and linezolid dropped to 16-32mg/L.

ExcerptReferenceRelevance
"The in vitro activity of the oxazolidinone linezolid was studied alone and in combination with three antibiotics acting on different cellular targets."( In vitro activity of linezolid alone and in combination with gentamicin, vancomycin or rifampicin against methicillin-resistant Staphylococcus aureus by time-kill curve methods.
Bugnon, D; Caillon, J; Donnio, PY; Jacqueline, C; Le Mabecque, V; Miegeville, AF; Potel, G, 2003
)
0.9
"The activities of linezolid, an oxazolidinone antibacterial agent active against gram-positive organisms, alone and in combination with 35 antimicrobial agents were tested in vitro against methicillin-sensitive (n = 1 to 2 strains) and methicillin-resistant (n = 8 to 10) Staphylococcus aureus strains; vancomycin-sensitive (n = 6) and vancomycin-resistant (n = 6 to 8) Enterococcus faecalis strains; vancomycin-sensitive (n = 5) and vancomycin-resistant (n = 6) Enterococcus faecium strains; penicillin-sensitive (n = 2 to 5), penicillin-intermediate (n = 5 to 6), and penicillin-resistant (n = 5 to 6) Streptococcus pneumoniae strains; Escherichia coli (n = 6); and Klebsiella pneumoniae (n = 6)."( In vitro activities of linezolid combined with other antimicrobial agents against Staphylococci, Enterococci, Pneumococci, and selected gram-negative organisms.
Sweeney, MT; Zurenko, GE, 2003
)
0.96
"A rat model was used to investigate the efficacy of linezolid, alone or in combination with levofloxacin and vancomycin, in the prevention of vascular prosthetic graft infection resulting from methicillin-resistant Staphylococcus epidermidis with intermediate resistance to glycopeptides."( Prophylactic efficacy of linezolid alone or combined with levofloxacin and vancomycin in a rat subcutaneous pouch model of graft infection caused by Staphylococcus epidermidis with intermediate resistance to glycopeptides.
Cirioni, O; D'Amato, G; Del Prete, MS; Ghiselli, R; Giacometti, A; Mocchegiani, F; Orlando, F; Saba, V; Scalise, G; Silvestri, C, 2003
)
0.87
" The purpose of this study was to evaluate the in vivo activity of linezolid combined with gentamicin using a methicillin-resistant Staphylococcus aureus (MRSA) endocarditis experimental model."( In vivo efficacy of linezolid in combination with gentamicin for the treatment of experimental endocarditis due to methicillin-resistant Staphylococcus aureus.
Asseray, N; Batard, E; Bugnon, D; Caillon, J; Dube, L; Jacqueline, C; Kergueris, MF; Le Mabecque, V; Potel, G, 2004
)
0.88
"Indifference or moderate antagonism of linezolid combined with other antibiotics in vitro and in vivo have mainly been reported in the literature."( In vitro and in vivo synergistic activities of linezolid combined with subinhibitory concentrations of imipenem against methicillin-resistant Staphylococcus aureus.
Batard, E; Bugnon, D; Caillon, J; Jacqueline, C; Kergueris, MF; Le Mabecque, V; Miegeville, AF; Navas, D; Potel, G, 2005
)
0.85
" Linezolid is a weak monoamine oxidase inhibitor and has been reported to interact with selective serotonin reuptake inhibitors (SSRIs)."( Drug interactions between linezolid and selective serotonin reuptake inhibitors: case report involving sertraline and review of the literature.
Andrus, MR; Byrd, DC; Clark, DB, 2006
)
1.54
"Linezolid in combination with ertapenem showed in vitro synergy against methicillin-resistant Staphylococcus aureus strains."( In vitro and in vivo assessment of linezolid combined with ertapenem: a highly synergistic combination against methicillin-resistant Staphylococcus aureus.
Batard, E; Bugnon, D; Caillon, J; Grossi, O; Jacqueline, C; Le Mabecque, V; Miegeville, AF; Potel, G, 2006
)
2.05
" To explore strategies to overcome resistance development, we studied the effects of rifalazil in combination with several different antibiotics in an in vitro time-kill model, against both log phase and stationary phase Staphylococcus aureus cells."( Enhanced activity of rifalazil in combination with levofloxacin, linezolid, or mupirocin against Staphylococcus aureus in vitro.
Murphy, CK; Osburne, MS; Rothstein, DM, 2006
)
0.57
" A positive interaction was shown when the lipopeptides were combined with beta-lactams and vancomycin."( In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
Cirioni, O; Della Vittoria, A; Giacometti, A; Kamysz, W; Licci, A; Okroj, M; Scalise, G; Silvestri, C, 2007
)
0.34
"The objective of this paper was to investigate the in vitro effects of linezolid combined with five antistaphylococcal antibiotics--doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin--upon methicillin-susceptible Staphylococcus aureus (MSSA)."( In vitro activity of linezolid in combination with doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin against methicillin-susceptible Staphylococcus aureus.
Cantón, E; Colombo Gainza, E; Gil Brusola, A; Gobernado, M; Ortiz Estévez, R; Sahuquillo Arce, JM, 2006
)
0.89
"2 was combined with clarithromycin and minocycline."( In vitro activity of aurein 1.2 alone and in combination with antibiotics against gram-positive nosocomial cocci.
Cirioni, O; Della Vittoria, A; Giacometti, A; Kamysz, W; Nadolski, P; Riva, A; Scalise, G; Silvestri, C; Łukasiak, J, 2007
)
0.34
" The objective of this study was also to determine the effects of the interaction of linezolid when it was combined with rifampicin and test this effect against strains of methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis."( Linezolid alone and in combination with rifampicin prevents experimental vascular graft infection due to methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis.
Baltalarli, A; Duver, H; Goksin, I; Kaan Inan, B; Kaleli, I; Onem, G; Ozcan, V; Sacar, M; Sacar, S; Turgut, H, 2007
)
2.01
" This study describes the synergistic activity of oritavancin in combination with gentamicin, linezolid, moxifloxacin, or rifampin in time-kill studies against methicillin-susceptible, vancomycin-intermediate, and vancomycin-resistant Staphylococcus aureus."( Assessment by time-kill methodology of the synergistic effects of oritavancin in combination with other antimicrobial agents against Staphylococcus aureus.
Arhin, FF; Belley, A; McKay, GA; Moeck, G; Neesham-Grenon, E; Parr, TR, 2008
)
0.57
"The knowledge about efficacy of linezolid alone or in combination with rifampin in device infections is limited."( Efficacy of linezolid alone and in combination with rifampin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Domenech, A; Euba, G; Gudiol, F; Murillo, O; Tubau, F; Verdaguer, R, 2008
)
1.01
"Linezolid alone showed moderate efficacy, whereas its combination with rifampin prevented the emergence of rifampin resistance."( Efficacy of linezolid alone and in combination with rifampin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Domenech, A; Euba, G; Gudiol, F; Murillo, O; Tubau, F; Verdaguer, R, 2008
)
2.17
"We investigated the activity of linezolid, alone and in combination with rifampin (rifampicin), against a methicillin-resistant Staphylococcus aureus (MRSA) strain in vitro and in a guinea pig model of foreign-body infection."( Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
Baldoni, D; Haschke, M; Rajacic, Z; Trampuz, A; Zimmerli, W, 2009
)
2.08
" In vitro, fosfomycin showed a synergistic effect when combined with the other antimicrobials tested."( Efficacy of fosfomycin and its combination with linezolid, vancomycin and imipenem in an experimental peritonitis model caused by a Staphylococcus aureus strain with reduced susceptibility to vancomycin.
Ariza, J; Cabellos, C; Domínguez, MA; Fernández, R; Gudiol, F; Pachón-Ibáñez, ME; Ribes, S; Tubau, F, 2011
)
0.62
" The aim of this study was to evaluate the efficacies of daptomycin at usual and high doses (equivalent to 6 and 10 mg/kg of body weight/day, respectively, in humans) and in combination with rifampin and to compare the activities to those of conventional anti-MRSA therapies."( Efficacy of usual and high doses of daptomycin in combination with rifampin versus alternative therapies in experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
Ariza, J; Cabellos, C; Cabo, J; Euba, G; Garrigós, C; Murillo, O; Tubau, F; Verdaguer, R, 2010
)
0.36
" Treatment with linezolid combined with TMP-SMZ resulted in a clear clinical improvement and bacterial clearance."( Linezolid combined with trimethoprim-sulfamethoxazole therapy for the treatment of disseminated nocardiosis.
Li, H; Shen, Q; Zhou, H; Zhou, J, 2011
)
2.16
" When combined with 8 mg/L rifampicin, MBECs for ciprofloxacin and linezolid dropped to 16-32 mg/L for the four isolates tested."( Effectiveness of ciprofloxacin or linezolid in combination with rifampicin against Enterococcus faecalis in biofilms.
Holmberg, A; Mörgelin, M; Rasmussen, M, 2012
)
0.89
"Serotonin syndrome can be a rare but life-threatening condition that is commonly the result of a drug-drug interaction causing excessive serotonin activity."( Probable drug-drug interaction leading to serotonin syndrome in a patient treated with concomitant buspirone and linezolid in the setting of therapeutic hypothermia.
Morrison, EK; Rowe, AS, 2012
)
0.59
" We carried out this study to determine the mutant prevention concentration (MPC) of linezolid when combined with minocycline against VRE strains, to determine the mechanism of drug resistance in vitro, and to provide a theoretical basis for the rational use of drugs against VRE."( Antimicrobial activity of linezolid combined with minocycline against vancomycin-resistant Enterococci.
Jiang, TT; Li, L; Su, JR; Wu, J, 2013
)
0.91
" decreased dramatically when combined with minocycline, and vice versa."( Antimicrobial activity of linezolid combined with minocycline against vancomycin-resistant Enterococci.
Jiang, TT; Li, L; Su, JR; Wu, J, 2013
)
0.69
" coli and MRSA when ranalexin was used in combination with antibiotics, even at concentrations of 1/4 MIC or 1/2 MIC of ranalexin, respectively."( Secretory ranalexin produced in recombinant Pichia pastoris exhibits additive or synergistic bactericidal activity when used in combination with polymyxin B or linezolid against multi-drug resistant bacteria.
Aleinein, RA; Schäfer, H; Wink, M, 2014
)
0.6
"The objective of this paper was to investigate the in vitro effects of fosfomycin combined with linezolid against methicillin-resistant Staphylococcus aureus (MRSA)."( In vitro activity of fosfomycin in combination with linezolid against clinical isolates of methicillin-resistant Staphylococcus aureus.
De-feng, L; Dong, W; Falagas, ME; Karageorgopoulos, DE; Rui, W; Xu-hong, Y, 2014
)
0.87
"Warfarin is known to interact with many drugs; however, there are currently no descriptions of an interaction with linezolid in the literature."( Potential drug interaction between warfarin and linezolid.
Arima, C; Hidaka, H; Kakuma, T; Masunaga, K; Miura, M; Naito, T; Qin, L; Sakai, Y; Watanabe, H, 2015
)
0.88
"Oxazolidinone pharmacology including structure-activity relationships, mode of action, pharmacokinetics, drug-drug interactions, and adverse drug reactions is reviewed."( Drug-drug interactions and safety of linezolid, tedizolid, and other oxazolidinones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.69
" The aim of the study was to investigate the in vitro activity of linezolid alone and in combination with imipenem, vancomycin or rifampicin to determine the most active therapy against MRSA strains."( EFFECT OF LINEZOLID ALONE AND IN COMBINATION WITH OTHER ANTIBIOTICS, ON METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS.
Azmy, M; Badawy, M; El Said, M; Gohar, H; Madany, N; Mansy, S; Yehia, H, 2016
)
1.07
" PK drug-drug interactions might partly be responsible and should be further investigated; protein binding appears to be stable and irrelevant."( Variable Linezolid Exposure in Intensive Care Unit Patients-Possible Role of Drug-Drug Interactions.
Dorn, C; Kees, F; Kees, MG; Kratzer, A; Liebchen, U; Salzberger, B; Schleibinger, M; Steinbach, CL; Töpper, C; Wicha, SG, 2016
)
0.85
" aureus activity of P128 alone and in combination with standard-of-care antibiotics on planktonic and biofilm-embedded cells."( Antibiofilm Activity and Synergistic Inhibition of Staphylococcus aureus Biofilms by Bactericidal Protein P128 in Combination with Antibiotics.
Desai, S; Nair, S; Poonacha, N; Sharma, U; Vipra, A, 2016
)
0.43
" In addition, the activity of the moxifloxacin + linezolid backbone in combination with one of the potentiator drugs was assessed."( Activity of moxifloxacin and linezolid against Mycobacterium tuberculosis in combination with potentiator drugs verapamil, timcodar, colistin and SQ109.
Aarnoutse, RE; de Knegt, GJ; de Steenwinkel, JE; de Vogel, CP; van der Meijden, A, 2017
)
1
"The in vitro activity of LZD in combination with five different antibiotics was evaluated using a microdilution checkerboard method and time-kill study against 12 clinical enterococcus isolates."( In vitro activity of linezolid alone and combined with other antibiotics against clinical enterococcal isolates.
Ahmadrajabi, R; Beitdaghar, M; Karmostaji, A; Saffari, F, 2019
)
0.83
" In the time-kill analysis, TRQ at 1/2 × MIC in combination with vancomycin at 1/2 × MIC, as well as TRQ at 1/8 × MIC in combination with linezolid at 1/2 × MIC decreased the viable colonies by ≥2log10 CFU/ml, resulting in a potent synergistic effect against planktonic MRSA."( In vitro antibacterial effects of Tanreqing injection combined with vancomycin or linezolid against methicillin-resistant Staphylococcus aureus.
Blažeković, B; Li, C; Liu, J; Ma, S; Ren, C; Sun, Y; Tian, G; Vladimir-Knežević, S; Wang, Y; Xing, Y; Yang, W, 2018
)
0.91
" Pharmacokinetic profiles in plasma and epithelial lining fluid (ELF) as well as the therapeutic efficacy of linezolid alone and in combination with rifampicin were investigated in a murine pneumonia model."( Increased activity of linezolid in combination with rifampicin in a murine pneumonia model due to MRSA.
Bu, MX; Li, L; Liao, XP; Liu, YH; Sun, J; Tao, MT; Xiong, YQ; Zhou, YF, 2018
)
1.01
"Rifampin (RIF) plus clarithromycin (CLR) for 8 weeks is now the standard of care for Buruli ulcer (BU) treatment, but CLR may not be an ideal companion for rifamycins due to bidirectional drug-drug interactions."( Oxazolidinones Can Replace Clarithromycin in Combination with Rifampin in a Mouse Model of Buruli Ulcer.
Almeida, DV; Converse, PJ; Grosset, JH; Lee, J; Li, SY; Nuermberger, EL; Omansen, TF, 2019
)
0.51
"We explored the potential synergistic effect of bedaquiline (BDQ) combined with moxifloxacin (MFX), gatifloxacin (GAT), clofazimine (CLO), and linezolid (LZD) for treatment of extensively drug-resistant tuberculosis (XDR-TB)."( No in vitro synergistic effect of bedaquiline combined with fluoroquinolones, linezolid, and clofazimine against extensively drug-resistant tuberculosis.
Chu, N; Dai, G; Dong, L; Huang, H; Huo, F; Jing, W; Li, Y; Lu, J; Pang, Y; Zong, Z, 2019
)
0.94
"Our in vitro data demonstrate no observed synergistic effects against XDR-TB for drug combinations that included BDQ in combination with MFX, GAT, LZD, or CLO."( No in vitro synergistic effect of bedaquiline combined with fluoroquinolones, linezolid, and clofazimine against extensively drug-resistant tuberculosis.
Chu, N; Dai, G; Dong, L; Huang, H; Huo, F; Jing, W; Li, Y; Lu, J; Pang, Y; Zong, Z, 2019
)
0.74
"This study aimed to explore daptomycin combined with fosfomycin or rifampin against the planktonic and adherent linezolid-resistant isolates of Enterococcus faecalis."( In vitro activities of daptomycin combined with fosfomycin or rifampin on planktonic and adherent linezolid-resistant isolates of Enterococcus faecalis.
Chen, Z; Deng, QW; Jiang, SB; Lin, ZW; Qi, GB; Qu, D; Sun, X; Tu, HP; Wu, Y; Yu, ZJ; Zheng, JX, 2019
)
0.94
"Despite its frequent use in clinical practice, fentanyl's pro-serotonergic effects are underrecognized, especially in combination with linezolid."( Linezolid and fentanyl: An underrecognized drug-to-drug interaction.
Abu Saleh, O; Barth, D; Corsini Campioli, C; Esquer Garrigos, Z; Sia, IG; Sohail, RM, 2020
)
2.2
" The results of our Greco universal response surface analysis showed that CFZ was at least additive with a clear trend towards synergy when combined with PMD, BDQ and LZD against Mtb in all explored metabolic states under in vitro checkerboard assay conditions."( Evaluating the effect of clofazimine against Mycobacterium tuberculosis given alone or in combination with pretomanid, bedaquiline or linezolid.
Almoslem, M; Drusano, GL; Duncanson, B; Kim, S; Louie, A; Myrick, J; Neely, M; Nole, J; Peloquin, CA; Scanga, CA; Schmidt, S; Yamada, W, 2022
)
0.92
" A population pharmacokinetic model was constructed to identify covariates and test potential drug-drug interactions that may account for interpatient variability."( Linezolid Population Pharmacokinetics to Improve Dosing in Cardiosurgical Patients: Factoring a New Drug-Drug Interaction Pathway.
Cojutti, PG; Della Siega, P; Gerussi, V; Pai, MP; Pea, F; Tascini, C, 2023
)
2.35
" Delpazolid is administered in combination with bedaquiline, delamanid and moxifloxacin."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91
"Linezolid is commonly used in intensive care units (ICU) but has the potential to interact with other drugs."( Prevalence of potential drug-drug interactions among intensive care unit patients receiving linezolid: a cross-sectional study.
Jiang, HY; Wang, X; Yu, LY; Yu, ZW; Zhao, YH, 2023
)
2.57
"Data of ICU patients receiving linezolid were extracted and included in the Hospital Prescription Analysis Program of China, and the risk of potential drug-drug interactions between concomitant drugs and linezolid was evaluated using the Lexicomp database."( Prevalence of potential drug-drug interactions among intensive care unit patients receiving linezolid: a cross-sectional study.
Jiang, HY; Wang, X; Yu, LY; Yu, ZW; Zhao, YH, 2023
)
1.42
"9% of patients had potential drug-drug interactions."( Prevalence of potential drug-drug interactions among intensive care unit patients receiving linezolid: a cross-sectional study.
Jiang, HY; Wang, X; Yu, LY; Yu, ZW; Zhao, YH, 2023
)
1.13
"ICU patients receiving linezolid have a high prevalence of potential drug-drug interactions, and efforts should be made to better recognize and manage this risk."( Prevalence of potential drug-drug interactions among intensive care unit patients receiving linezolid: a cross-sectional study.
Jiang, HY; Wang, X; Yu, LY; Yu, ZW; Zhao, YH, 2023
)
1.44

Bioavailability

Linezolid, an oxazolidinone antibiotic, has 100% oral bioavailability. The bioavailability of linezolid is not impaired by RYGBS. Linezolid offers a valuable alternative to more traditional therapies, such as glycopeptides.

ExcerptReferenceRelevance
"The Upjohn oxazolidinones, U-100592 and U-100766, are orally bioavailable synthetic antimicrobial agents with spectra of activity against antibiotic-susceptible and -resistant gram-positive pathogens."( In vivo activities of U-100592 and U-100766, novel oxazolidinone antimicrobial agents, against experimental bacterial infections.
Barbachyn, MR; Brickner, SJ; Ford, CW; Hamel, JC; Hutchinson, DK; Moerman, JK; Stapert, D; Wilson, DM; Yancey, RJ, 1996
)
0.29
" Linezolid, the oxazolidinone which has been selected for clinical development, has near complete oral bioavailability plus favourable pharmacokinetic and toxicity profiles."( Oxazolidinones: a review.
Diekema, DI; Jones, RN, 2000
)
1.22
" It has good pharmacokinetics, with equal bioavailability by both oral and intravenous routes and no need for dose adjustment in patients with renal impairment."( Linezolid.
French, G,
)
1.57
" Linezolid has almost 100% bioavailability and the area under the plasma concentration curve is identical after oral and iv."( Linezolid--a review of the first oxazolidinone.
Norrby, R, 2001
)
2.66
" Linezolid may be administered either intravenously or orally with oral bioavailability of approximately 100% and limited adverse effects."( The oxazolidinones as a new family of antimicrobial agent.
Marchese, A; Schito, GC, 2001
)
1.22
" The objectives of this study were twofold: (1) to compare the absorption of linezolid tablets given immediately following a high-fat meal with the absorption of tablets administered while fasting, and (2) to assess the bioavailability of a 375-mg oral dose given while fasting relative to a 375-mg dose of linezolid sterile solution given intravenously."( Linezolid absolute bioavailability and the effect of food on oral bioavailability.
Hopkins, NK; Jungbluth, GL; Sisson, TA; Stalker, DJ; Welshman, IR, 2001
)
1.98
" Linezolid is a parenteral agent that also possesses near-complete oral bioavailability plus favourable pharmacokinetic and toxic effect profiles."( Oxazolidinone antibiotics.
Diekema, DJ; Jones, RN, 2001
)
1.22
" It is well absorbed with high bioavailability that allows conversion to oral therapy as soon as the patient is clinically stable."( Linezolid: its role in the treatment of gram-positive, drug-resistant bacterial infections.
Ament, PW; Horne, JP; Jamshed, N, 2002
)
1.76
" bioavailability of > 95% in rat and dog, and > 70% in mouse."( Pharmacokinetics, toxicokinetics, distribution, metabolism and excretion of linezolid in mouse, rat and dog.
Adams, LA; Bush, EC; Chiba, K; Daley-Yates, PT; Feenstra, KL; Koike, S; Ozawa, N; Peng, GW; Sams, JP; Schuette, MR; Slatter, JG; Yamazaki, S, 2002
)
0.54
" LZD is rapidly absorbed following oral administration and bioavailability when compared with intravenous administration is almost 100%."( [Antimicrobial and clinical effect of linezolid (ZYVOX), new class of synthetic antibacterial drug].
Hashimoto, M; Irinoda, K; Nomura, S, 2002
)
0.59
" Oral bioavailability in humans was determined to be 100% and twice daily dosing in humans resulted in blood levels which even at trough values were in excess of the MIC90 for significant Gram-positive pathogens."( The discovery of linezolid, the first oxazolidinone antibacterial agent.
Barbachyn, MR; Ford, CW; Zurenko, GE, 2001
)
0.65
" Virtually complete oral bioavailability allows for 1:1 conversion between the intravenous and oral dosage forms."( Linezolid: an oxazolidinone antimicrobial agent.
Paladino, JA, 2002
)
1.76
" The almost-complete bioavailability of linezolid permits oral administration."( Quinupristin-dalfopristin and linezolid: evidence and opinion.
Eliopoulos, GM, 2003
)
0.88
"Linezolid, an oxazolidinone antibiotic, has 100% oral bioavailability and favorable activities against gram-positive pathogens including multidrug-resistant staphylococci, enterococci, and pneumococci."( Worldwide assessment of linezolid's clinical safety and tolerability: comparator-controlled phase III studies.
Cammarata, S; Hafkin, B; Isturiz, R; Le, V; Oliphant, TH; Remington, J; Rubinstein, E; Smith, LG; Standiford, HC, 2003
)
2.07
" Linezolid has complete bioavailability in parenteral and oral administration, is well tolerated and shows little toxicity, thus favoring a shortened hospital stay, improving the patient's quality of life and reducing social costs."( Treatment of gram-positive surgical sepsis: role of the oxazolidinones.
Carnuccio, P; Colizza, S; Cucchiara, G; Rodio, F; Rossi, S, 2003
)
1.23
" Oral linezolid has excellent bioavailability and activity against MRSA and MR-CoNS and offers the potential for outpatient treatment of MRSA and MR-CoNS infections."( Early switch and early discharge opportunities in intravenous vancomycin treatment of suspected methicillin-resistant staphylococcal species infections.
Goetz, MB; Parodi, S; Rhew, DC,
)
0.61
" Linezolid possesses a high activity against all multiresistant gram-positive cocci, favourable pharmacokinetics, a good safety profile, a complete bioavailability after and administration permitting switch therapy, a low capacity of inducing resistance, and both clinical and microbiologic efficacy as demonstrated by a number of clinical trials conducted on thousands of patients."( [The role of linezolid in the therapy of infections caused by multiresistant gram-positive cocci].
Corti, G; Paradisi, F, 2004
)
1.6
" The compound's excellent oral bioavailability and reasonable safety profile, along with the increasing incidence of resistant infections, means that linezolid offers a valuable alternative to more traditional therapies such as vancomycin."( The safety and efficacy of linezolid in orthopaedic practice for the treatment of infection due to antibiotic-resistant organisms.
Giannoudis, PV; Harwood, PJ, 2004
)
0.82
" The excellent bioavailability after oral administration (almost 100%) makes it suitable for outpatient treatment and treatment by general practitioners."( [Linezolid, an agent from a new class of antibiotics].
Bernards, AT; Kuijper, EJ; Schippers, EF, 2004
)
1.23
"Linezolid is an oxazolidinone antimicrobial with excellent oral bioavailability and tissue penetration and is active against multidrug-resistant skin/soft tissue pathogens."( Pharmacokinetics and pharmacodynamics of linezolid in obese patients with cellulitis.
Citron, DM; Goldstein, EJ; Havlichek, DH; Kak, V; Peloquin, CA; Schooley, SL; Stein, GE; Tyrrell, KL, 2005
)
2.04
" With an excellent oral bioavailability and acceptable safety profile, linezolid offers a valuable alternative to more traditional therapies, such as glycopeptides."( Role of linezolid in the treatment of orthopedic infections.
Bassetti, D; Bassetti, M; Beltrame, A; Di Biagio, A; Righi, E; Rosso, R, 2005
)
1
" Therefore, the bioavailability of linezolid administered enterally in the presence of enteral feedings in hospitalized patients was examined."( Absolute bioavailability and pharmacokinetics of linezolid in hospitalized patients given enteral feedings.
Beringer, P; Gill, M; Gurevitch, M; Hoem, N; Louie, S; Nguyen, M; Wong-Beringer, A, 2005
)
0.86
" Linezolid is a pararental drug that also possesses near-complete oral bioavailability and a favourable pharmacokinetic profile."( Oxazolidinones--a new class of broad-spectrum chemotherapeutics.
Pasternak, K; Sztanke, K; Sztanke, M, 2004
)
1.23
" The oral bioavailability of linezolid is approximately 100%, thus allowing sequential intravenous-to-oral administration without changing the drug or dosage regimen."( Linezolid: a pharmacoeconomic review of its use in serious Gram-positive infections.
Figgitt, DP; Plosker, GL, 2005
)
2.06
"The aim of this study was to determine the bioavailability of a novel oxazolidinone, DRF-6196, in mice and rats following intravenous (i."( Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid.
Bhamidipati, R; Das, J; Dravid, PV; Mullangi, R; Narasimhulu, PC; Srinivas, NR; Tvrs, S; Venkatesh, P,
)
0.34
" With its oral bioavailability profiles, it obviously holds great promise."( In vitro activity of linezolid and other antibiotics against Gram-positive bacteria from the major teaching hospitals in Kuwait.
Al Sweih, N; Jamal, W; Mokaddas, E; Phillips, OA; Rotimi, VO, 2005
)
0.65
" Prosthesis retention, in conjunction with debridement and prolonged (for at least 3 months) oral antibiotic therapy, can be an alternative for early postoperative or late acute haematogenous infections, when the duration of symptoms is less than 1 month, the implant is stable, and the pathogen is relatively avirulent and sensitive to an orally well absorbed antibiotic."( Management of infections of osteoarticular prosthesis.
Barberán, J, 2006
)
0.33
" Linezolid is a new antibiotic with high bioavailability and an outstanding safety profile, synergistic with imipenem, which may deserve a place in the armamentarium for severe pneumonia in children."( Effectiveness of linezolid and imipenem association in the treatment of severe community-acquired pneumonia in children: two case reports.
Caillon, J; Christophe Roze, J; Denizot, S; Godon, N; Gras-Le Guen, C; Podevin, G; Potel, G, 2006
)
1.58
" Linezolid is the first of a new class of antimicrobial agents known as the oxazolidinones with activity against gram-positive bacteria similar to that of vancomycin and yet its oral bioavailability allows for enteral administration."( Preliminary experience with the use of oral linezolid in infants for the completion of antibiotic therapy in the outpatient setting after admission to the pediatric intensive care unit.
Sullivan, J; Tobias, JD,
)
1.3
" Linezolid is well absorbed in the intestinal system."( [Linezolid in the treatment of antibiotic-resistant gram-positive infections of the musculoskeletal system].
Jahoda, D; Landor, I; Nyc, O; Pokorný, D; Sosna, A, 2006
)
2.15
" Pharmacocinetics studies have shown that linezolid has an excellent bioavailability allowing a fast relay per os."( [Linezolid: antibacterial activity, clinical efficacy and resistance].
Bourgeois-Nicolaos, N; Butel, MJ; Doucet-Populaire, F; Piriou, O,
)
1.31
" It is well absorbed with high bioavailability after oral administration and generally well tolerated."( [Linezolid--novel antibiotic for the treatment of gram-positive bacterial infections].
Jankowski, A; Stefanik, W, 2006
)
1.24
"Linezolid is an attractive alternative for orthopedic infections because of oral bioavailability and activity against methicillin-resistant staphylococci and vancomycin-resistant enterococci."( Efficacy and safety of linezolid for Gram-positive orthopedic infections: a prospective case series.
Hamilton, CW; Rao, N, 2007
)
2.09
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" Furthermore, in vivo efficacies and pharmacokinetic properties of the selected compounds were also disclosed herein; the selected compounds showed reasonable bioavailability as well as in vivo efficacy comparable to that of linezolid."( Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
Chen, Y; Fan, H; Ji, R; Jiang, Z; Yang, Y; Zhang, S; Zhong, D, 2008
)
0.53
"The excellent oral bioavailability and the Gram-positive antimicrobial spectrum make linezolid an attractive antibiotic for treatment of osteoarticular infections."( Experience with linezolid therapy in children with osteoarticular infections.
Chen, CJ; Chiu, CH; Huang, YC; Lee, ZL; Lin, TY; Yang, WE, 2007
)
0.91
" It has an excellent bioavailability both intravenously and orally and a very good safety profile both in adults and in children."( Linezolid in children: recent patents and advances.
Velissariou, IM, 2007
)
1.78
"We have developed a first generation of hybrid sparsomycin-linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant gram-positive bacteria as well as the fastidious gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis."( Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
Bhattacharjee, A; Chen, S; Chen, Y; Duffy, E; Farmer, J; Goldberg, J; Hanselmann, R; Ippolito, JA; Johnson, G; Lou, R; Orbin, A; Oyelere, A; Salvino, J; Springer, D; Tran, J; Wang, D; Wu, Y; Zhou, J, 2008
)
0.59
" The availability of intravenous and oral formulations, with near 100% bioavailability of the latter, is hoped to facilitate the management of multiply drug-resistant Gram-positive infections."( Linezolid: a review of safety and tolerability.
Rubinstein, E; Vinh, DC, 2009
)
1.8
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" PNU-100480 doses to 1000 mg were well absorbed and showed approximately proportional increases in exposures of parent and metabolites."( Pharmacokinetics and whole-blood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers.
Campbell, S; Dimitrova, D; Friedland, G; Jakubiec, WM; Kumar, V; Ladutko, L; Li, X; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, AM; Wallis, RS, 2010
)
0.36
" Moreover, the availability of intravenous and oral formulation with an excellent bioavailability of the latter, is hoped to facilitate the management of these infections."( [Linezolide in paediatrics].
Ménager, C; Moulin, F, 2010
)
1.27
" It is unique amongst antibiotics active against most multiply-resistant Gram-positive bacteria in that there is an oral preparation with 100% bioavailability and an extensive volume of distribution."( Linezolid pharmacokinetics and pharmacodynamics in clinical treatment.
Dryden, MS, 2011
)
1.81
"Fusidic acid (CEM-102), an orally bioavailable fusidane antibiotic with a unique mode of action, is under development for treatment of acute gram-positive bacterial skin and skin structure infections, including those caused by methicillin-susceptible and methicillin-resistant Staphylococcus aureus and streptococci."( A randomized, double-blind phase 2 study comparing the efficacy and safety of an oral fusidic acid loading-dose regimen to oral linezolid for the treatment of acute bacterial skin and skin structure infections.
Clark, K; Corey, GR; Craft, JC; Das, A; Degenhardt, TP; Fernandes, P; Moriarty, SR; Scott, D; Still, JG, 2011
)
0.57
" This compound also showed excellent pharmacokinetic profiles, with a half-life of more than 5 h as well as an oral bioavailability of 81% in rats."( Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
Fan, H; Gao, S; Guo, B; He, H; Huang, Y; Wang, H; Xin, Q; Yang, Y, 2011
)
0.37
" Two compounds were identified that exhibit both oral bioavailability in rat and clinically relevant bacterial susceptibility profiles against major respiratory pathogens."( Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
Achorn, C; Chen, CL; Clark, RB; Deng, Y; Fyfe, C; Grossman, TH; He, M; Hogan, PC; Hunt, DK; O'Brien, WJ; Plamondon, L; Rönn, M; Sutcliffe, JA; Xiao, XY; Zhu, Z, 2012
)
0.38
" Parametric population pharmacokinetic analysis was used to evaluate bioavailability and the influence of total body weight (TBW) on pharmacokinetic parameters."( Oral bioavailability of linezolid before and after Roux-en-Y gastric bypass surgery: is dose modification necessary in obese subjects?
Ameri, D; Hamilton, R; Pai, MP; Thai, XC, 2013
)
0.7
"The bioavailability of linezolid is not impaired by RYGBS."( Oral bioavailability of linezolid before and after Roux-en-Y gastric bypass surgery: is dose modification necessary in obese subjects?
Ameri, D; Hamilton, R; Pai, MP; Thai, XC, 2013
)
1.01
"Linezolid may be an interesting alternative for prosthetic joint infection (PJI) due to its bioavailability and its antimicrobial spectrum."( Linezolid in late-chronic prosthetic joint infection caused by gram-positive bacteria.
Ariza, J; Cobo, J; del Toro, MD; Euba, G; Jover-Sáenz, A; Lora-Tamayo, J; Palomino, J; Riera, M; Rodríguez-Pardo, D, 2013
)
3.28
" This study was conducted to evaluate the pharmacokinetics (PKs) and relative bioavailability of suspension (reference) and tablet (test) formulations of Linezolid (LZD)."( Pharmacokinetics and relative bioavailability evaluation of linezolid suspension and tablet formulations.
Helmy, SA, 2013
)
0.83
" Of primary importance when treating cSSTIs is the agent's clinical efficacy against the causative pathogens, as well as its bioavailability in the skin and associated structures."( European perspective and update on the management of complicated skin and soft tissue infections due to methicillin-resistant Staphylococcus aureus after more than 10 years of experience with linezolid.
Baguneid, M; Bassetti, M; Bouza, E; Dryden, M; Nathwani, D; Wilcox, M, 2014
)
0.59
" The high oral bioavailability of linezolid makes it an attractive oral alternative to glycopeptides and its use has increased in the last decade."( Clinical experience with linezolid for the treatment of orthopaedic implant infections.
García-Ramiro, S; Martínez-Pastor, JC; Mensa, J; Morata, L; Soriano, A; Tornero, E, 2014
)
0.98
" This antibiotic is bactericidal and is orally bioavailable in mice."( Structure-activity relationship for the oxadiazole class of antibiotics.
Antunes, NT; Boudreau, MA; Chang, M; Ding, D; Lastochkin, E; Leemans, E; Lichtenwalter, K; Mobashery, S; O'Daniel, PI; Peng, Z; Pi, H; Schroeder, VA; Song, W; Spink, E; Suckow, MA; Testero, SA; Vakulenko, S; Wolter, WR, 2015
)
0.42
" The compound also demonstrated high oral bioavailability (F = 99."( Discovery of a Teraryl Oxazolidinone Compound (S)-N-((3-(3-Fluoro-4-(4-(pyridin-2-yl)-1H-pyrazol-1-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)acetamide Phosphate as a Novel Antimicrobial Agent with Enhanced Safety Profile and Efficacies.
Ang, W; Chang, Y; Chen, G; Li, G; Liu, Y; Long, H; Luo, Y; Sang, Z; Tang, J; Wang, Z; Wei, Y; Yang, S; Yang, T; Yang, X; Zhang, J, 2015
)
0.42
" This new quinazolinone has potent activity against methicillin-resistant (MRSA) strains, low clearance, oral bioavailability and shows efficacy in a mouse neutropenic thigh infection model."( Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
Bastian, M; Bouley, R; Chang, M; Ding, D; Lastochkin, E; Mobashery, S; Peng, Z; Schroeder, VA; Song, W; Suckow, MA; Wolter, WR, 2016
)
0.43
" Pharmacokinetic parameters such as oral clearance, oral volume of distribution of the central compartment, time to reach maximum plasma concentration, absorption rate constant, and half-life in humans were predicted from animals using allometric scaling."( Prediction of Plasma Concentration-time Profiles of Drugs in Humans from Animals Following Oral Administration: An Allometric Approach.
Mahmood, I, 2016
)
0.43
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" The addition of other orally bioavailable anti-staphylococcal agents to tedizolid may be unlikely to improve killing but further research is warranted to assess the impact of these combinations on resistance prevention, or against biofilm-embedded organisms."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" Oral MRX-I was associated with a greater bioavailability and exposure when administered with food, and minimal accumulation of MRX-I occurred after multiple-dose administration."( Single- and Multiple-Dose Study To Determine the Safety, Tolerability, Pharmacokinetics, and Food Effect of Oral MRX-I versus Linezolid in Healthy Adult Subjects.
Eckburg, PB; Ge, Y; Hafkin, B, 2017
)
0.66
" Pharmacokinetic studies indicate that 1 has an oral bioavailability with an average F-value of 27."( An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
Eslamimehr, S; Franzblau, SG; Kong, Y; Kurosu, M; Lemieux, MR; Mitachi, K; Park, F; Pressly, JD; Siricilla, S; Wang, Y; Yang, D, 2018
)
0.48
" These compounds were found to be orally bioavailable and highly effective."( Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
Eswaran, S; Narayanan, S; Shivarudraiah, P; Shruthi, TG; Subramanian, S, 2019
)
0.51
" Consequently, compound 10 was orally bioavailable with a highly-acceptable pharmacokinetic profile in vivo that exhibited a half-life of 4 h and achieved a maximum plasma concentration that exceeded the minimum inhibitory concentration (MIC) values against all tested bacterial isolates."( Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
Abutaleb, NS; Elsebaei, MM; Hagras, M; Li, D; Mahgoub, AA; Mayhoub, AS; Mohammad, H; Seleem, MN, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Pharmacokinetic analysis showed that bioavailability of oral levonadifloxacin was 90% and similar pharmacokinetic profile of levonadifloxacin by both routes provide an option for IV to oral switch for the treatment of subjects."( Efficacy and Safety of a Novel Broad-Spectrum Anti-MRSA Agent Levonadifloxacin Compared with Linezolid for Acute Bacterial Skin and Skin Structure Infections: A Phase 3, Openlabel, Randomized Study.
Bhagwat, S; Bhatia, A; Chavan, R; Friedland, HD; Gutte, R; Joshi, P; Kumbhar, D; Llorens, L; Mastim, M; Palwe, SR; Patel, M; Periasamy, H; Shah, M, 2020
)
0.78
"Many lead compounds fail to reach clinical trials despite being potent because of low bioavailability attributed to their insufficient solubility making solubility a primary and crucial factor in early phase drug discovery."( Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Baidya, ATK; Das, B; Kumar, R; Mathew, AT; Yadav, AK, 2022
)
0.72
" para-Aminosalicylic acid (PAS), an important second-line agent for treating drug-resistant Mycobacterium tuberculosis, has moderate bioavailability and rapid clearance that necessitate high daily doses of up to 12 g per day, which in turn causes severe gastrointestinal disturbances presumably by disruption of gut microbiota and host epithelial cells."( Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
Aldrich, CC; Baughn, AD; Boshoff, HIM; Dartois, V; Hegde, PV; Howe, MD; Jia, Z; Pan, Y; Remache, B; Sharma, S; Zimmerman, MD, 2022
)
0.72
" Postoperatively, the study group had higher bone graft fusion rate, shorter mean bone graft fusion time, and higher paraspinal cyst absorption rate than the control group (P<0."( Analysis of efficacy and safety of linezolid-based chemotherapeutic regimens for patients with postoperative multidrug-resistant spinal tuberculosis.
Dai, X; Feng, J; Qiao, J; Xia, P; Xu, F; Yang, L, 2022
)
1
" Oxazolidinone antibiotics such as linezolid have excellent oral bioavailability and provide coverage against MRSA infections."( The Novel Oxazolidinone TBI-223 Is Effective in Three Preclinical Mouse Models of Methicillin-Resistant Staphylococcus aureus Infection.
Archer, NK; Dikeman, DA; Fotouhi, N; Gordon, O; Gough, E; Kaushik, A; Miller, LS; Mumtaz, M; Nuermberger, EL; Orlando, N; Ortines, RV; Patel, AM; Upton, AM; Wang, Y; Youn, C; Zhang, J, 2022
)
1
"This study is an economic analysis seeking to examine cost savings that may be accrued from usage of oral linezolid in place of OPAT IV daptomycin in patients requiring prolonged courses of IV or highly bioavailable oral antibiotic therapy."( A cost minimisation analysis comparing oral linezolid and intravenous daptomycin administered via an outpatient parenteral antibiotic therapy programme in patients requiring prolonged antibiotic courses.
Faller, E; Jackson, A, 2023
)
1.39

Dosage Studied

A daily dosage of 600 mg of linezolid was well tolerated without stopping treatment in any case. A tedizolid dose of 200 mg/day or 700 mg twice a week is recommended for testing in patients.

ExcerptRelevanceReference
" faecalis sera from patients dosed with either drug were generally inhibitory at the peak timepoint, but at trough only linezolid exhibited a persistent effect."( Serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid.
Batts, DH; Daley-Yates, PT; Pawsey, SD; Schaadt, RD; Stalker, DJ; Zurenko, GE, 1997
)
0.7
" A dose-response study was performed with PNU-100480 and linezolid (both at 25, 50, and 100 mg/kg of body weight)."( Activities of several novel oxazolidinones against Mycobacterium tuberculosis in a murine model.
Chase, S; Cynamon, MH; Klemens, SP; Sharpe, CA, 1999
)
0.55
" At a dosage of 100 mg/kg/day, linezolid treatment led to an approximately 100-fold reduction in viable cells per gram of abscess."( Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium.
Eliopoulos, GM; Moellering, RC; Schülin, T; Thauvin-Eliopoulos, C, 1999
)
0.87
" 1 mirogram/ml at 16 to 17 h after orogastric dosing at 25 mg/kg."( Efficacy of linezolid in experimental otitis media.
Albut, R; Figueira, M; Pelton, SI; Stalker, D, 2000
)
0.69
" Unpublished clinical data, adverse effects, and dosing information were abstracted from product labeling."( Linezolid for the treatment of resistant gram-positive cocci.
Bain, KT; Wittbrodt, ET, 2001
)
1.75
" Results of PAE testing support twice-daily dosing of linezolid in humans."( Post-antibiotic growth suppression of linezolid against Gram-positive bacteria.
Giles, C; Munckhof, WJ; Turnidge, JD, 2001
)
0.83
") dosed linezolid and intravenously (i."( Efficacy of linezolid in treatment of experimental endocarditis caused by methicillin-resistant Staphylococcus aureus.
Batts, DH; Buchanan, LV; Dailey, CF; Dileto-Fang, CL; Ford, CW; Gibson, JK; Oramas-Shirey, MP, 2001
)
1.12
" We demonstrated equivalence of intravenous and oral dosing in this patient, suggesting that oral linezolid may be an excellent alternative to intravenous vancomycin for CF patients infected with MRSA."( Successful treatment of methicillin-resistant Staphylococcus aureus pulmonary infection with linezolid in a patient with cystic fibrosis.
Blumberg, EA; Ferrin, M; Meagher, A; Zuckerman, JB, 2002
)
0.75
" Blood and urine samples were collected until 48 h after dosing and assayed for linezolid concentrations using a validated high-performance liquid chromatography method."( Age and sex effects on the pharmacokinetics of linezolid.
Hopkins, NK; Jungbluth, GL; Sisson, TL, 2002
)
0.8
"9, respectively, and the percentage of time the drug remained above the MIC for the 12-h dosing interval was 100%; the corresponding ratios in ELF were 120 and 16."( Intrapulmonary pharmacokinetics of linezolid.
Conte, JE; Golden, JA; Kipps, J; Zurlinden, E, 2002
)
0.59
" Dosage reductions are not necessary, even in severe renal impairment, but about one third of the dose is eliminated during dialysis."( [New treatment option for gram-positive infections in critically ill patients - overview over linezolid].
Krueger, WA; Unertl, KE, 2002
)
0.53
" Results are in agreement with the assumption of a limited accumulation of linezolid under the dosage regimen given."( Single- and multiple-dose pharmacokinetics of linezolid and co-amoxiclav in healthy human volunteers.
Borner, K; Burkhardt, O; Köppe, P; Lode, H; Nord, CE; Pletz, MW; von der Höh, N, 2002
)
0.8
" A rabbit endocarditis model was used to compare the in vivo activities of different linezolid regimens mimicking intermittent dosing of 10 mg/kg of body weight every 12 h for 5 days or continuous (constant-rate) infusion of a daily dose of 20 mg/kg (for 5 days) or 40 mg/kg (for 3 and 5 days) and the activities of intermittent dosing and continuous infusion of vancomycin (for 5 days)."( In vivo efficacy of continuous infusion versus intermittent dosing of linezolid compared to vancomycin in a methicillin-resistant Staphylococcus aureus rabbit endocarditis model.
Batard, E; Boutoille, D; Bugnon, D; Caillon, J; Hamel, A; Jacqueline, C; Kergueris, MF; Perez, L; Potel, G, 2002
)
0.77
" Oral bioavailability in humans was determined to be 100% and twice daily dosing in humans resulted in blood levels which even at trough values were in excess of the MIC90 for significant Gram-positive pathogens."( The discovery of linezolid, the first oxazolidinone antibacterial agent.
Barbachyn, MR; Ford, CW; Zurenko, GE, 2001
)
0.65
"Patients received linezolid in a dosage of 600 mg intravenously (iv) and/or orally twice daily."( The efficacy and safety of linezolid as treatment for Staphylococcus aureus infections in compassionate use patients who are intolerant of, or who have failed to respond to, vancomycin.
Birmingham, MC; Forrest, A; Moise, PA; Schentag, JJ, 2002
)
0.95
" Drug concentration and half-life were adjusted to simulate clinical dosing (600 mg twice daily) of linezolid."( Comparison of linezolid activities under aerobic and anaerobic conditions against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium.
Gunderson, BW; Hovde, LB; Ibrahim, KH; Peloquin, CA; Rotschafer, JC, 2003
)
0.9
" Virtually complete oral bioavailability allows for 1:1 conversion between the intravenous and oral dosage forms."( Linezolid: an oxazolidinone antimicrobial agent.
Paladino, JA, 2002
)
1.76
" Its elimination half-life allows dosing twice per day, and alteration of drug dosage is not required in patients with impaired renal or hepatic function."( Linezolid: the first oxazolidinone antimicrobial.
Moellering, RC, 2003
)
1.76
" The potential for alternative day or thrice weekly dosing with teicoplanin may offer further cost advantages whilst maintaining equivalent clinical effectiveness."( Cost-minimization analysis and audit of antibiotic management of bone and joint infections with ambulatory teicoplanin, in-patient care or outpatient oral linezolid therapy.
Ajdukiewicz, K; Barlow, GD; Clift, B; Davey, P; France, AJ; Gray, K; Morrison, J; Nathwani, D, 2003
)
0.52
"0 mg/L) for the majority of the 12 h dosing interval."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.55
"Oral and intravenous linezolid exhibit linear pharmacokinetics, with concentrations remaining above the target MIC90 for most of the dosing interval."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.86
" Terminal phase tissue residue and excretion data were compared to data from rats dosed orally with [(14)C]sodium acetate."( Assessment of radioactive residues arising from radiolabel instability in a multiple dose tissue distribution study in rats.
Chiba, K; Courtney, M; Easter, JA; Fate, GD; Johnson, MG; Jones, BW; Koets, MD; Norris, LR; Sams, JP; Slatter, JG, 2003
)
0.32
"Ten adult patients undergoing bronchoscopy for diagnostic purposes were given oral linezolid at a dosage of 600 mg twice a day for a total of six doses."( Intrapulmonary penetration of linezolid.
Andrews, J; Honeybourne, D; Jevons, G; Tobin, C; Wise, R, 2003
)
0.83
" teicoplanin) dosed per approved prescription information."( Hospital resource use and cost of treatment with linezolid versus teicoplanin for treatment of serious gram-positive bacterial infections among hospitalized patients from South America and Mexico: results from a multicenter trial.
Balan, DA; Li, JZ; López, H; Mozaffari, E; Rittenhouse, BE; Tang, T; Vidal, G; Willke, RJ; Zitto, T, 2003
)
0.57
" We conclude that no adjustment of the linezolid dosage is needed in subjects with renal dysfunction or subjects on hemodialysis."( Pharmacokinetics of linezolid in subjects with renal dysfunction.
Aronoff, GR; Batts, DH; Brier, ME; Hopkins, NK; Jungbluth, GL; O'Grady, M; Ryan, KK; Stalker, DJ, 2003
)
0.91
" Therefore it is important to determine the specific pharmacokinetic characteristics for individual drugs in pediatric patients so that appropriate age-specific dosage regimens can be developed and evaluated in clinical trials."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
1.76
"Because of the higher clearance and lower area under the drug concentration-time curve, a shorter dosing interval for linezolid is required for children younger than 12 years of age to produce adequate drug exposure against target Gram-positive pathogens."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
1.97
" Dosing frequency (two to three times daily) varied depending on age and clinical diagnosis."( Safety and tolerability of linezolid in children.
Bruss, JB; Edge-Padbury, B; Goldfarb, J; Kaplan, SA; Naberhuis-Stehouwer, S; Saiman, L; Wible, K, 2003
)
0.62
" The nonlinearity is not relevant over the therapeutic dosage range."( Clinical pharmacokinetics of linezolid, a novel oxazolidinone antibacterial.
Jungbluth, GL; Stalker, DJ, 2003
)
0.61
" Evaluation of the pharmacokinetic data would appear to support the use of linezolid dosing regimens currently approved for infants and young children in neonates with postnatal age greater than 7 days."( Impact of ontogeny on linezolid disposition in neonates and infants.
Abdel-Rahman, SM; Bruss, JB; Grzebyk, RP; Hopkins, NK; Jungbluth, GL; Kearns, GL; Van Den Anker, JN; Welshman, IR, 2003
)
0.86
" Chance of success in bacteraemia, LRTI and SSSI also appear to be higher when concentrations remain above the MIC for the entire dosing interval."( Clinical pharmacodynamics of linezolid in seriously ill patients treated in a compassionate use programme.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.61
"A simple, selective, precise, and stability-indicating high-performance thin layer chromatographic method of analysis of Linezolid both as a bulk drug and in formulations was developed and validated in pharmaceutical dosage form."( Stability indicating HPTLC determination of linezolid as bulk drug and in pharmaceutical dosage form.
Agrawal, H; Kaul, N; Mahadik, KR; Paradkar, AR, 2003
)
0.79
"The pharmacokinetics of many drugs are altered in patients with cystic fibrosis (CF), often necessitating different dosage requirements than those used in non-CF patients."( Linezolid pharmacokinetics in adult patients with cystic fibrosis.
Bosso, JA; Flume, PA; Gray, SL, 2004
)
1.77
"An in vitro pharmacodynamic model was used to simulate standard dosing regimens of linezolid, levofloxacin, and vancomycin against the isolates 79, R921, and P9802-020."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
1.99
" The appearance of increasing antimicrobial resistance can challenge the efficacy of these drugs when concentrations do not exceed the MIC for 40% to 50% of the dosing interval."( Basic pharmacodynamics of antibacterials with clinical applications to the use of beta-lactams, glycopeptides, and linezolid.
Craig, WA, 2003
)
0.53
" Mean levels exceed the required MIC for the treatment of MRSA for >80% of the dosing period for serum and the majority of the dosing period for sputum."( Serum and sputum concentrations following the oral administration of linezolid in adult patients with cystic fibrosis.
Conway, S; Denton, M; Etherington, C; Hulme, B; Peckham, DG; Saralaya, D; Tobin, CM, 2004
)
0.56
"At the conclusion of this learning activity, participants should be familiar with the modes of action, clinical indications, dosage regimens, and contraindications and cautions for several novel antibacterial agents for skin and skin structure infections."( Novel antibacterial agents for skin and skin structure infections.
Schweiger, ES; Weinberg, JM, 2004
)
0.32
" The findings of these studies collectively suggest that once-daily dosing of telavancin may provide an effective approach for the treatment of clinically relevant infections with gram-positive organisms."( Pharmacodynamics of telavancin (TD-6424), a novel bactericidal agent, against gram-positive bacteria.
Hegde, SS; Judice, JK; Kaniga, K; McCullough, J; Obedencio, G; Pace, J; Reyes, N; Shaw, JP; Skinner, R; Thomas, R; Vanasse, N; Wiens, T, 2004
)
0.32
" It is not known whether dosage adjustments are necessary in patients treated with continuous renal replacement therapies."( Elimination of linezolid by an in vitro extracorporeal circuit model.
Hansen, M; Hoffmann, E; Krueger, WA; Schroeder, TH; Stephan, M; Unertl, K, 2004
)
0.68
" It exhibits good penetration into pulmonary, as well as skin and related structure tissues, and does not require dosage adjustment in hepatic or renal dysfunction."( A review of linezolid: the first oxazolidinone antibiotic.
Dotter, B; Madaras-Kelly, K; Stevens, DL, 2004
)
0.7
" Human therapeutic dosing regimens for nafcillin, daptomycin, vancomycin, linezolid, and gentamicin were simulated."( Impact of high-inoculum Staphylococcus aureus on the activities of nafcillin, vancomycin, linezolid, and daptomycin, alone and in combination with gentamicin, in an in vitro pharmacodynamic model.
LaPlante, KL; Rybak, MJ, 2004
)
0.78
" Serum levels exceeded the breakpoint of 4 mg/L for the entire dosing interval in all subjects (400 mg dose every 12 h) with an AUC/MIC of 399."( Pharmacokinetic studies of linezolid and teicoplanin in the critically ill.
Aarons, L; Cepeda, JA; Kibbler, C; MacGowan, A; Nalda-Molina, R; Shaw, S; Shulman, R; Singer, M; Tobin, C; Whitehouse, T; Wilson, AP, 2005
)
0.63
"Linezolid dosage at 600 mg every 12 h was adequate in the critically ill without need for adjustment for renal function."( Pharmacokinetic studies of linezolid and teicoplanin in the critically ill.
Aarons, L; Cepeda, JA; Kibbler, C; MacGowan, A; Nalda-Molina, R; Shaw, S; Shulman, R; Singer, M; Tobin, C; Whitehouse, T; Wilson, AP, 2005
)
2.07
"Single-lumen central venous catheters colonized with biofilm-embedded Staphylococcus aureus, Staphylococcus epidermidis or vancomycin-resistant Enterococcus faecium (VRE) were treated with simulated clinical dosing regimens of linezolid 600 mg every 12 h or vancomycin 1 g every 12 h in a one-compartment in vitro pharmacodynamic model."( Antibacterial activity of linezolid and vancomycin in an in vitro pharmacodynamic model of gram-positive catheter-related bacteraemia.
Coyle, EA; Lewis, RE; Prince, RA; Raad, II; Wiederhold, NP, 2005
)
0.81
" The venlafaxine dosage was decreased to 150 mg/day, and symptoms gradually abated over 36 hours."( Serotonin toxicity associated with concomitant use of linezolid.
Bergeron, L; Boulé, M; Perreault, S, 2005
)
0.58
"Clinicians should pay special attention to patients treated with serotonergic drugs, especially those receiving dosages in the higher end of the normal range who are prescribed linezolid, and consider tapering or reducing the dosage of serotonergic drugs for the duration of antibiotic therapy."( Serotonin toxicity associated with concomitant use of linezolid.
Bergeron, L; Boulé, M; Perreault, S, 2005
)
0.77
" The aim of this prospective, single-centre, open-label, two-arm study was to investigate the pharmacokinetics of linezolid during continuous venovenous haemofiltration (CVVH) in critically ill patients and to derive a dosage recommendation."( Multiple-dose pharmacokinetics of linezolid during continuous venovenous haemofiltration.
Heinz, G; Jaeger, W; Karth, GD; Kornek, GV; Locker, GJ; Meyer, B; Nikfardjam, M; Thalhammer, F, 2005
)
0.82
" These data suggest that a schedule of 600 mg linezolid at least twice daily may also be an appropriate dosing for patients with severe Gram-positive infections undergoing CVVH with both types of membranes."( Multiple-dose pharmacokinetics of linezolid during continuous venovenous haemofiltration.
Heinz, G; Jaeger, W; Karth, GD; Kornek, GV; Locker, GJ; Meyer, B; Nikfardjam, M; Thalhammer, F, 2005
)
0.87
" This suggests that a dosage of 600 mg administered intravenously twice daily to critically ill patients with Gram-positive ventilator-associated pneumonia would achieve success against organisms with minimum inhibitory concentrations as high as 2-4 mg/L in both plasma and epithelial lining fluid."( Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC; Toutain, J, 2005
)
0.58
" Because the vitreous concentrations appeared to exponentially trend upward with time and 33% of the late group achieved sufficient MIC90 levels for the common pathogens found in postoperative endophthalmitis, adequate concentrations might be achieved with an altered dosing regimen to achieve higher serum steady state levels."( Human vitreous distribution of linezolid after a single oral dose.
Ciulla, TA; Comer, GM; Peloquin, C; Wheeler, J,
)
0.42
" The oral bioavailability of linezolid is approximately 100%, thus allowing sequential intravenous-to-oral administration without changing the drug or dosage regimen."( Linezolid: a pharmacoeconomic review of its use in serious Gram-positive infections.
Figgitt, DP; Plosker, GL, 2005
)
2.06
"v) and oral dosing and to compare the pharmacokinetics with those obtained following linezolid dosing."( Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid.
Bhamidipati, R; Das, J; Dravid, PV; Mullangi, R; Narasimhulu, PC; Srinivas, NR; Tvrs, S; Venkatesh, P,
)
0.56
" Treatment with linezolid at a dosage of 10 mg/kg every 8 h intravenously for a duration of 16 days and 14 days, respectively, was well tolerated and led to complete clinical recovery and clearance of the organism from all body sites."( Linezolid treatment of glycopeptide-resistant Enterococcus faecium in very low birth weight premature neonates.
Bauer, K; Groll, AH; Hoehn, R; Schaefer, V; Schloesser, RL, 2006
)
2.12
" This may be due to the poor penetration of vancomycin into the lung, and alternate dosing regimens to increase tissue levels need to be further studied."( Methicillin-Resistant S. aureus Ventilator-Associated Pneumonia: Strategies to Prevent and Treat.
Lam, AP; Wunderink, RG, 2006
)
0.33
" Our findings emphasise the importance of optimal dosage of linezolid to prevent the emergence of resistance."( Emergence of linezolid-resistant Staphylococcus aureus during treatment of pulmonary infection in a patient with cystic fibrosis.
Andrade, SS; Barth, AL; Gales, AC; Lutz, L; Machado, A; Sader, HS, 2006
)
0.95
" It does not appear that supplemental dosing of linezolid is necessary in patients undergoing CVVHDF."( Clearance of linezolid via continuous venovenous hemodiafiltration.
Assaly, R; Malhotra, D; Mauro, LS; Peloquin, CA; Schmude, K, 2006
)
0.96
" Based on the model-predicted unbound concentrations in ISF, a scheme of more-frequent daily dosing of linezolid for some critically ill patients might be taken into consideration to avoid subinhibitory unbound concentrations in the infected tissue."( Pharmacokinetics of unbound linezolid in plasma and tissue interstitium of critically ill patients after multiple dosing using microdialysis.
Buerger, C; Dehghanyar, P; Joukhadar, C; Kloft, C; Plock, N, 2006
)
0.84
"Although daily-half doses of linezolid were effective in patients with intractable or extensive MDR-TB, this dosage regimen did not reduce long-term use-related side effects, such as peripheral and optic neuropathy."( Efficacy and tolerability of daily-half dose linezolid in patients with intractable multidrug-resistant tuberculosis.
Hong, SB; Kim, DS; Kim, MN; Kim, WD; Kim, WS; Koh, Y; Lee, SD; Lim, CM; Oh, YM; Park, IN; Shim, TS, 2006
)
0.88
" The serum and CSF linezolid concentrations exceeded the pharmacodynamic breakpoint of 4 microg/ml for susceptible target pathogens for the entire dosing interval in the majority of patients."( Serum and cerebrospinal fluid concentrations of linezolid in neurosurgical patients.
Anagnostaki, M; Baltopoulos, G; Boutzouka, E; Markantonis, SL; Myrianthefs, P; Panidis, D; Vlachos, K, 2006
)
0.92
" Urine samples were taken every 2 h during the whole dosing interval of the particular antibiotic."( Urinary bactericidal activity of oral antibiotics against common urinary tract pathogens in an ex vivo model.
Bedenic, B; Bubonja, M; Budimir, A; Topic, M, 2006
)
0.33
" Once-a-week dosing with dalbavancin may obviate the need for the continued presence of IV lines in some patients, which could translate into fewer local infections and blood stream infections and which could facilitate transfer of the patients to skilled nursing facilities."( Dalbavancin: a review for dermatologists.
Scheinfeld, N, 2006
)
0.33
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Linezolid, active against methicillin-resistant strains and available in oral and intravenous dosage forms, is a potential alternative to vancomycin for the treatment of PJIs."( Linezolid versus vancomycin for prosthetic joint infections: a cost analysis.
Cheung, KW; Hui, M; Lee, GC; So, RK; You, JH, 2007
)
2.69
" aregenerative anemia, neutropenia and thrombopenia, developed 3 weeks and 5 weeks after initiating linezolid therapy at a conventional dosage (600 mg bid)."( Linezolid-related pancytopenia in organ-transplant patients: report of two cases.
Faguer, S; Fillola, G; Guitard, J; Kamar, N; Rostaing, L, 2007
)
2
" Furthermore, bactericidal activity (titres > or = 1:2) was observed for at least 6 h (50% of the dosing interval) against four of these five strains."( Linezolid tissue penetration and serum activity against strains of methicillin-resistant Staphylococcus aureus with reduced vancomycin susceptibility in diabetic patients with foot infections.
Havlichek, DH; Missavage, A; Peloquin, CA; Schooley, S; Stein, GE, 2007
)
1.78
" The patient did not respond to 5 days of appropriately dosed linezolid and daptomycin and remained bacteremic because abscess drainage was not an option in this case and the continuous, high-grade MRSA bacteremia continued despite appropriate therapy."( Methicillin-resistant Staphylococcus aureus (MRSA) mitral valve acute bacterial endocarditis (ABE) in a patient with Job's syndrome (hyperimmunoglobulin E syndrome) successfully treated with linezolid and high-dose daptomycin.
Cunha, BA; Kodali, V; Krol, V,
)
0.56
" In response, some clinicians increased vancomycin dosing to >or=4 g/day."( Larger vancomycin doses (at least four grams per day) are associated with an increased incidence of nephrotoxicity.
Drusano, GL; Graves, J; Lodise, TP; Lomaestro, B, 2008
)
0.35
" Therefore, a correct dosing regimen for the time-dependent molecules (i."( [Pharmacological rationale for choice of antibiotics for intraabdominal infections].
Mazzei, T; Novelli, A, 2008
)
0.35
" The lower dosage for the pharmacodynamically optimized regimen may decrease drug toxicity."( Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
Brown, DL; Drusano, GL; Heine, HS; Kim, K; Kinzig-Schippers, M; Liu, W; Louie, A; Sörgel, F; VanScoy, B, 2008
)
0.6
" However, in the current study we show LZD accumulation occurring with repeated dosing during hemodialysis in a 64-year-old man receiving hemodialysis treatment."( Pharmacokinetics of repeated dosing of linezolid in a hemodialysis patient with chronic renal failure.
Hayashi, W; Hiraki, Y; Kamimura, H; Kamohara, R; Karube, Y; Mizoguchi, A; Tsuji, Y, 2008
)
0.62
" However, our drug level results suggest that further investigation is needed to determine the optimal dosing of linezolid in treatment of central nervous system infection in pediatric patients."( Successful treatment of vancomycin-resistant enterococcal ventriculitis in a pediatric patient with linezolid.
Maranich, AM; Rajnik, M, 2008
)
0.77
" aureus strains was studied by in vitro simulation of 5-day antibiotic dosing over a wide range of AUC(24)/MIC ratios."( Linezolid pharmacodynamics with Staphylococcus aureus in an in vitro dynamic model.
Firsov, AA; Lubenko, IY; Portnoy, YA; Smirnova, MV; Strukova, EN; Vostrov, SN; Zinner, SH, 2009
)
1.8
" Linezolid was administered intravenously at a dosage of 10 mg/kg every 8 h and then orally."( Pharmacokinetics and tolerance of linezolid for meticillin-resistant Staphylococcus aureus mediastinitis in paediatric patients.
Fujita, N; Hamaoka, K; Kato, R; Kokufu, T; Kosaka, T; Shime, N; Sugioka, N, 2009
)
1.54
"Linezolid clearance is enhanced in children with CF requiring a higher dosage regimen."( Pharmacokinetics and pharmacodynamics of linezolid in children with cystic fibrosis.
Ahmad, N; Brown, ME; Jafri, HS; McCracken, GH; Murphey, DK; Prestidge, CB; Salvatore, CM; Sanchez, PJ; Santos, RP; Siegel, JD; Urbancyzk, B, 2009
)
2.06
" These changes are of sufficient magnitude that linezolid concentrations may be sub-therapeutic in some patients and we suggest that the dosage interval may need to be decreased in this patient population."( Pharmacokinetic evaluation of linezolid in patients with major thermal injuries.
Birraux, G; Bret, P; Hovsepian, L; Le Floch, R; Lovering, AM; Stephanazzi, J; Vinsonneau, C, 2009
)
0.9
"48, %T(MSW) (% of the dosing interval that concentrations fall in the MSW)=40%] and ATCC 51299 and GP32 (AUC/MIC=30."( In vitro analysis of resistance selection by linezolid in vancomycin-susceptible and -resistant Enterococcus faecalis and Enterococcus faecium.
Allen, GP; Bierman, BC, 2009
)
0.61
" We conclude that pharmacokinetics of linezolid are altered in burn patients, in a magnitude sufficient that linezolid concentration may be subtherapeutic in some patients and we suggest that the dosage interval may need to be decreased in this patient population."( [Pharmacokinetic evaluation of linezolid in patients with major thermal injuries].
Arnould, JF; Birraux, G; Bret, P; Hovsepian, L; Le Floch, R; Lovering, AM; Stephanazzi, J; Vinsonneau, C, 2010
)
0.92
"001) than were cefazolin, vancomycin, or linezolid based on the dose-response profiles."( In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
Abbanat, D; Bush, K; Fernandez, J; Flamm, RK; Hilliard, JJ; Melton, JL; Santoro, CM; Zhang, W, 2010
)
0.63
" The dosage of linezolid was 600 mg daily."( Linezolid in the treatment of multidrug-resistant tuberculosis.
Flood, J; Mase, S; Raftery, A; Schecter, GF; Scott, C; True, L, 2010
)
2.16
" This study was limited due to an inability to assess for the effects of hetero-resistance and appropriate vancomycin dosing on outcomes."( Efficacy and safety of linezolid in methicillin-resistant Staphylococcus aureus (MRSA) complicated skin and soft tissue infection (cSSTI): a meta-analysis.
Bounthavong, M; Hsu, DI, 2010
)
0.67
" The best method of managing linezolid dosage in such a complex group of patients, whose physiology can vary daily, would be to use therapeutic drug monitoring."( Pharmacokinetics of linezolid in septic patients with and without extended dialysis.
Haefeli, WE; Hempel, G; Hoppe-Tichy, T; Lichtenstern, C; Ober, MC; Saleh, S; Schwenger, V; Sonntag, HG; Swoboda, S; Weigand, MA, 2010
)
0.98
"95 but appeared not clinically relevant because it did not result in different dosing advice."( Limited sampling strategies for therapeutic drug monitoring of linezolid in patients with multidrug-resistant tuberculosis.
Alffenaar, JW; Kosterink, JG; Proost, JH; Uges, DR; van Altena, R; van der Werf, TS, 2010
)
0.6
" Recently, the therapeutic efficacy of vancomycin in the treatment of hospitalized patients with MRSA infections has been questioned due to the emergence of MRSA strains with reduced susceptibility to vancomycin together with concerns related to inadequate dosing and poor tissue penetration of the drug."( The importance of tissue penetration in achieving successful antimicrobial treatment of nosocomial pneumonia and complicated skin and soft-tissue infections caused by methicillin-resistant Staphylococcus aureus: vancomycin and linezolid.
Stein, GE; Wells, EM, 2010
)
0.54
" Linezolid demonstrates adequate penetration into lung and other soft issues with sustained concentrations above the minimum inhibitory concentrations for susceptible pathogens, including MRSA, for the majority of the dosing interval."( The importance of tissue penetration in achieving successful antimicrobial treatment of nosocomial pneumonia and complicated skin and soft-tissue infections caused by methicillin-resistant Staphylococcus aureus: vancomycin and linezolid.
Stein, GE; Wells, EM, 2010
)
1.45
" As a consequence, studies have recommended higher doses or more frequent dosing or both for some antibiotics in patients with major burns, but data are lacking for many of the antibiotics reserved for treatment of life-threatening infections."( Potential subtherapeutic linezolid and meropenem antibiotic concentrations in a patient with severe burns and sepsis.
Allen, JM; Davies, JG; Dheansa, BS; Donaldson, PM; Hallam, MJ; Hanlon, GW; James, SE,
)
0.43
" Due to its bacteriostatic property, the cumulative percentages of the dosing interval during which the drug concentration exceeded the MIC (T > MIC), 66."( Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
Arpin, C; Ba, BB; Bikie Bi Nso, B; Dubois, V; Quentin, C; Saux, MC, 2010
)
0.74
" In Group 2, eyes were dosed in accordance with a keratitis protocol (1 drop of 2 mg/mL every 15 minutes for 1 hour)."( Ocular penetration of topically applied linezolid in a rabbit model.
Bourcier, T; Dory, A; Gaucher, D; Jehl, F; Lefevre, S; Prevost, G; Saleh, M; Sauer, A; Speeg-Schatz, C, 2010
)
0.63
" When coadministered with rifampin, area under the plasma concentration-time curve over the dosing interval and maximum concentration values for linezolid were reduced approximately 32% and 21%, respectively."( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism.
Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011
)
0.81
" Linezolid was administered intravenously twice daily at a dosage of 600 mg."( Linezolid concentrations in infected soft tissue and bone following repetitive doses in diabetic patients with bacterial foot infections.
Joukhadar, C; Mauric, O; Popovic, M; Scharnagl, E; Schintler, MV; Spendel, S; Traunmüller, F, 2010
)
2.71
" However, in vitro dose-response curves for bone chips impregnated with different kinds of antibiotics are not available."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" In a separate experiment, in vitro dose-response curves were established for bone chips impregnated with cefazolin and vancomycin solutions at five different concentrations."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" The in vitro dose-response curves show that the free-zone diameter increases logarithmically with antibiotic concentration."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" The in vitro dose-response curve can be used to determine the optimal concentration(s) for local application."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" Nearly 70% of the respondent hospitals reported having a vancomycinspecific dosing or monitoring guideline in place."( Hospital policies and practices on prevention and treatment of infections caused by methicillin-resistant Staphylococcus aureus.
Hennenfent, J; Lambert, BL; McBride, MV; Rodvold, KA; Schiff, G; Schumock, GT; Trese, AM; Tverdek, F; Yang, Y, 2010
)
0.36
" An optimal antibacterial effect is achieved when plasma drug concentrations are above the minimum inhibitory concentration (MIC) [T>MIC] for the entire length of treatment and the ratio between the area under the plasma concentration-time curve (AUC) and the MIC (AUC/MIC) is greater than 100, as is most commonly obtained with administration of the standard dosage of linezolid 600 mg twice daily."( Pharmacological issues of linezolid: an updated critical review.
Danesi, R; Del Tacca, M; Di Paolo, A; Guidotti, E; Malacarne, P, 2010
)
0.83
" A dosage regimen of 10mg/kg body weight given either orally or intravenously every 8h in infants aged >or=1 week and the same dose given every 12h in infants <1 week was shown to be safe and effective with a mean treatment duration of 10-28 days."( Linezolid treatment of nosocomial bacterial infection with multiresistant Gram-positive pathogens in preterm infants: a systematic review.
Kocher, S; Müller, W; Resch, B, 2010
)
1.8
" In order to reduce its adverse effects and maintain efficacy, we investigated whether linezolid in a reduced dosage resulted in drug serum concentrations exceeding a ratio of the in vitro minimum inhibitory concentration (MIC) to the area under the serum concentration-time curve (AUC) over 24 hours (AUC(24)) [AUC(24)/MIC] of >100."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
0.82
" Larger numbers of patients should be studied to confirm the efficacy of the linezolid 300 mg twice-daily dosage in MDR-TB or XDR-TB treatment."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
0.83
"The objective of the present retrospective observational study carried out in patients receiving a standard dosage of linezolid and undergoing routine therapeutic drug monitoring (TDM) was to assess the interindividual variability in plasma exposure, to identify the prevalence of attainment of optimal pharmacodynamics, and to define if an intensive program of TDM may be warranted in some categories of patients."( Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
Cojutti, P; Cristini, F; Franceschi, L; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2010
)
0.86
" Further investigation into β-lactam dosing strategies against different BORSA strains is warranted in order to avoid possible therapy failure."( Diminished in vitro antibacterial activity of oxacillin against clinical isolates of borderline oxacillin-resistant Staphylococcus aureus.
Beisser, PS; Croes, S; Deurenberg, RH; Neef, C; Stobberingh, EE; Terporten, PH, 2010
)
0.36
" There were no hematologic or other safety signals during 28 days of dosing at 600 mg twice daily."( Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis.
Bedarida, G; Campbell, S; Jakubiec, W; Kumar, V; Ladutko, L; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, A; Wallis, RS; Zhu, T, 2011
)
0.37
" Linezolid was given at a dosage of 600 mg, iv, q12h."( [Clinical analysis of 102 blood disease patients with gram positive cocci infection treated with Linezolid].
Fu, R; Guan, J; Liang, Y; Liu, H; Qu, W; Ruan, EB; Shao, ZH; Song, J; Wang, GJ; Wang, HQ; Wang, XM; Wu, YH; Xing, LM, 2010
)
1.49
" For a successful therapy it is of vital importance that these compounds are used judiciously and dosed appropriately."( Comparison of the pharmacokinetic properties of vancomycin, linezolid, tigecyclin, and daptomycin.
Derendorf, H; Estes, KS, 2010
)
0.6
"To address issues of antibiotic dosing during sustained low-efficiency dialysis by using available pharmacokinetic data, intermittent and continuous renal replacement therapy dialysis guidelines, and our experience with sustained low-efficiency dialysis."( Antibiotic dosing during sustained low-efficiency dialysis: special considerations in adult critically ill patients.
Bogard, KN; Erwin, MW; Fuller, PD; Olsen, KM; Peterson, NT; Plumb, TJ, 2011
)
0.37
"Published clinical trials, case reports, and reviews of antibiotic dosing in humans during sustained low-efficiency dialysis."( Antibiotic dosing during sustained low-efficiency dialysis: special considerations in adult critically ill patients.
Bogard, KN; Erwin, MW; Fuller, PD; Olsen, KM; Peterson, NT; Plumb, TJ, 2011
)
0.37
" Appropriate dose and calculation of dosing intervals is essential to provide adequate antibiotic therapy in these patients."( Antibiotic dosing during sustained low-efficiency dialysis: special considerations in adult critically ill patients.
Bogard, KN; Erwin, MW; Fuller, PD; Olsen, KM; Peterson, NT; Plumb, TJ, 2011
)
0.37
" This stresses the importance of an optimal dosing of the antibiotic when SCVs are present."( Intra- and extracellular activities of dicloxacillin and linezolid against a clinical Staphylococcus aureus strain with a small-colony-variant phenotype in an in vitro model of THP-1 macrophages and an in vivo mouse peritonitis model.
Frimodt-Møller, N; Hughes, D; Lemaire, S; Sandberg, A; Tulkens, PM; Van Bambeke, F; von Eiff, C, 2011
)
0.61
" The present population pharmacokinetic/pharmacodynamic (PPK/PD) study was undertaken to elucidate the factors that determine linezolid levels, the relationship between exposure to linezolid and a decrease in platelet counts, and appropriate dosage adjustments based on exposure levels."( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
0.82
" Dose fractionation studies showed that AUC/MIC was the pharmacodynamic index linked with efficacy, indicating that once-daily dosing in humans is feasible."( In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model.
Drusano, GL; Kulawy, R; Liu, W; Louie, A, 2011
)
0.37
" difficile epidemic strains (ribotypes 027 and 106) and linezolid was dosed to achieve human gut concentrations."( Evaluation of linezolid for the treatment of Clostridium difficile infection caused by epidemic strains using an in vitro human gut model.
Baines, SD; Freeman, J; Hobbs, JK; Huscroft, GS; Lovering, AM; Noel, AR; O'Connor, R; Todhunter, SL; Wilcox, MH, 2011
)
0.98
" difficile PCR ribotype 106 viable counts declined at a faster rate than those of PCR ribotype 027 following dosing with linezolid, but cytotoxin titres declined at a similar rate to an untreated control."( Evaluation of linezolid for the treatment of Clostridium difficile infection caused by epidemic strains using an in vitro human gut model.
Baines, SD; Freeman, J; Hobbs, JK; Huscroft, GS; Lovering, AM; Noel, AR; O'Connor, R; Todhunter, SL; Wilcox, MH, 2011
)
0.94
" Monte Carlo simulation was performed to assess the activities of the linezolid dosing regimens against 42 contemporary MRSA isolates recovered from CF patients."( Pharmacokinetics of intravenous and oral linezolid in adults with cystic fibrosis.
Keel, RA; Kloft, C; Knauft, RF; Kuti, JL; Muhlebach, M; Nicolau, DP; Pope, JS; Schaeftlein, A, 2011
)
0.87
" Appropriate linezolid dosage and hospital infection control measures are essential to avoid the spread of linezolid resistance."( Clinical experience with linezolid in infants and children.
Garazzino, S; Tovo, PA, 2011
)
1.04
" Hourly plasma and dialysate samples were obtained over a 12-h dosing interval following 3 to 4 doses of linezolid (600 mg intravenously every 12 h)."( Determination of tissue penetration and pharmacokinetics of linezolid in patients with diabetic foot infections using in vivo microdialysis.
Kuti, JL; Nicolau, DP; Shepard, A; Wiskirchen, DE, 2011
)
0.83
"5, 1 (end of infusion), 2, 4, 8, 12, and 24 h after intravenous dosing of linezolid 600 and 1,200 mg."( Lack of an effect of standard and supratherapeutic doses of linezolid on QTc interval prolongation.
Alvey, C; Choo, HW; Cuozzo, C; Damle, B; Kirby, D; Labadie, RR; Riley, S, 2011
)
0.84
" In summary, these findings point to highly variable PK/PD properties of linezolid in severely ill patients, providing the rationale for targeting linezolid dosage to each individual patient's specific properties."( Clinical pharmacokinetic/pharmacodynamic profile of linezolid in severely ill intensive care unit patients.
Dong, H; Dong, Y; Lei, J; Li, H; Sun, J; Wang, M; Wang, X; Xing, J; You, H; Zhu, H, 2011
)
0.85
" Three dosing regimens were simulated with each drug alone: linezolid (AUC(24)/MIC 30, 60 and 200 h-L30, L60 and L200, respectively) and doxycycline (AUC(24)/MIC 90, 180 and 520 h - D90, D180 and D520, respectively) and in combination: linezolid plus doxycycline (L30+D90; L60+D180 and L200+D520)."( The antistaphylococcal pharmacodynamics of linezolid alone and in combination with doxycycline in an in vitro dynamic model.
Dovzhenko, SA; Firsov, AA; Kobrin, MB; Portnoy, YA; Smirnova, MV; Strukova, EN; Zinner, SH, 2011
)
0.87
"We evaluated the possible association between trough linezolid (LZD) concentrations and platelet counts using a dose-response curve with a logit model equation."( Correlation between serum linezolid concentration and the development of thrombocytopenia.
Hiraike, M; Hiraki, Y; Kamimura, H; Karube, Y; Matsumoto, K; Misumi, N; Morita, K; Tsuji, Y, 2012
)
0.93
" An early and adequate antibiotic treatment at correct dosage is extremely important."( [Antibiotic dose adjustment in the treatment of MRSA infections in patients with acute renal failure undergoing continuous renal replacement therapies].
Carcelero, E; Soy, D, 2012
)
0.38
" Early initiated continuous monitoring of hematological values and linezolid dosage adjustment for body weight are recommended."( Immediate hematological toxicity of linezolid in healthy volunteers with different body weight: a phase I clinical trial.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Guo, D; Liang, B; Liu, Y; Vouloumanou, EK; Wang, R, 2012
)
0.89
"My general pharmacokinetic scaling theory is discussed for the important matter of determining pediatric dosing for existing and new therapeutic drugs when optimal, or near-optimal, dosing for adults is known."( Scaling adult doses of antifungal and antibacterial agents to children.
Dawson, TH, 2012
)
0.38
" No significant differences were detected in the subgroup efficacy analysis (daily linezolid dosage ≤ 600 mg versus >600 mg)."( Efficacy, safety and tolerability of linezolid containing regimens in treating MDR-TB and XDR-TB: systematic review and meta-analysis.
Alffenaar, JW; Anger, HA; Caminero, JA; Castiglia, P; Centis, R; D'Ambrosio, L; De Lorenzo, S; Ferrara, G; Koh, WJ; Migliori, GB; Schecter, GF; Shim, TS; Singla, R; Skrahina, A; Sotgiu, G; Spanevello, A; Udwadia, ZF; Villar, M; Zampogna, E; Zellweger, JP; Zumla, A, 2012
)
0.88
" Dosage adjustments were performed when C(min) ≥10 mg/L and/or AUC₂₄ ≥400 mg/L · h."( Therapeutic drug monitoring may improve safety outcomes of long-term treatment with linezolid in adult patients.
Cojutti, P; Del Pin, B; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2012
)
0.6
" Dosage adjustments were needed in 40% versus 0% of patients in the linezolid group (n = 35) versus the linezolid + rifampicin group (n = 10), respectively."( Therapeutic drug monitoring may improve safety outcomes of long-term treatment with linezolid in adult patients.
Cojutti, P; Del Pin, B; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2012
)
0.84
" Thus, more aggressive vancomycin dosing has the potential to improve efficacy."( Treatment of methicillin-resistant Staphylococcus aureus ventilator-associated pneumonia with high-dose vancomycin or linezolid.
Boucher, BA; Christopher Wood, G; Croce, MA; Fabian, TC; Hamilton, LA; Magnotti, LJ; Martin, JB; Swanson, JM, 2012
)
0.59
" In a recent prospective, randomized, open-label, comparator-controlled, multicenter, phase 4 clinical trial in adults with complicated skin and soft tissue infections (cSSTIs) caused by methicillin-resistant Staphylococcus aureus (MRSA), linezolid achieved clinical and microbiologic success comparable to appropriately dosed intravenous vancomycin."( Clinical efficacy of oral linezolid compared with intravenous vancomycin for the treatment of methicillin-resistant Staphylococcus aureus-complicated skin and soft tissue infections: a retrospective, propensity score-matched, case-control analysis.
Baruch, AM; Bhattacharyya, H; Biswas, P; Itani, KM; Reisman, A, 2012
)
0.86
" The aggressive vancomycin dosing regimens are still associated with unacceptable high microbiological failure rates and it is not currently possible to achieve probability of target attainment at higher vancomycin MICs of 2 mg/l."( Does resistance in severe infections caused by methicillin-resistant Staphylococcus aureus give you the 'creeps'?
Brink, AJ, 2012
)
0.38
"Continued monitoring of patients on aggressive vancomycin dosing schedules is advised."( Does resistance in severe infections caused by methicillin-resistant Staphylococcus aureus give you the 'creeps'?
Brink, AJ, 2012
)
0.38
"The optimal dosage of linezolid to avoid hematologic toxicity is unknown."( A reduced linezolid dosage maintains favorable efficacy with minimal hematologic toxicity in a methicillin-resistant Staphylococcus aureus-infected patient with renal insufficiency.
Anraku, Y; Horio, M; Kawaguchi, T; Miyakawa, T; Mizuta, H; Ohmura, T; Okada, T; Saito, H; Taguchi, K, 2013
)
1.11
" Linezolid remains costly, and a reduced dosage and duration may result in fewer adverse events and lower cost."( Linezolid-containing regimens for the treatment of drug-resistant tuberculosis in South African children.
Hallbauer, UM; Hesseling, AC; Rose, PC; Schaaf, HS; Seddon, JA, 2012
)
2.73
" The areas under the curve for the 12-h dosing interval (AUCτ) were similar between moderately obese and morbidly obese groups: 130."( Pharmacokinetics of intravenous linezolid in moderately to morbidly obese adults.
Bhalodi, AA; Kuti, JL; Nicolau, DP; Papasavas, PK; Tishler, DS, 2013
)
0.67
" Dose-response data were analyzed by a maximum effect (E(max)) model using nonlinear regression."( Inoculum effects of ceftobiprole, daptomycin, linezolid, and vancomycin with Staphylococcus aureus and Streptococcus pneumoniae at inocula of 10(5) and 10(7) CFU injected into opposite thighs of neutropenic mice.
Andes, DR; Craig, WA; Lee, DG; Murakami, Y, 2013
)
0.65
"Our findings suggest that a weight-adjusted, 10 mg/kg regimen of linezolid may be more appropriate than fixed dosing for patients of different body weight."( Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Karageorgopoulos, DE; Liang, B; Wang, R, 2013
)
0.9
" In a suspected case, the doctor was recommended to discontinue, decrease the dosage or keep the drug under observation; and a follow-up of the patient's platelet count was made in order to classify the relationship between the drug and thrombocytopenia."( [Incidence of drug-induced thrombocytopenia in hospitalized patients].
Álvarez-Arroyo, L; Delgado-Sánchez, O; Seco-Melantuche, R,
)
0.13
" The doctor was recommended to discontinue the drug (2), decrease the dosage (3) or keep it under observation (3), with 100% acceptance."( [Incidence of drug-induced thrombocytopenia in hospitalized patients].
Álvarez-Arroyo, L; Delgado-Sánchez, O; Seco-Melantuche, R,
)
0.13
" Further studies are required to evaluate whether therapeutic drug monitoring-guided dosage adjustment of linezolid decreases the adverse effects while maintaining treatment efficacy in patients with renal dysfunction."( High plasma linezolid concentration and impaired renal function affect development of linezolid-induced thrombocytopenia.
Hatakeyama, S; Hisaka, A; Moriya, K; Nukui, Y; Okamoto, K; Suzuki, H; Yamamoto, T; Yata, N; Yotsuyanagi, H, 2013
)
0.98
"We evaluated treatment with linezolid, dosed at 800 mg once daily for 1 to 4 months as guided by sputum culture status and tolerance and then at 1,200 mg thrice weekly until ≥ 1 year after culture conversion, in addition to individually optimized regimens among 10 consecutive patients with extensively drug-resistant tuberculosis or fluoroquinolone-resistant multidrug-resistant tuberculosis."( Can intermittent dosing optimize prolonged linezolid treatment of difficult multidrug-resistant tuberculosis?
Chan, RC; Chang, KC; Chau, CH; Cheung, SW; Leung, CC; Tam, CM; Wen, PK; Yew, WW, 2013
)
0.95
" Linezolid was given intravenously (IV) at a dosage of 600 mg q12h and vancomycin IV at 500 mg q6h."( Vancomycin versus linezolid in the treatment of methicillin-resistant Staphylococcus aureus meningitis.
Arda, B; Aydemir, S; Bardak-Ozcem, S; Dalbasti, T; Pullukcu, H; Ruksen, M; Sipahi, H; Sipahi, OR; Turhan, T; Ulusoy, S; Yurtseven, T; Zileli, M, 2013
)
1.63
"Limited data on linezolid dosing in the morbidly obese population show lower serum drug concentrations than those in nonobese patients, but no clinical failure has been reported when treating MRSA skin and soft tissue infections or MRSA tracheitis."( Subtherapeutic linezolid concentrations in a patient with morbid obesity and methicillin-resistant Staphylococcus aureus pneumonia: case report and review of the literature.
Lee, KB; Muzevich, KM, 2013
)
1.09
"The oral liquid formulations poses an alternative way in providing medications to pediatric patients, geriatric patients, patients with feeding tubes, and patients who cannot swallow solid dosage forms."( Pharmacokinetics and relative bioavailability evaluation of linezolid suspension and tablet formulations.
Helmy, SA, 2013
)
0.63
" In vivo dose-response studies demonstrated that oral linezolid administration sufficiently decreased bronchoalveolar lavage fluid levels of IFN-γ at day 7 postinfluenza infection in a dose-dependent manner."( Linezolid decreases susceptibility to secondary bacterial pneumonia postinfluenza infection in mice through its effects on IFN-γ.
Birket, SE; Breslow-Deckman, JM; Feola, DJ; Garvy, BA; Ho, TN; Hoskins, SN; Mattingly, CM, 2013
)
2.08
" Because there are physiologic, pharmacologic, and dosing differences related to weight, it is important to evaluate the impact of weight on antimicrobial agents to optimize clinical outcomes."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
"We analyzed data from 2 clinical trials of patients randomized to receive a fixed dose of linezolid or weight-based dosing of vancomycin for the treatment of cSSSIs or NP caused by MRSA."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.61
" Among patients with cSSSIs, clinical success rates at the study end with fixed-dose linezolid were similar across all weight quartiles and similar to weight-based dosing of vancomycin for Q1-3."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.61
"Except for Q4 within the vancomycin-treated patients for MRSA cSSSI, the efficacy of fixed-dosed linezolid and weight-based dosing of vancomycin was maintained across all weight quartiles and MRSA infection types."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.61
" In such cases, we suggest optimized adjustment of the linezolid dosage regimen."( Developments in the pharmacokinetic/pharmacodynamic index of linezolid: a step toward dose optimization using Monte Carlo simulation in critically ill patients.
Chen, L; Dong, H; Dong, Y; Sun, J; Wang, T; Xie, J; Zhao, Y, 2014
)
0.89
" These results suggested that therapeutic drug monitoring and dosage individualization of linezolid in patients with severe burns were necessary."( Comparison of the pharmacokinetics of linezolid in burn and non-burn rabbits.
Chu, WL; Feng, YQ; Gao, L; Li, X; Ma, JL; Wang, XQ; Zhang, QZ, 2015
)
0.91
" This study was aimed to evaluate whether standard dosing of linezolid leads to therapeutic serum concentrations in critically ill patients."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
1
"In this prospective observational study, 30 critically ill adult patients with suspected infections received standard dosing of 600 mg linezolid intravenously twice a day."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
0.96
" The findings suggest that therapeutic drug monitoring of linezolid might be helpful for adequate dosing of linezolid in critically ill patients."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
1
" Breast milk samples were obtained over a 12-hour dosing interval on day 1 (after a single dose of therapy) and again on day 14 (at steady state)."( Transfer of linezolid into breast milk.
Cooper, SD; Felkins, K; Hale, TW; Rowe, HE, 2014
)
0.78
" This recommended initial dosage and subsequent dosage adjustment for the target concentration range should avoid adverse events, thereby enabling effective linezolid-based therapies to be continued."( Analysis of thrombocytopenic effects and population pharmacokinetics of linezolid: a dosage strategy according to the trough concentration target and renal function in adult patients.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2014
)
0.83
"To report on linezolid exposure in a paediatric population who routinely underwent therapeutic drug monitoring (TDM) for dosage optimization and to assess the factors affecting interpatient variability."( Pharmacokinetic/pharmacodynamic evaluation of linezolid in hospitalized paediatric patients: a step toward dose optimization by means of therapeutic drug monitoring and Monte Carlo simulation.
Cojutti, P; Crichiutti, G; Isola, M; Maximova, N; Pea, F, 2015
)
1.04
" Simulations showed a PTA of ≥ 90% with the current dosing regimens in both groups only for pathogens with an MIC ≤ 1 mg/L."( Pharmacokinetic/pharmacodynamic evaluation of linezolid in hospitalized paediatric patients: a step toward dose optimization by means of therapeutic drug monitoring and Monte Carlo simulation.
Cojutti, P; Crichiutti, G; Isola, M; Maximova, N; Pea, F, 2015
)
0.68
" TDM is a diagnostic standard for the individualization of polypharmcotherapy based on validated analytical methods (in particular LC-MS/MS and HPLC-methods) in order to optimize dosing and drug safety."( [Therapeutic Drug Monitoring of antiinfectives in intensive care medicine].
Adam, R; Michels, G; Müller, C; Nosseir, NS; Pfister, R; Wiesen, MH, 2014
)
0.4
" Administration of higher than standard doses of linezolid and therapeutic drug monitoring should therefore be considered as options to optimise linezolid dosing in critically ill patients with CNS infections."( Plasma and cerebrospinal fluid concentrations of linezolid in neurosurgical critically ill patients with proven or suspected central nervous system infections.
Alvarez-Lerma, F; Basas, M; Campillo, N; Ferrández, O; Grau, S; Horcajada, JP; Lipman, J; Luque, S; Roberts, JA, 2014
)
0.91
"The minimum inhibitory concentrations (MICs) of vancomycin and norvancomycin for half of the isolates decreased below the susceptibility break point, and the MIC of linezolid for one isolate was decreased to the blood and epithelial lining fluid concentration using the current dosing regimen."( Colistin and anti-Gram-positive bacterial agents against Acinetobacter baumannii.
Bai, Y; Di, X; Liu, B; Liu, Y; Wang, J; Wang, R; Zhang, X, 2014
)
0.6
" Most adverse events resolved after reducing the dosage of linezolid or temporarily discontinuing linezolid."( Efficacy, safety and tolerability of linezolid for the treatment of XDR-TB: a study in China.
Gu, J; Hao, X; Lin, F; Liu, G; Liu, X; Liu, Y; Sun, H; Tang, S; Wang, X; Wu, M; Yao, L; Zen, L; Zhang, X; Zhang, Z, 2015
)
0.93
" A high drug exposure NOEL on oral dosing in the rat suggested that a high therapeutic margin could be achieved."( Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
Basarab, GS; Brassil, P; Doig, P; Galullo, V; Gowravaram, M; Haimes, HB; Kern, G; Kutschke, A; McNulty, J; Schuck, VJ; Stone, G, 2014
)
0.4
" The present study aimed to define the pharmacokinetic parameters of intravenous linezolid in pediatric patients and assess the rationale for the approved dosage recommendations."( Linezolid dosage in pediatric patients based on pharmacokinetics and pharmacodynamics.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2015
)
2.09
" The main objective of this review is to compare the relative efficacies, dosing strategies, and side-effect profiles of quinupristin-dalfopristin, linezolid, and daptomycin for VRE bacteremia in the pediatric population."( Optimizing therapy for vancomycin-resistant enterococcal bacteremia in children.
Hsu, AJ; Tamma, PD, 2014
)
0.6
" aureus RMs (resistant to 2× and 4×MIC but not 8× and 16×MIC) were enriched at ratios of the 24-h area under the concentration-time curve (AUC24) to the MIC that provide linezolid concentrations between the MIC and MPC for 100% (AUC24/MIC, 60 h) and 86% (AUC24/MIC, 120 h) of the dosing interval."( In vitro resistance studies with bacteria that exhibit low mutation frequencies: prediction of "antimutant" linezolid concentrations using a mixed inoculum containing both susceptible and resistant Staphylococcus aureus.
Edelstein, MV; Firsov, AA; Golikova, MV; Portnoy, YA; Romanov, AV; Strukova, EN; Zinner, SH, 2015
)
0.82
" The result from the present investigation indicates that STELLA® when coupled with biorelevant dissolution media can predict the in vivo performance of the drug product with prediction error less than 20% irrespective of the dosage form (immediate release versus modified release) and BCS Classification."( Prediction of in vivo drug performance using in vitro dissolution coupled with STELLA: a study with selected drug products.
Aggarwal, D; Chakraborty, S; Yadav, L, 2015
)
0.42
"We conclude that anti-MRSA antibiotics are utilized via various dosage regimens by a majority of CF Foundation accredited care programs for the treatment of chronic MRSA in PEx, and there is no consensus on the best treatment approach."( Utilization of antibiotics for methicillin-resistant Staphylococcus aureus infection in cystic fibrosis.
Ampofo, K; Chin, MJ; Dasenbrook, E; Epps, KL; Marshall, BC; Montague, M; Olson, J; Young, DC; Zobell, JT, 2015
)
0.42
"Standard doses of linezolid and meropenem will provide inhibitory concentrations and thus pharmacodynamic antagonism throughout the whole dosing interval for MSSA."( Pharmacodynamic and response surface analysis of linezolid or vancomycin combined with meropenem against Staphylococcus aureus.
Kees, MG; Kloft, C; Kuss, J; Wicha, SG, 2015
)
1.01
" Therapeutic drug monitoring dosage adjustments may be especially useful in patients with renal dysfunction and severe MRSA infection."( Treatment of mediastinitis due to methicillin-resistant Staphylococcus aureus in a renal dysfunction patient undergoing adjustments to the linezolid dose.
Ashizawa, N; Fukahara, K; Nagura, S; Narukawa, M; Obi, H; Ota, Y; Tashiro, M; To, H; Tsuji, Y; Yamamoto, Y; Yoshimura, N, 2015
)
0.62
" A higher dosage of the drug showed a higher accumulation in these bacteria in a dosing range of 5-50 ng/mL."( Thinking outside the "bug": a unique assay to measure intracellular drug penetration in gram-negative bacteria.
Isabella, V; Joubran, C; Miller, A; Miller-Vedam, L; Nayar, A; Tentarelli, S; Zhou, Y, 2015
)
0.42
" Linezolid, at a dosage of 1200 or 600 mg daily, was included to complete the treatment if no other sensitive drugs were available."( Retrospective study of tolerability and efficacy of linezolid in patients with multidrug-resistant tuberculosis (1998-2014).
Carrillo Gómez, R; González-Ruano Pérez, P; Martínez-Prieto, M; Noguerado Asensio, A; Pascual Pareja, JF; Ramírez-Lapausa, M, 2016
)
1.6
" In both cases the dosage was reduced to 600 mg per day, with improvement of the anemia and paresthesias."( Retrospective study of tolerability and efficacy of linezolid in patients with multidrug-resistant tuberculosis (1998-2014).
Carrillo Gómez, R; González-Ruano Pérez, P; Martínez-Prieto, M; Noguerado Asensio, A; Pascual Pareja, JF; Ramírez-Lapausa, M, 2016
)
0.68
"A daily dosage of 600 mg of linezolid was well tolerated without stopping treatment in any case."( Retrospective study of tolerability and efficacy of linezolid in patients with multidrug-resistant tuberculosis (1998-2014).
Carrillo Gómez, R; González-Ruano Pérez, P; Martínez-Prieto, M; Noguerado Asensio, A; Pascual Pareja, JF; Ramírez-Lapausa, M, 2016
)
0.98
"Thirty-five patients with ACLF who had been subjected to intravenous administration of 600 mg linezolid every 12 hours for more than 7 days were categorized as a ACLF treatment (ACLF-T) group, 72 patients without ACLF treated with the same dosage of linezolid were recruited as a non-ACLF treatment (NACLF-T) group, and 70 patients with ACLF without linezolid treatment served as an ACLF control (ACLF-C) group."( High frequency of thrombocytopenia in patients with acute-on-chronic liver failure treated with linezolid.
Li, JZ; Li, LJ; Lu, YF; Xie, ZY; Xu, LC; Yu, W; Zhang, YM; Zhou, N, 2015
)
0.85
"Tedizolid phosphate is the second commercially available oxazolidinone antibiotic, although the first one in class that is dosed once daily."( Tedizolid: The First Once-Daily Oxazolidinone Class Antibiotic.
Burdette, SD; Trotman, R, 2015
)
0.42
" Overall, linezolid dosage was mainly reduced (56."( A 1 year retrospective audit of quality indicators of clinical pharmacological advice for personalized linezolid dosing: one stone for two birds?
Baraldo, M; Cojutti, P; Dose, L; Pea, F, 2016
)
1.05
" The microplate bioassay was optimized regarding the responses of low, medium, and high doses of linezolid, negative and positive controls, and the slope, intercept, and correlation coefficient of dose-response curves."( Development, Optimization, and Validation of a Microplate Bioassay for Relative Potency Determination of Linezolid Using a Design Space Concept, and its Measurement Uncertainty.
Francisco, FL; Lourenço, FR; Ostronoff, CS; Saviano, AM,
)
0.56
"Few data are available to guide linezolid dosing during renal replacement therapy."( Population pharmacokinetics of linezolid in critically ill patients on renal replacement therapy: comparison of equal doses in continuous venovenous haemofiltration and continuous venovenous haemodiafiltration.
Lefrant, JY; Lipman, J; Louart, B; Muller, L; Roberts, JA; Roger, C; Saissi, G; Wallis, SC, 2016
)
1
" Seven blood samples were collected over one dosing interval and analysed by a validated chromatographic method."( Population pharmacokinetics of linezolid in critically ill patients on renal replacement therapy: comparison of equal doses in continuous venovenous haemofiltration and continuous venovenous haemodiafiltration.
Lefrant, JY; Lipman, J; Louart, B; Muller, L; Roberts, JA; Roger, C; Saissi, G; Wallis, SC, 2016
)
0.72
" Although linezolid therapy is known to result in thrombocytopenia, dosage adjustment or therapeutic drug monitoring of linezolid is not generally necessary."( Successful treatment of methicillin-resistant Staphylococcus aureus osteomyelitis with combination therapy using linezolid and rifampicin under therapeutic drug monitoring.
Ashizawa, N; Gejo, R; Higashi, Y; Kawago, K; Kimura, T; Narukawa, M; Nogami, M; Tashiro, M; Tsuji, Y; Yamamoto, Y, 2016
)
1.05
" The role of individualized drug dosing regimens for other oxazolidinones remains to be proven."( Drug monitoring and individual dose optimization of antimicrobial drugs: oxazolidinones.
Alffenaar, JW; Cattaneo, D; Neely, M, 2016
)
0.43
" The changes summarized are clinically relevant and may serve as rationale for dosing recommendations in this particular population."( Pharmacokinetics of linezolid in critically ill patients.
Dimitrijevic, A; Jankovic, SM; Kostic, M; Sazdanovic, P; Stefanovic, S, 2016
)
0.76
" Acute renal or liver failure decrease clearance of linezolid, but renal replacement therapy is capable of restoring clearance back to normal, obviating the need for dosage adjustment."( Pharmacokinetics of linezolid in critically ill patients.
Dimitrijevic, A; Jankovic, SM; Kostic, M; Sazdanovic, P; Stefanovic, S, 2016
)
1.01
" Fifty-two critically ill patients with severe infections receiving standard dosing of linezolid participated in this prospective observational study."( Predictors of Inadequate Linezolid Concentrations after Standard Dosing in Critically Ill Patients.
Frechen, S; Frey, L; Fuhr, U; Holdt, LM; Maier, B; Scharf, C; Taubert, M; Vogeser, M; Zander, J; Zoller, M, 2016
)
0.96
" Several strategies are available for adjusting the dosage regimen of LZD, but therapeutic drug monitoring is highly recommended when it is used."( Kinetics of Linezolid in Continuous Renal Replacement Therapy: An In Vitro Study.
De Rosa, S; Ferrari, F; Loregian, A; Pagni, S; Palú, G; Ronco, C; Sartori, M; Zampieri, L; Zancato, M, 2016
)
0.81
" Omadacycline offers once daily oral and IV dosing and a clinical tolerability and safety profile that compares favorably with contemporary antibiotics used across serious community-acquired infections where resistance has rendered many less effective."( Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic.
Steenbergen, J; Tanaka, SK; Villano, S, 2016
)
0.43
"Several studies have demonstrated that the ideal therapeutic effect of linezolid cannot be achieved in critically ill patients with the recommended standard dosing regimen of 600 mg every 12 h (q12h)."( Pharmacokinetic/pharmacodynamic evaluation of linezolid for the treatment of staphylococcal infections in critically ill patients.
Chen, L; Dong, H; Dong, Y; Sun, J; Wang, T; Wang, X; Xie, J; Zeng, X, 2016
)
0.93
" The comfortable oral dosage and tolerance of linezolid opens the possibility for sequential antimicrobial treatment (SAT) in stable patients after a period of intravenous treatment."( Sequential antimicrobial treatment with linezolid for neurosurgical infections: efficacy, safety and cost study.
Castillo-Ojeda, E; Gil-Navarro, MV; Gómez-Gómez, MJ; Jiménez-Mejías, ME; Márquez-Rivas, FJ; Martín-Gandul, C; Mayorga-Buiza, MJ; Rivero-Garvía, M, 2016
)
0.96
" However, linezolid has a narrow therapeutic window, and the optimal dosing strategy that minimizes the substantial toxicity associated with linezolid's prolonged use in tuberculosis treatment has not been determined, limiting the potential impact of this anti-mycobacterial agent."( Linezolid in the treatment of drug-resistant tuberculosis: the challenge of its narrow therapeutic index.
Maartens, G; Meintjes, G; Wasserman, S, 2016
)
2.28
" Expert commentary: Prospective pharmacokinetic-pharmacodynamic studies are required to define optimal therapeutic targets and to inform improved linezolid dosing strategies for drug-resistant tuberculosis."( Linezolid in the treatment of drug-resistant tuberculosis: the challenge of its narrow therapeutic index.
Maartens, G; Meintjes, G; Wasserman, S, 2016
)
2.08
"12h is still the clinically recommended empirical dosage for Gram-positive bacterial infections."( Optimization of linezolid treatment regimens for Gram-positive bacterial infections based on pharmacokinetic/pharmacodynamic analysis.
Chen, Y; Guo, Y; Liang, X; Yang, M; Yu, J; Zhang, J; Zhang, Y; Zhu, D, 2017
)
0.8
" There were no serious side effects observed with the use of linezolid in reduced dosage of 600 mg×1/day for a duration of 9 months."( Mycobacterium chelonae hand infection after steroid injection in a patient with rheumatoid arthritis receiving long-term linezolid therapy.
Olesen, JS; Wang, M; Wejse, C, 2017
)
0.9
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" Because LZD toxicity is dose- and duration-dependent, and is driven by elevated trough concentrations and prolonged exposure to concentrations inhibiting mitochondrial protein synthesis, several innovative dosing strategies can be employed to optimize its usage."( Evolving strategies for dose optimization of linezolid for treatment of tuberculosis.
Nuermberger, E, 2016
)
0.69
" Although strategies to overcome these insufficient levels have been discussed, appropriate alternative dosing regimens remain to be identified."( Optimization of linezolid therapy in the critically ill: the effect of adjusted infusion regimens.
Frechen, S; Frey, L; Fuhr, U; Scharf, C; Taubert, M; Vogeser, M; Zander, J; Zoller, M, 2017
)
0.8
"A pronounced enrichment of mutants resistant to 2×, 4× and 8× MIC was observed at AUC24/MIC ratios of 30 and 60 when linezolid concentrations were within the MSW for more than half of the dosing interval for each strain."( Testing the mutant selection window hypothesis with Staphylococcus aureus exposed to linezolid in an in vitro dynamic model.
Alieva, KN; Dovzhenko, SA; Edelstein, MV; Firsov, AA; Golikova, MV; Kobrin, MB; Portnoy, YA; Romanov, AV; Strukova, EN; Zinner, SH, 2017
)
0.89
"The purpose of this study was to identify the optimum dosing regimen of linezolid in sepsis patients with and without renal dysfunction and sepsis patients on low-dose continuous renal replacement therapy (CRRT) using a pharmacokinetics/pharmacokinetics (PK/PD) approach."( Population pharmacokinetics/pharmacodynamics of linezolid in sepsis patients with and without continuous renal replacement therapy.
Ide, T; Ikawa, K; Morikawa, N; Nakajima, K; Nishi, S; Takahashi, Y; Takeda, K; Takesue, Y; Ueda, T, 2018
)
0.97
" Dosing regimens were evaluated using cumulative fraction of response (CFR) and safety probability (trough level < 7 µg/mL) by Monte Carlo simulation."( Population pharmacokinetics/pharmacodynamics of linezolid in sepsis patients with and without continuous renal replacement therapy.
Ide, T; Ikawa, K; Morikawa, N; Nakajima, K; Nishi, S; Takahashi, Y; Takeda, K; Takesue, Y; Ueda, T, 2018
)
0.74
"We identified different dosage strategies to achieve target linezolid concentrations according to renal function and use of CRRT in sepsis patients."( Population pharmacokinetics/pharmacodynamics of linezolid in sepsis patients with and without continuous renal replacement therapy.
Ide, T; Ikawa, K; Morikawa, N; Nakajima, K; Nishi, S; Takahashi, Y; Takeda, K; Takesue, Y; Ueda, T, 2018
)
0.98
"Linezolid dosing at 300 mg q12h may retain the efficacy of the 600 mg q12h licensed dosing with improved safety."( Linezolid pharmacokinetics in MDR-TB: a systematic review, meta-analysis and Monte Carlo simulation.
Alffenaar, JC; Bolhuis, M; Bonnett, L; Caws, M; Dartois, V; Davies, G; Hodel, EM; Johnson, JL; Millard, J; Pertinez, H; Sloan, DJ; Tiberi, S, 2018
)
3.37
" Optimal dosing was determined based on achievement of the surrogate pharmacodynamics target for efficacy: a ratio of the area under the concentration-time curve to minimum inhibitory concentration >80."( Population Pharmacokinetics of Intravenous Linezolid in Premature Infants.
Autmizguine, J; Goyer, I; Kassir, N; Litalien, C; Moussa, A; Ovetchkine, P; Théorêt, Y; Thibault, C, 2019
)
0.78
" Within this subset, the duration of linezolid dosage to first symptoms is 235 ± 71 days."( Case Report: Linezolid Optic Neuropathy and Proposed Evidenced-based Screening Recommendation.
Dempsey, SP; Sickman, A; Slagle, WS, 2018
)
1.12
" Further studies are needed to determine the optimum dosage and the optimal duration of linezolid treatment in children."( Linezolid-containing Treatment Regimens for Tuberculosis in Children.
Baquero-Artigao, F; Blázquez-Gamero, D; Carazo, B; Del Rosal, T; Jiménez, AB; Mellado, MJ; Moreno-Pérez, D; Pérez-Gorricho, B; Prieto, LM; Rubio, F; Santiago, B; Tagarro, A, 2019
)
2.18
" The Emax Hill equation was used to model the dose-response relationship."( Increased activity of linezolid in combination with rifampicin in a murine pneumonia model due to MRSA.
Bu, MX; Li, L; Liao, XP; Liu, YH; Sun, J; Tao, MT; Xiong, YQ; Zhou, YF, 2018
)
0.8
"For patients with infection of the central nervous system and who are sensitive to the drug, the usual dosing regimens of linezolid can achieve a good therapeutic effect."( Pharmacokinetics and pharmacodynamics of linezolid in plasma/cerebrospinal fluid in patients with cerebral hemorrhage after lateral ventricular drainage by Monte Carlo simulation.
Kong, L; Tang, Y; Wu, C; Wu, X; Zhang, X, 2018
)
0.95
" Through Monte Carlo simulations the quantitative output of this in vitro study was bridged to the human patient population to inform optimal dosage regimens while accounting for clinical minimum inhibitory concentration (MIC) distributions."( Dose optimization of moxifloxacin and linezolid against tuberculosis using mathematical modeling and simulation.
Brown, DL; Derendorf, H; Drusano, GL; Heinrichs, MT; Louie, A; Maynard, MS; Peloquin, CA; Rand, KH; Sy, SKB, 2019
)
0.78
" A tedizolid dose of 200 mg/day or 700 mg twice a week is recommended for testing in patients; the intermittent tedizolid dosing schedule could be much safer than daily linezolid."( The Sterilizing Effect of Intermittent Tedizolid for Pulmonary Tuberculosis.
Cirrincione, K; Deshpande, D; Dheda, K; Gumbo, T; Lee, PS; Nuermberger, E; Srivastava, S, 2018
)
0.68
" Here, our aim was to search relevant pharmacokinetics (PK)/pharmacodynamics (PD) literature to identify the effective PK/PD index and to define the optimal daily dose and dosing frequency of linezolid in MDR-TB regimens."( Linezolid-based Regimens for Multidrug-resistant Tuberculosis (TB): A Systematic Review to Establish or Revise the Current Recommended Dose for TB Treatment.
Akkerman, OW; Alffenaar, JC; Bolhuis, MS; Ghimire, S; Gumbo, T; Srivastava, S; Sturkenboom, MGG, 2018
)
2.11
" However, specific dosing recommendations for this population are still lacking."( Pharmacokinetic evaluation of linezolid administered intravenously in obese patients with pneumonia.
Blot, S; Boussery, K; Colin, P; Degroote, S; Koulenti, D; Koulouras, V; Malliotakis, P; Mantzarlis, K; Van Bocxlaer, J; Xie, F, 2019
)
0.8
" Monte Carlo simulations were carried out to investigate the PTA and time to target attainment for linezolid dosing against MRSA."( Pharmacokinetic evaluation of linezolid administered intravenously in obese patients with pneumonia.
Blot, S; Boussery, K; Colin, P; Degroote, S; Koulenti, D; Koulouras, V; Malliotakis, P; Mantzarlis, K; Van Bocxlaer, J; Xie, F, 2019
)
1.02
" Standard linezolid dosing in obese pneumonia patients with MRSA (MICs of 1-4 mg/L) leads to unacceptably low (near zero to 60%) PTA for patients <65 years old."( Pharmacokinetic evaluation of linezolid administered intravenously in obese patients with pneumonia.
Blot, S; Boussery, K; Colin, P; Degroote, S; Koulenti, D; Koulouras, V; Malliotakis, P; Mantzarlis, K; Van Bocxlaer, J; Xie, F, 2019
)
1.2
"Standard linezolid dosing is likely to provide insufficient target attainment against MRSA in obese patients."( Pharmacokinetic evaluation of linezolid administered intravenously in obese patients with pneumonia.
Blot, S; Boussery, K; Colin, P; Degroote, S; Koulenti, D; Koulouras, V; Malliotakis, P; Mantzarlis, K; Van Bocxlaer, J; Xie, F, 2019
)
1.22
" The aim of this study was to develop a population pharmacokinetic model for linezolid in children and optimize the dosing strategy in order to improve therapeutic efficacy."( Population Pharmacokinetics and Dosing Optimization of Linezolid in Pediatric Patients.
Li, SC; Wang, Y; Xu, H; Ye, Q; Zhang, L, 2019
)
0.99
"Antibiotic therapy is a crucial aspect of the management of hospitalized patients, however, current standard dosing protocols have been shown to often attain inadequate plasmatic concentrations which may impair the clinical outcome and promote the selection of multidrug-resistant bacteria."( LC-MS/MS method for simultaneous determination of linezolid, meropenem, piperacillin and teicoplanin in human plasma samples.
Banfi, G; Castagna, A; Ferrari, D; Locatelli, M; Premaschi, S; Ripa, M, 2019
)
0.77
" Stochastic PK/pharmacodynamic (PD) simulations were carried out to evaluate current regimen combinations and dosing guidelines in distinct patient strata."( Tuberculosis drugs' distribution and emergence of resistance in patient's lung lesions: A mechanistic model and tool for regimen and dose optimization.
Bang, H; Barry, CE; Dartois, V; Eum, S; Fox, WS; Gupta, SV; Lee, M; Savic, RM; Shim, T; Strydom, N; Via, LE; Zimmerman, M, 2019
)
0.51
" By applying various antibiotic combinations against a single pathogen in multiple chambers, the IMS could identify the optimal drug combination and the minimum effective dosage by evaluating the fractional inhibitory concentration index."( An integrated microfluidic system for antimicrobial susceptibility testing with antibiotic combination.
Chien, CC; Kuo, FC; Lee, GB; Lee, MS; Lee, WB; You, HL, 2019
)
0.51
" Studies of explanted lungs from patients with drug-resistant tuberculosis have shown substantial drug-specific gradients across pulmonary cavities, suggesting that alternative dosing and drug delivery strategies are needed to reduce functional monotherapy at the site of disease."( The Lancet Respiratory Medicine Commission: 2019 update: epidemiology, pathogenesis, transmission, diagnosis, and management of multidrug-resistant and incurable tuberculosis.
Dheda, K; Dooley, KE; Furin, J; Gumbo, T; Maartens, G; Murray, M; Nardell, EA; Warren, RM, 2019
)
0.51
" Therapeutic Drug Monitoring (TDM) is a clinical strategy that assesses the response of an individual patient and helps adjust the dosing regimen to maximize efficacy while minimizing toxicity."( Therapeutic Drug Monitoring Can Improve Linezolid Dosing Regimens in Current Clinical Practice: A Review of Linezolid Pharmacokinetics and Pharmacodynamics.
Alffenaar, JW; Cattaneo, D; Konicki, R; Marriott, DJE; Neely, M; Rao, GG, 2020
)
0.83
"Linezolid is increasingly used for the treatment of tuberculosis resistant to first-line agents, but the most effective dosing strategy is yet unknown."( Fourteen-Day Bactericidal Activity, Safety, and Pharmacokinetics of Linezolid in Adults with Drug-Sensitive Pulmonary Tuberculosis.
Burger, DA; Dawson, R; De Jager, VR; Diacon, AH; Everitt, D; Mendel, CM; Narunsky, K; Nedelman, J; Pappas, F; Vanker, N, 2020
)
2.24
" A better understanding of exposure-response relationships governing LZD efficacy and toxicity will inform dosing strategies."( Pharmacodynamic Correlates of Linezolid Activity and Toxicity in Murine Models of Tuberculosis.
Barnes-Boyle, K; Bigelow, KM; Deitchman, AN; Dooley, KE; Li, SY; Nuermberger, EL; Savic, RM; Soni, H; Tyagi, S, 2021
)
0.91
" Technical factors included investment in the optimization of dosing for improved drug exposure, toxicological evaluation of the purified eutomer from a diastereomer and the failure to develop an effective research formulation."( Decision making in the pharmaceutical industry - A tale of three antibiotics.
Hunt, A; Kirsch, DR, 2020
)
0.56
" Despite their excellent efficacy, optimal dosing strategies to limit their toxicities are still under development."( Radiosynthesis and Biodistribution of
Freundlich, JS; Jadhav, R; Jain, SK; Klunk, MH; Mota, F; Ordonez, AA; Ruiz-Bedoya, CA, 2020
)
0.56
" The study aimed to identify a target pharmacokinetics/pharmacodynamics (PK/PD) index of the efficacy of linezolid treatment, and to estimate the optimum dosage regimen of linezolid in sepsis patients."( Dosage regimen and toxicity risk assessment of linezolid in sepsis patients.
Chen, L; Dong, H; Dong, Y; Dou, L; Fan, D; Han, X; Meng, D, 2020
)
1.03
" Different dosing regimens were evaluated using Monte Carlo simulation."( Dosage regimen and toxicity risk assessment of linezolid in sepsis patients.
Chen, L; Dong, H; Dong, Y; Dou, L; Fan, D; Han, X; Meng, D, 2020
)
0.82
"This study identified different dosing strategies to achieve target linezolid PK/PD values according to whether sepsis patients were treated with continuous renal replacement therapy."( Dosage regimen and toxicity risk assessment of linezolid in sepsis patients.
Chen, L; Dong, H; Dong, Y; Dou, L; Fan, D; Han, X; Meng, D, 2020
)
1.05
"The aim was to characterize linezolid population pharmacokinetics in plasma and interstitial space fluid of subcutaneous adipose tissue (target site) of obese compared with non-obese patients and to determine dosing regimens enabling adequate therapy using Monte Carlo simulations."( Risk of target non-attainment in obese compared to non-obese patients in calculated linezolid therapy.
Busse, D; Dietrich, A; Dorn, C; Ehmann, L; Huisinga, W; Kloft, C; Petroff, D; Simon, P; Wrigge, H; Zeitlinger, M, 2020
)
1.08
" Further clinical studies with adjusted dosing regimens in for example intensive care patients are needed."( Risk of target non-attainment in obese compared to non-obese patients in calculated linezolid therapy.
Busse, D; Dietrich, A; Dorn, C; Ehmann, L; Huisinga, W; Kloft, C; Petroff, D; Simon, P; Wrigge, H; Zeitlinger, M, 2020
)
0.78
" Dosing of medications during ECMO can be challenging due to several factors, including sequestration of medications within ECMO circuits, alterations in volume of distribution, and changes in drug clearance."( Pharmacokinetics of linezolid for methicillin-resistant Staphylococcus aureus pneumonia in an adult receiving extracorporeal membrane oxygenation.
Mohrien, K; Nikolos, P; Osorio, J; Rose, C, 2020
)
0.88
" Finally, 20 and 33 were proved to target Ddl in bacterio via intracellular LC-MS dosage of d-Ala, l-Ala and d-Ala-d-Ala."( Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting d-alanyl-d-alanine ligase in bacterio.
Ameryckx, A; Frédérick, R; Pochet, L; Saadi, BE; Van Bambeke, F; Wang, G; Wouters, J; Yildiz, E, 2020
)
0.56
" Using C3HeB/FeJ and BALB/c mouse models of tuberculosis disease, thrice-weekly linezolid dosing was compared with daily dosing, with intermittent dosing introduced (i) from treatment initiation or (ii) after an initial period of daily dosing."( Preserved Efficacy and Reduced Toxicity with Intermittent Linezolid Dosing in Combination with Bedaquiline and Pretomanid in a Murine Tuberculosis Model.
Bigelow, KM; Chang, YS; Dooley, KE; Nuermberger, EL; Tasneen, R, 2020
)
1.03
" Nevertheless caution is required because of the adverse effects it causes, especially when the linezolid daily dosage exceeds 600 mg."( Linezolid: a Promising Agent for the Treatment of Multiple and Extensively Drug-Resistant Tuberculosis.
Dedes, VK; Fermeli, DD; Liarakos, AD; Marantos, TD; Panayiotakopoulos, GD; Panoutsopoulos, GI, 2020
)
2.22
"According to the drug label, linezolid dosage adjustments are not needed in geriatric patients."( Supra-therapeutic Linezolid Trough Concentrations in Elderly Patients: A Call for Action?
Baldelli, S; Bonini, I; Cattaneo, D; Clementi, E; Cozzi, V; Fusi, M; Gervasoni, C, 2021
)
1.25
" Reduced linezolid dosing schemes should be potentially considered in elderly patients at a low risk of treatment failure, ideally guided by therapeutic drug monitoring."( Supra-therapeutic Linezolid Trough Concentrations in Elderly Patients: A Call for Action?
Baldelli, S; Bonini, I; Cattaneo, D; Clementi, E; Cozzi, V; Fusi, M; Gervasoni, C, 2021
)
1.37
"Therapeutic drug monitoring (TDM) and model-informed precision dosing (MIPD) have evolved as important tools to inform rational dosing of antibiotics in individual patients with infections."( From Therapeutic Drug Monitoring to Model-Informed Precision Dosing for Antibiotics.
Alffenaar, JW; Friberg, LE; Koch, BCP; Märtson, AG; Minichmayr, IK; Nielsen, EI; Wicha, SG, 2021
)
0.62
" The current anti-MRSA antibiotics and medications for ABPA dosing recommendations are discussed."( State of the art in cystic fibrosis pharmacology optimization of antimicrobials in the treatment of cystic fibrosis pulmonary exacerbations: III. Executive summary.
Epps, KL; Epps, QJ; Young, DC; Zobell, JT, 2021
)
0.62
" The final PK model was then used to construct software for dosage individualization, and the performance of the software was assessed using 10 new patients not used to construct the original population PK model."( Dosage Individualization of Linezolid: Precision Dosing of Linezolid To Optimize Efficacy and Minimize Toxicity.
Álvarez-Lerma, F; Barceló-Vidal, J; Campillo, N; Grau, S; Hope, W; Horcajada, JP; Luque, S; Masclans-Enviz, JR; Muñoz-Bermudez, R; Neely, M; Sorli, L, 2021
)
0.92
"The aim of this study is to use a population pharmacokinetic (PK) approach to evaluate the optimal dosing strategy for linezolid (LNZ) in critically ill patients."( Pharmacokinetics of Linezolid Dose Adjustment for Creatinine Clearance in Critically Ill Patients: A Multicenter, Prospective, Open-Label, Observational Study.
Chen, C; Chen, S; Hou, Y; Lan, J; Li, Z; Luo, J; Qiu, B; Wang, X; Wang, Y; Wu, Z; Yao, F; Zheng, Z, 2021
)
1.15
" For MIC ≤2 mg/L, the standard dosing regimen (600 mg q12h) for patients with severe renal impairment (CrCL, 40 mL/min) and standard dosing or 900 mg q12h for patients with normal renal functions (CrCL, 80 mL/min) could achieve PTTA ≥74%."( Pharmacokinetics of Linezolid Dose Adjustment for Creatinine Clearance in Critically Ill Patients: A Multicenter, Prospective, Open-Label, Observational Study.
Chen, C; Chen, S; Hou, Y; Lan, J; Li, Z; Luo, J; Qiu, B; Wang, X; Wang, Y; Wu, Z; Yao, F; Zheng, Z, 2021
)
0.94
"We evaluated Nix-TB trial data (NCT02333799, N = 109) to provide dosing recommendations to potentially minimize linezolid toxicity in patients with extensively drug-resistant tuberculosis."( Proposed Linezolid Dosing Strategies to Minimize Adverse Events for Treatment of Extensively Drug-Resistant Tuberculosis.
Conradie, F; Imperial, MZ; Nedelman, JR; Savic, RM, 2022
)
1.35
"Simple neuropathy symptom and hemoglobin monitoring may guide linezolid dosing to avoid toxicities, but prospective testing is needed to confirm the benefit-to-risk ratio."( Proposed Linezolid Dosing Strategies to Minimize Adverse Events for Treatment of Extensively Drug-Resistant Tuberculosis.
Conradie, F; Imperial, MZ; Nedelman, JR; Savic, RM, 2022
)
1.38
" The probability of target attainment (PTA, PK/PD target: unbound (f) area-under-the-concentration-time-curve (AUC)/minimal inhibitory concentration (MIC) of 119) as well as a region-specific cumulative fraction of response (CFR) were estimated for different dosing regimens."( Population pharmacokinetics and target attainment analysis of linezolid in multidrug-resistant tuberculosis patients.
Baldelli, S; Cattaneo, D; Kroemer, N; Tietjen, AK; Wicha, SG, 2022
)
0.96
"For many antibiotics, the convenient one-fits-all dosing regimen had to be abandoned."( Quantification of Antibiotics in Patient Samples: State of the Art in Standardization and Proficiency Testing.
Hess, C; Kessler, A; Schneider, H; Steimer, W, 2022
)
0.72
"Severe lactic acidosis, a mitochondrial toxicity caused by the recommended standard dosage of linezolid (LZD), may occur in patients with impaired renal function."( Lactic acidosis associated with standard dose linezolid in a kidney recipient with impaired renal function.
Chen, CC; Lin, SH; Liu, WT,
)
0.61
" Therefore, standard dosing of anti-infective agents may not reach the optimal therapeutic targets."( Simultaneous determination of linezolid and voriconazole serum concentrations using liquid chromatography-tandem mass spectrometry.
Bian, X; Fang, J; He, X; Hu, F; Lu, Q; Shi, K; Wang, X, 2022
)
1.01
" Linezolid dosage adjustment was performed on days 3-5 based on the trough concentration."( Initial trough concentration may be beneficial in preventing linezolid-induced thrombocytopenia.
Atsuda, K; Hiratsuka, K; Inoue, G; Kawamura, A; Komatsu, T; Nakamura, M; Sakanoue, K; Takaso, M; Takayama, Y; Uchiyama, K, 2022
)
1.87
" Among the mono-fluorinated analogs prepared, 5-fluoro-PAS, exhibited the best activity and an 11-fold decreased rate of inactivation by NAT-1 that translated to a 5-fold improved exposure as measured by area-under-the-curve (AUC) following oral dosing to CD-1 mice."( Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
Aldrich, CC; Baughn, AD; Boshoff, HIM; Dartois, V; Hegde, PV; Howe, MD; Jia, Z; Pan, Y; Remache, B; Sharma, S; Zimmerman, MD, 2022
)
0.72
" However, the long-term use of this drug for TB treatment has been limited by adverse reactions and uncertainty regarding optimal dosage regimens for balancing drug efficacy and safety across different populations."( Linezolid Pharmacokinetics/Pharmacodynamics-Based Optimal Dosing for Multidrug-Resistant Tuberculosis.
Chu, N; Ding, Y; Li, Q; Liu, Z; Lu, Y; Nie, W; Shi, W; Wang, Q; Yang, Y; Zhou, W; Zhu, H, 2022
)
2.16
" The probability of target attainment for different dosage regimens was evaluated via Monte Carlo simulation."( Linezolid Pharmacokinetics/Pharmacodynamics-Based Optimal Dosing for Multidrug-Resistant Tuberculosis.
Chu, N; Ding, Y; Li, Q; Liu, Z; Lu, Y; Nie, W; Shi, W; Wang, Q; Yang, Y; Zhou, W; Zhu, H, 2022
)
2.16
"Optimal dosage regimens for patients weighing < 50 kg and ≥ 50 kg were 450 mg/d and 600 mg/d, respectively."( Linezolid Pharmacokinetics/Pharmacodynamics-Based Optimal Dosing for Multidrug-Resistant Tuberculosis.
Chu, N; Ding, Y; Li, Q; Liu, Z; Lu, Y; Nie, W; Shi, W; Wang, Q; Yang, Y; Zhou, W; Zhu, H, 2022
)
2.16
"The optimal linezolid dosage should be adjusted based on the patient's body size, renal function and age."( Parametric population pharmacokinetics of linezolid: A systematic review.
Chen, YT; Jiao, Z; Qin, Y; Ye, YR; Zhang, LL, 2022
)
1.36
" Alternative dosing regimens are suggested to address these insufficient levels, which are substantial factors contributing to the emergence of multidrug-resistant bacteria, resulting in increased morbidity and mortality among people who are critically ill."( Applying pharmacokinetic/pharmacodynamic measurements for linezolid in critically ill patients: optimizing efficacy and reducing resistance occurrence.
Abozahra, RR; El-Gaml, RM; El-Khodary, NM; El-Masry, SM; El-Tayar, AA, 2022
)
0.97
" This comprehensive review aimed to summarize population pharmacokinetic models of linezolid, by focusing on dosage optimization to maximize the probability of attaining a certain pharmacokinetic-pharmacodynamic parameter in special populations."( A Review of Population Pharmacokinetic Analyses of Linezolid.
Bandín-Vilar, E; Campos-Toimil, M; Castro-Balado, A; Fernández-Ferreiro, A; García-Quintanilla, L; González-Barcia, M; Mangas-Sanjuan, V; Mondelo-García, C; Zarra-Ferro, I, 2022
)
1.2
" Dosage regimens simulated the human PK of DAL (1500 mg, single dose), vancomycin (VAN) (1000 mg/12 h) and linezolid (LZD) (600 mg/12 h), alone and with RIF (600 mg/24 h)."( Comparative efficacy of dalbavancin alone and with rifampicin against in vitro biofilms in a pharmacodynamic model with methicillin-resistant Staphylococcus aureus.
Benavent, E; El Haj, C; Gomez-Junyent, J; Murillo, O; Rigo-Bonnin, R; Rosselló, I; Sierra, Y; Soldevila, L; Torrejón, B, 2022
)
0.93
"Currently, antibiotic treatment is often a standard dosing regimen in bone and joint infections (BJI)."( The mysteries of target site concentrations of antibiotics in bone and joint infections: what is known? A narrative review.
Abdulla, A; Bos, K; de Winter, BCM; Koch, BCP; Muller, AE; Oosterhoff, M; van Oldenrijk, J; Zhao, Q, 2022
)
0.72
" Ciprofloxacin, cefazolin, cefuroxime, vancomycin and linezolid seem to have adequate average exposure if correlating total concentration to ECOFF, when standard dosing is used."( The mysteries of target site concentrations of antibiotics in bone and joint infections: what is known? A narrative review.
Abdulla, A; Bos, K; de Winter, BCM; Koch, BCP; Muller, AE; Oosterhoff, M; van Oldenrijk, J; Zhao, Q, 2022
)
0.97
" Therefore, conventional or standard dosing regimens do not achieve satisfactory anti-infective effects."( A UPLC-MS/MS method for simultaneous determination of eight special-grade antimicrobials in human plasma and application in TDM.
Liu, G; Qi, Y, 2022
)
0.72
" The dosage was selected based on mouse pharmacokinetic analysis of both linezolid and TBI-223, as well as measurement of the MICs."( The Novel Oxazolidinone TBI-223 Is Effective in Three Preclinical Mouse Models of Methicillin-Resistant Staphylococcus aureus Infection.
Archer, NK; Dikeman, DA; Fotouhi, N; Gordon, O; Gough, E; Kaushik, A; Miller, LS; Mumtaz, M; Nuermberger, EL; Orlando, N; Ortines, RV; Patel, AM; Upton, AM; Wang, Y; Youn, C; Zhang, J, 2022
)
0.95
" Therefore, there is a need to use not only new drug molecules with antibacterial activities in the dosage form but also a different approach to pharmacotherapeutic strategies for skin infections, which lead to a reduction in the concentration of biocides."( Linezolid@MOF-74 as a host-guest system with antimicrobial activity.
Aguila-Rosas, J; Guzmán, A; Ibarra, IA; Lara-García, HA; Lima, E; Quirino-Barreda, CT; Ramos, D; Santiago-Tellez, A, 2022
)
2.16
" The standard linezolid dosage regimen achieved the therapeutic range in only 54."( Linezolid Population Pharmacokinetics to Improve Dosing in Cardiosurgical Patients: Factoring a New Drug-Drug Interaction Pathway.
Cojutti, PG; Della Siega, P; Gerussi, V; Pai, MP; Pea, F; Tascini, C, 2023
)
2.71
" Hence, new compounds are being developed, available drugs are repurposed, and the dosing of existing drugs is optimized, resulting in the largest drug development portfolio in TB history."( New and Repurposed Drugs for the Treatment of Active Tuberculosis: An Update for Clinicians.
Abulfathi, AA; Aguilar Diaz, JM; Boeree, MJ; Kuipers, S; Magis-Escurra, C; Raaijmakers, J; Svensson, EM; Te Brake, LH; van Ingen, J, 2023
)
0.91
" Thus, it is necessary to decide the antibiotic dosage considering the CRRT clearance in addition to residual renal function."( UHPLC-MS/MS method for simultaneous quantification of doripenem, meropenem, ciprofloxacin, levofloxacin, pazufloxacin, linezolid, and tedizolid in filtrate during continuous renal replacement therapy.
Goto, K; Itoh, H; Kai, M; Kitano, T; Ohchi, Y; Suzuki, Y; Tanaka, R; Tatsuta, R; Yasuda, N, 2023
)
1.12
"To summarize the pharmacokinetics of linezolid to optimize the dosing regimen in special populations."( Linezolid pharmacokinetics: a systematic review for the best clinical practice.
Heidari, S; Khalili, H, 2023
)
2.63
" In pediatrics, reducing the linezolid dosing interval to 8 h is suggested."( Linezolid pharmacokinetics: a systematic review for the best clinical practice.
Heidari, S; Khalili, H, 2023
)
2.64
" The objectives of this study were to establish a population pharmacokinetic model for linezolid in plasma and cerebrospinal fluid, as well as to optimize dosing strategies in this susceptible population."( Population Pharmacokinetics and Dosing Regimen Optimization of Linezolid in Cerebrospinal Fluid and Plasma of Post-operative Neurosurgical Patients.
Cao, P; Dong, H; Li, S; Meng, L; Wang, Y; Zhu, Y, 2023
)
1.37
" Based on simulation results, optimal dosage regimens stratified by various renal functions and inflammatory status were proposed."( Population Pharmacokinetics and Dosing Regimen Optimization of Linezolid in Cerebrospinal Fluid and Plasma of Post-operative Neurosurgical Patients.
Cao, P; Dong, H; Li, S; Meng, L; Wang, Y; Zhu, Y, 2023
)
1.15
"Dose adjustment, shortening the dosing interval, and continuous infusion were proposed as regimen optimization."( A Systematic Review of Linezolid Pharmacokinetics/Pharmacodynamics in Patients Undergoing Continuous Renal Replacement Therapy: Does One Size Fit All?
Chen, F; Ge, XH; Guo, HL; Ji, X; Liu, Y; Miao, HJ; Xu, J; Zhang, Y, 2023
)
1.22
" He was diagnosed with meningitis and the dosage of vancomycin was increased."( Nosocomial meningitis caused by Staphylococcus haemolyticus in a child with neutropenia in the absence of intracranial devices: a case report.
Fujikawa, T; Hasegawa, D; Kasai, M; Kosaka, Y; Mizuno, S; Uemura, S, 2023
)
0.91
" Linezolid dosing and clinical management was provider driven, and most patients had linezolid adjusted by therapeutic drug monitoring."( Implementation of Bedaquiline, Pretomanid, and Linezolid in the United States: Experience Using a Novel All-Oral Treatment Regimen for Treatment of Rifampin-Resistant or Rifampin-Intolerant Tuberculosis Disease.
Andrino, BB; Ashkin, D; Burgos, M; Caloia, LA; Chen, L; Colon-Semidey, A; DeSilva, MB; Dhanireddy, S; Dorman, SE; Dworkin, FF; Easton, AV; Gaensbauer, JT; Ghassemieh, B; Gomez, ME; Goswami, ND; Haley, CA; Hammond-Epstein, H; Horne, D; Jasuja, S; Jones, BA; Kaplan, LJ; Khan, AE; Kracen, E; Labuda, S; Landers, KM; Lardizabal, AA; Lasley, MT; Letzer, DM; Lopes, VK; Lubelchek, RJ; Mihalyov, A; Misch, EA; Murray, JA; Narita, M; Nilsen, DM; Ninneman, MJ; Ogawa, L; Oladele, A; Overman, M; Patricia Macias, C; Peloquin, CA; Peter Cegielski, J; Ray, SM; Ritger, KA; Rowlinson, MC; Sabuwala, N; Schechter, MC; Schiller, TM; Schwartz, LE; Spitters, C; Thomson, DB; Tresgallo, RR; Valois, P, 2023
)
2.08
" Use of individualized linezolid dosing and monitoring likely enhanced safety and treatment completion."( Implementation of Bedaquiline, Pretomanid, and Linezolid in the United States: Experience Using a Novel All-Oral Treatment Regimen for Treatment of Rifampin-Resistant or Rifampin-Intolerant Tuberculosis Disease.
Andrino, BB; Ashkin, D; Burgos, M; Caloia, LA; Chen, L; Colon-Semidey, A; DeSilva, MB; Dhanireddy, S; Dorman, SE; Dworkin, FF; Easton, AV; Gaensbauer, JT; Ghassemieh, B; Gomez, ME; Goswami, ND; Haley, CA; Hammond-Epstein, H; Horne, D; Jasuja, S; Jones, BA; Kaplan, LJ; Khan, AE; Kracen, E; Labuda, S; Landers, KM; Lardizabal, AA; Lasley, MT; Letzer, DM; Lopes, VK; Lubelchek, RJ; Mihalyov, A; Misch, EA; Murray, JA; Narita, M; Nilsen, DM; Ninneman, MJ; Ogawa, L; Oladele, A; Overman, M; Patricia Macias, C; Peloquin, CA; Peter Cegielski, J; Ray, SM; Ritger, KA; Rowlinson, MC; Sabuwala, N; Schechter, MC; Schiller, TM; Schwartz, LE; Spitters, C; Thomson, DB; Tresgallo, RR; Valois, P, 2023
)
1.48
" Nonetheless, there is a lack in pharmacokinetics information for this population, and dosing criteria may vary between healthcare centers."( Model-informed precision dosing of antimicrobial drugs in pediatrics: experiences from a pilot scale program.
Arriaga-García, FJ; Medellín-Garibay, SE; Milán-Segovia, RDC; Pérez-González, LF; Rodríguez-Báez, AS; Romano-Moreno, S; Velarde-Salcedo, R, 2023
)
0.91
" In addition, the possibility of compensation by dosage adjustments was evaluated."( Rifampicin reduces plasma concentration of linezolid in patients with infective endocarditis.
Bock, M; Bruun, NE; Bundgaard, H; Christensen, JJ; Christiansen, U; Elming, H; Fosbøl, EL; Fuursted, K; Gill, S; Helweg-Larsen, J; Høfsten, DE; Høiby, N; Ihlemann, N; Iversen, K; Køber, L; Moser, C; Povlsen, JA; Pries-Heje, MM; Rosenvinge, FS; Schwartz, F; Torp-Pedersen, C; Tønder, N; Van Hasselt, JGC; Wang, H, 2023
)
1.17
" Model-based dosing simulations showed that rifampicin cotreatment decreased the PTA of linezolid from 94."( Rifampicin reduces plasma concentration of linezolid in patients with infective endocarditis.
Bock, M; Bruun, NE; Bundgaard, H; Christensen, JJ; Christiansen, U; Elming, H; Fosbøl, EL; Fuursted, K; Gill, S; Helweg-Larsen, J; Høfsten, DE; Høiby, N; Ihlemann, N; Iversen, K; Køber, L; Moser, C; Povlsen, JA; Pries-Heje, MM; Rosenvinge, FS; Schwartz, F; Torp-Pedersen, C; Tønder, N; Van Hasselt, JGC; Wang, H, 2023
)
1.4
"Amoxicillin, ceftriaxone, several oral cephalosporins, tedizolid, and dalbavancin exhibited anti-treponemal activity at concentrations achievable in human plasma following regular dosing regimens."( Antimicrobial susceptibility of Treponema pallidum subspecies pallidum: an in-vitro study.
Canut, A; Giacani, L; González-Beiras, C; González-Candelas, F; Greninger, AL; Lieberman, NAP; Mitjà, O; Mueller, J; Pérez-Mañá, C; Rodríguez-Gascón, A; Suñer, C; Tantalo, LC; Tapia, K; Ubals, M; Vall Mayans, M, 2023
)
0.91
"Antibiotic therapy requires appropriate dosage of drugs for effective treatment."( A Liquid Chromatography-Tandem Mass Spectrometry Method for Simultaneously Determining Meropenem and Linezolid in Blood and Cerebrospinal Fluid.
Berska, J; Bugajska, J; Sztefko, K, 2024
)
1.66
" All the patients started with a dosage of 600 mg, twice daily."( Linezolid dose adjustment according to therapeutic drug monitoring helps reach the goal concentration in severe patients, and the oldest seniors benefit more.
Liang, P; Qu, C; Xu, Y; Yang, X, 2023
)
2.35
"8%, and 75% of patients had supra-therapeutic linezolid trough concentrations at the first TDM assessment in different age group, leading to the dosage adjustment rate of 31."( Linezolid dose adjustment according to therapeutic drug monitoring helps reach the goal concentration in severe patients, and the oldest seniors benefit more.
Liang, P; Qu, C; Xu, Y; Yang, X, 2023
)
2.61
" The linezolid dosage adjustments according to TDM help reach the therapeutic concentration."( Linezolid dose adjustment according to therapeutic drug monitoring helps reach the goal concentration in severe patients, and the oldest seniors benefit more.
Liang, P; Qu, C; Xu, Y; Yang, X, 2023
)
2.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
protein synthesis inhibitorA compound, usually an anti-bacterial agent or a toxin, which inhibits the synthesis of a protein.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
oxazolidinoneAn oxazolidine containing one or more oxo groups.
morpholinesAny compound containing morpholine as part of its structure.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
acetamidesCompounds with the general formula RNHC(=O)CH3.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (90)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency27.31710.000811.382244.6684AID686978; AID686979
EWS/FLI fusion proteinHomo sapiens (human)Potency9.42540.001310.157742.8575AID1259253; AID1259255; AID1259256
estrogen nuclear receptor alphaHomo sapiens (human)Potency13.33320.000229.305416,493.5996AID743079
GVesicular stomatitis virusPotency37.90830.01238.964839.8107AID1645842
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.48130.01789.637444.6684AID588834
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
Interferon betaHomo sapiens (human)Potency37.90830.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)105.40000.00032.63119.0000AID1207747
Bile salt export pumpHomo sapiens (human)IC50 (µMol)566.50000.11007.190310.0000AID1449628; AID1473738
30S ribosomal protein S6Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S7Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L15Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)20.00000.00011.774010.0000AID1056339; AID745377
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)20.00000.00011.753610.0000AID1056336; AID745375
50S ribosomal protein L10Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L11Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L7/L12Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L19Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L1Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L20Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L27Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L28Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L29Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L31Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L31 type BEscherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L32Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L33Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L34Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L35Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L36Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S10Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S11Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S12Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S13Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S16Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S18Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S19Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S20Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S2Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S3Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S4Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S5Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S8Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S9Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L13Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L14Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L16Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L23Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S15Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
DNA gyrase subunit AEscherichia coli K-12IC50 (µMol)32.00000.02390.56295.2300AID1167728
DNA gyrase subunit BEscherichia coli K-12IC50 (µMol)32.00000.00500.43985.2300AID1167728
50S ribosomal protein L17Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L21Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L30Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L6Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S14Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S17Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S1Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L18Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)20.00000.00002.015110.0000AID1056337; AID745376
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)20.00000.00002.800510.0000AID1056338; AID745378
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50 (µMol)17.00000.00040.764912.5000AID126688
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)46.00000.00002.37899.7700AID1265126
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki33.97500.00192.379710.0000AID292903; AID303963; AID319168; AID751392
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)8.19000.00021.557410.0000AID1553385
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)9.55000.00001.89149.5700AID1265127; AID434137
Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)IC50 (µMol)8.19008.19008.19008.1900AID1553386
Cytochrome P450 2C19Homo sapiens (human)Ki53.00000.00010.830010.0000AID303963
50S ribosomal protein L2Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L3Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L24Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L4Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L22Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L5Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
30S ribosomal protein S21Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
50S ribosomal protein L25Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)105.40000.00032.59559.0000AID1207747
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)105.40000.00032.63119.0000AID1207747
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)105.40000.00032.25459.6000AID1207747
50S ribosomal protein L36 2Escherichia coli K-12IC50 (µMol)1,150.00000.00891.20355.0000AID531644; AID531645
Dual specificity tyrosine-phosphorylation-regulated kinase 1AMus musculus (house mouse)IC50 (µMol)20.00000.01202.50605.0000AID1056337
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
ReninCallithrix jacchus (white-tufted-ear marmoset)IC50 (µMol)17.00000.08003.12676.7000AID434137
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)3.07800.06008.9128130.5170AID1902; AID1914
Estrogen receptorRattus norvegicus (Norway rat)EC50 (µMol)5.99800.006022.3670130.5170AID1914
Estrogen receptor betaRattus norvegicus (Norway rat)EC50 (µMol)5.99800.006022.3670130.5170AID1914
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)INH100.00000.10000.10000.1000AID1553380
Cytochrome P450 3A4Homo sapiens (human)INH100.00001.70002.85004.0000AID1553384
Cytochrome P450 2D6Homo sapiens (human)INH100.00003.20003.40003.6000AID1553383
Cytochrome P450 2C9 Homo sapiens (human)INH100.00004.40007.00009.1000AID1553381
Cytochrome P450 2C19Homo sapiens (human)INH100.00007.00007.00007.0000AID1553382
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (235)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytoplasmic translation30S ribosomal protein S6Escherichia coli K-12
translation30S ribosomal protein S6Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S7Escherichia coli K-12
negative regulation of translation30S ribosomal protein S7Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S7Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S7Escherichia coli K-12
translation30S ribosomal protein S7Escherichia coli K-12
negative regulation of translation30S ribosomal protein S7Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L15Escherichia coli K-12
translation50S ribosomal protein L15Escherichia coli K-12
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
cytoplasmic translation50S ribosomal protein L10Escherichia coli K-12
translation50S ribosomal protein L10Escherichia coli K-12
regulation of translation50S ribosomal protein L10Escherichia coli K-12
negative regulation of translation50S ribosomal protein L10Escherichia coli K-12
translation50S ribosomal protein L11Escherichia coli K-12
translational termination50S ribosomal protein L11Escherichia coli K-12
stringent response50S ribosomal protein L11Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L11Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L11Escherichia coli K-12
translation50S ribosomal protein L11Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L7/L12Escherichia coli K-12
translation50S ribosomal protein L7/L12Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L19Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L19Escherichia coli K-12
translation50S ribosomal protein L19Escherichia coli K-12
negative regulation of translational initiation50S ribosomal protein L1Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L1Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L1Escherichia coli K-12
translation50S ribosomal protein L1Escherichia coli K-12
regulation of translation50S ribosomal protein L1Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L20Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L20Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L20Escherichia coli K-12
translation50S ribosomal protein L20Escherichia coli K-12
negative regulation of translation50S ribosomal protein L20Escherichia coli K-12
cytosolic ribosome assembly50S ribosomal protein L27Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L27Escherichia coli K-12
regulation of cell growth50S ribosomal protein L27Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L27Escherichia coli K-12
translation50S ribosomal protein L27Escherichia coli K-12
positive regulation of ribosome biogenesis50S ribosomal protein L27Escherichia coli K-12
assembly of large subunit precursor of preribosome50S ribosomal protein L27Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L28Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L28Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L28Escherichia coli K-12
translation50S ribosomal protein L28Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L29Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L29Escherichia coli K-12
translation50S ribosomal protein L29Escherichia coli K-12
translation50S ribosomal protein L31Escherichia coli K-12
translational initiation50S ribosomal protein L31Escherichia coli K-12
negative regulation of cytoplasmic translational initiation50S ribosomal protein L31Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L31Escherichia coli K-12
translation50S ribosomal protein L31Escherichia coli K-12
cellular response to zinc ion starvation50S ribosomal protein L31 type BEscherichia coli K-12
cytoplasmic translation50S ribosomal protein L31 type BEscherichia coli K-12
translation50S ribosomal protein L31 type BEscherichia coli K-12
response to reactive oxygen species50S ribosomal protein L32Escherichia coli K-12
response to radiation50S ribosomal protein L32Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L32Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L32Escherichia coli K-12
translation50S ribosomal protein L32Escherichia coli K-12
response to antibiotic50S ribosomal protein L33Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L33Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L33Escherichia coli K-12
translation50S ribosomal protein L33Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L34Escherichia coli K-12
translation50S ribosomal protein L34Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L35Escherichia coli K-12
translation50S ribosomal protein L35Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L36Escherichia coli K-12
translation50S ribosomal protein L36Escherichia coli K-12
transcription antitermination30S ribosomal protein S10Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S10Escherichia coli K-12
translation30S ribosomal protein S10Escherichia coli K-12
transcription antitermination30S ribosomal protein S10Escherichia coli K-12
regulation of DNA-templated transcription elongation30S ribosomal protein S10Escherichia coli K-12
ribosome biogenesis30S ribosomal protein S10Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S11Escherichia coli K-12
translation30S ribosomal protein S11Escherichia coli K-12
Group I intron splicing30S ribosomal protein S12Escherichia coli K-12
positive regulation of RNA splicing30S ribosomal protein S12Escherichia coli K-12
RNA folding30S ribosomal protein S12Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S12Escherichia coli K-12
translation30S ribosomal protein S12Escherichia coli K-12
response to antibiotic30S ribosomal protein S12Escherichia coli K-12
maintenance of translational fidelity30S ribosomal protein S12Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S13Escherichia coli K-12
translation30S ribosomal protein S13Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S16Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S16Escherichia coli K-12
DNA metabolic process30S ribosomal protein S16Escherichia coli K-12
translation30S ribosomal protein S16Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S18Escherichia coli K-12
translation30S ribosomal protein S18Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S19Escherichia coli K-12
translation30S ribosomal protein S19Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S19Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S20Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S20Escherichia coli K-12
translation30S ribosomal protein S20Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S2Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S2Escherichia coli K-12
translation30S ribosomal protein S2Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S3Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S3Escherichia coli K-12
translation30S ribosomal protein S3Escherichia coli K-12
transcription antitermination30S ribosomal protein S4Escherichia coli K-12
negative regulation of translational initiation30S ribosomal protein S4Escherichia coli K-12
maintenance of translational fidelity30S ribosomal protein S4Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S4Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S4Escherichia coli K-12
DNA-templated transcription termination30S ribosomal protein S4Escherichia coli K-12
translation30S ribosomal protein S4Escherichia coli K-12
regulation of translation30S ribosomal protein S4Escherichia coli K-12
transcription antitermination30S ribosomal protein S4Escherichia coli K-12
ribosome biogenesis30S ribosomal protein S4Escherichia coli K-12
response to antibiotic30S ribosomal protein S4Escherichia coli K-12
ribosomal small subunit biogenesis30S ribosomal protein S4Escherichia coli K-12
maintenance of translational fidelity30S ribosomal protein S5Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S5Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S5Escherichia coli K-12
translation30S ribosomal protein S5Escherichia coli K-12
response to antibiotic30S ribosomal protein S5Escherichia coli K-12
regulation of mRNA stability30S ribosomal protein S8Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S8Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S8Escherichia coli K-12
translation30S ribosomal protein S8Escherichia coli K-12
regulation of translation30S ribosomal protein S8Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S9Escherichia coli K-12
translation30S ribosomal protein S9Escherichia coli K-12
negative regulation of translation50S ribosomal protein L13Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L13Escherichia coli K-12
translation50S ribosomal protein L13Escherichia coli K-12
negative regulation of translation50S ribosomal protein L13Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L14Escherichia coli K-12
translation50S ribosomal protein L14Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L16Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L16Escherichia coli K-12
translation50S ribosomal protein L16Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L23Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L23Escherichia coli K-12
translation50S ribosomal protein L23Escherichia coli K-12
translation30S ribosomal protein S15Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S15Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S15Escherichia coli K-12
translation30S ribosomal protein S15Escherichia coli K-12
regulation of translation30S ribosomal protein S15Escherichia coli K-12
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit AEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit AEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
response to antibioticDNA gyrase subunit AEscherichia coli K-12
chromosome organizationDNA gyrase subunit AEscherichia coli K-12
negative regulation of DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit BEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit BEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit BEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
response to antibioticDNA gyrase subunit BEscherichia coli K-12
chromosome organizationDNA gyrase subunit BEscherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L17Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L17Escherichia coli K-12
translation50S ribosomal protein L17Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L21Escherichia coli K-12
translation50S ribosomal protein L21Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L30Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L30Escherichia coli K-12
translation50S ribosomal protein L30Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L6Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L6Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L6Escherichia coli K-12
translation50S ribosomal protein L6Escherichia coli K-12
response to antibiotic50S ribosomal protein L6Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S14Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S14Escherichia coli K-12
translation30S ribosomal protein S14Escherichia coli K-12
response to antibiotic30S ribosomal protein S17Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S17Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S17Escherichia coli K-12
translation30S ribosomal protein S17Escherichia coli K-12
response to antibiotic30S ribosomal protein S17Escherichia coli K-12
translation30S ribosomal protein S1Escherichia coli K-12
RNA secondary structure unwinding30S ribosomal protein S1Escherichia coli K-12
negative regulation of cytoplasmic translation30S ribosomal protein S1Escherichia coli K-12
positive regulation of cytoplasmic translation30S ribosomal protein S1Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S1Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S1Escherichia coli K-12
translation30S ribosomal protein S1Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L18Escherichia coli K-12
translation50S ribosomal protein L18Escherichia coli K-12
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
tricarboxylic acid cycleSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
succinate metabolic processSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
mitochondrial electron transport, succinate to ubiquinoneSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
nervous system developmentSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
respiratory electron transport chainSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
proton motive force-driven mitochondrial ATP synthesisSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
ribosomal large subunit assembly50S ribosomal protein L2Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L2Escherichia coli K-12
translation50S ribosomal protein L2Escherichia coli K-12
negative regulation of DNA-templated DNA replication initiation50S ribosomal protein L2Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L3Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L3Escherichia coli K-12
translation50S ribosomal protein L3Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L24Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L24Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L24Escherichia coli K-12
translation50S ribosomal protein L24Escherichia coli K-12
transcriptional attenuation50S ribosomal protein L4Escherichia coli K-12
negative regulation of cytoplasmic translation50S ribosomal protein L4Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L4Escherichia coli K-12
DNA-templated transcription termination50S ribosomal protein L4Escherichia coli K-12
translation50S ribosomal protein L4Escherichia coli K-12
regulation of translation50S ribosomal protein L4Escherichia coli K-12
negative regulation of translation50S ribosomal protein L4Escherichia coli K-12
ribosome assembly50S ribosomal protein L4Escherichia coli K-12
negative regulation of DNA-templated transcription50S ribosomal protein L4Escherichia coli K-12
response to antibiotic50S ribosomal protein L4Escherichia coli K-12
translation50S ribosomal protein L22Escherichia coli K-12
cytosolic ribosome assembly50S ribosomal protein L22Escherichia coli K-12
assembly of large subunit precursor of preribosome50S ribosomal protein L22Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L22Escherichia coli K-12
translation50S ribosomal protein L22Escherichia coli K-12
ribosome assembly50S ribosomal protein L22Escherichia coli K-12
response to antibiotic50S ribosomal protein L22Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L5Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L5Escherichia coli K-12
translation50S ribosomal protein L5Escherichia coli K-12
ribosomal small subunit assembly30S ribosomal protein S21Escherichia coli K-12
cytoplasmic translation30S ribosomal protein S21Escherichia coli K-12
translation30S ribosomal protein S21Escherichia coli K-12
translation50S ribosomal protein L25Escherichia coli K-12
response to radiation50S ribosomal protein L25Escherichia coli K-12
negative regulation of translation50S ribosomal protein L25Escherichia coli K-12
ribosomal large subunit assembly50S ribosomal protein L25Escherichia coli K-12
cytoplasmic translation50S ribosomal protein L25Escherichia coli K-12
translation50S ribosomal protein L25Escherichia coli K-12
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
translation50S ribosomal protein L36 2Escherichia coli K-12
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (126)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
structural constituent of ribosome30S ribosomal protein S6Escherichia coli K-12
protein binding30S ribosomal protein S6Escherichia coli K-12
rRNA binding30S ribosomal protein S6Escherichia coli K-12
mRNA 5'-UTR binding30S ribosomal protein S6Escherichia coli K-12
small ribosomal subunit rRNA binding30S ribosomal protein S6Escherichia coli K-12
tRNA binding30S ribosomal protein S7Escherichia coli K-12
RNA binding30S ribosomal protein S7Escherichia coli K-12
mRNA binding30S ribosomal protein S7Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S7Escherichia coli K-12
protein binding30S ribosomal protein S7Escherichia coli K-12
rRNA binding30S ribosomal protein S7Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L15Escherichia coli K-12
protein binding50S ribosomal protein L15Escherichia coli K-12
rRNA binding50S ribosomal protein L15Escherichia coli K-12
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
GTPase activity50S ribosomal protein L10Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L10Escherichia coli K-12
protein binding50S ribosomal protein L10Escherichia coli K-12
rRNA binding50S ribosomal protein L10Escherichia coli K-12
ribosome binding50S ribosomal protein L10Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L10Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L11Escherichia coli K-12
protein binding50S ribosomal protein L11Escherichia coli K-12
rRNA binding50S ribosomal protein L11Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L11Escherichia coli K-12
GTPase activity50S ribosomal protein L7/L12Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L7/L12Escherichia coli K-12
protein binding50S ribosomal protein L7/L12Escherichia coli K-12
protein homodimerization activity50S ribosomal protein L7/L12Escherichia coli K-12
ribosome binding50S ribosomal protein L7/L12Escherichia coli K-12
mRNA binding50S ribosomal protein L7/L12Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L19Escherichia coli K-12
rRNA binding50S ribosomal protein L19Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L19Escherichia coli K-12
tRNA binding50S ribosomal protein L1Escherichia coli K-12
RNA binding50S ribosomal protein L1Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L1Escherichia coli K-12
protein binding50S ribosomal protein L1Escherichia coli K-12
rRNA binding50S ribosomal protein L1Escherichia coli K-12
mRNA regulatory element binding translation repressor activity50S ribosomal protein L20Escherichia coli K-12
mRNA binding50S ribosomal protein L20Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L20Escherichia coli K-12
rRNA binding50S ribosomal protein L20Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L20Escherichia coli K-12
tRNA binding50S ribosomal protein L27Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L27Escherichia coli K-12
protein binding50S ribosomal protein L27Escherichia coli K-12
rRNA binding50S ribosomal protein L27Escherichia coli K-12
ribosome binding50S ribosomal protein L27Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L28Escherichia coli K-12
protein binding50S ribosomal protein L28Escherichia coli K-12
rRNA binding50S ribosomal protein L28Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L29Escherichia coli K-12
rRNA binding50S ribosomal protein L29Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L31Escherichia coli K-12
zinc ion binding50S ribosomal protein L31Escherichia coli K-12
rRNA binding50S ribosomal protein L31Escherichia coli K-12
metal ion binding50S ribosomal protein L31Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L31 type BEscherichia coli K-12
structural constituent of ribosome50S ribosomal protein L32Escherichia coli K-12
protein binding50S ribosomal protein L32Escherichia coli K-12
tRNA binding50S ribosomal protein L33Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L33Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L34Escherichia coli K-12
protein binding50S ribosomal protein L34Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L35Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L36Escherichia coli K-12
tRNA binding30S ribosomal protein S10Escherichia coli K-12
transcription antitermination factor activity, RNA binding30S ribosomal protein S10Escherichia coli K-12
RNA binding30S ribosomal protein S10Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S10Escherichia coli K-12
protein binding30S ribosomal protein S10Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S11Escherichia coli K-12
protein binding30S ribosomal protein S11Escherichia coli K-12
rRNA binding30S ribosomal protein S11Escherichia coli K-12
small ribosomal subunit rRNA binding30S ribosomal protein S11Escherichia coli K-12
tRNA binding30S ribosomal protein S12Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S12Escherichia coli K-12
protein binding30S ribosomal protein S12Escherichia coli K-12
rRNA binding30S ribosomal protein S12Escherichia coli K-12
misfolded RNA binding30S ribosomal protein S12Escherichia coli K-12
tRNA binding30S ribosomal protein S13Escherichia coli K-12
RNA binding30S ribosomal protein S13Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S13Escherichia coli K-12
protein binding30S ribosomal protein S13Escherichia coli K-12
rRNA binding30S ribosomal protein S13Escherichia coli K-12
four-way junction DNA binding30S ribosomal protein S16Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S16Escherichia coli K-12
endonuclease activity30S ribosomal protein S16Escherichia coli K-12
DNA endonuclease activity30S ribosomal protein S16Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S18Escherichia coli K-12
protein binding30S ribosomal protein S18Escherichia coli K-12
rRNA binding30S ribosomal protein S18Escherichia coli K-12
mRNA 5'-UTR binding30S ribosomal protein S18Escherichia coli K-12
small ribosomal subunit rRNA binding30S ribosomal protein S18Escherichia coli K-12
tRNA binding30S ribosomal protein S19Escherichia coli K-12
RNA binding30S ribosomal protein S19Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S19Escherichia coli K-12
rRNA binding30S ribosomal protein S19Escherichia coli K-12
RNA binding30S ribosomal protein S20Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S20Escherichia coli K-12
ornithine decarboxylase inhibitor activity30S ribosomal protein S20Escherichia coli K-12
rRNA binding30S ribosomal protein S20Escherichia coli K-12
small ribosomal subunit rRNA binding30S ribosomal protein S20Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S2Escherichia coli K-12
protein binding30S ribosomal protein S2Escherichia coli K-12
zinc ion binding30S ribosomal protein S2Escherichia coli K-12
RNA binding30S ribosomal protein S3Escherichia coli K-12
mRNA binding30S ribosomal protein S3Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S3Escherichia coli K-12
rRNA binding30S ribosomal protein S3Escherichia coli K-12
mRNA regulatory element binding translation repressor activity30S ribosomal protein S4Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S4Escherichia coli K-12
protein binding30S ribosomal protein S4Escherichia coli K-12
rRNA binding30S ribosomal protein S4Escherichia coli K-12
mRNA 5'-UTR binding30S ribosomal protein S4Escherichia coli K-12
RNA binding30S ribosomal protein S5Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S5Escherichia coli K-12
protein binding30S ribosomal protein S5Escherichia coli K-12
rRNA binding30S ribosomal protein S5Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S8Escherichia coli K-12
rRNA binding30S ribosomal protein S8Escherichia coli K-12
tRNA binding30S ribosomal protein S9Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S9Escherichia coli K-12
RNA binding30S ribosomal protein S9Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L13Escherichia coli K-12
zinc ion binding50S ribosomal protein L13Escherichia coli K-12
mRNA 5'-UTR binding50S ribosomal protein L13Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L13Escherichia coli K-12
mRNA binding50S ribosomal protein L13Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L14Escherichia coli K-12
protein binding50S ribosomal protein L14Escherichia coli K-12
rRNA binding50S ribosomal protein L14Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L14Escherichia coli K-12
tRNA binding50S ribosomal protein L16Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L16Escherichia coli K-12
rRNA binding50S ribosomal protein L16Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L23Escherichia coli K-12
protein binding50S ribosomal protein L23Escherichia coli K-12
rRNA binding50S ribosomal protein L23Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S15Escherichia coli K-12
rRNA binding30S ribosomal protein S15Escherichia coli K-12
small ribosomal subunit rRNA binding30S ribosomal protein S15Escherichia coli K-12
DNA bindingDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit AEscherichia coli K-12
protein bindingDNA gyrase subunit AEscherichia coli K-12
ATP bindingDNA gyrase subunit AEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit AEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit AEscherichia coli K-12
identical protein bindingDNA gyrase subunit AEscherichia coli K-12
DNA bindingDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit BEscherichia coli K-12
protein bindingDNA gyrase subunit BEscherichia coli K-12
ATP bindingDNA gyrase subunit BEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit BEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit BEscherichia coli K-12
metal ion bindingDNA gyrase subunit BEscherichia coli K-12
structural constituent of ribosome50S ribosomal protein L17Escherichia coli K-12
protein binding50S ribosomal protein L17Escherichia coli K-12
RNA binding50S ribosomal protein L21Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L21Escherichia coli K-12
rRNA binding50S ribosomal protein L21Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L30Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L6Escherichia coli K-12
rRNA binding50S ribosomal protein L6Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L6Escherichia coli K-12
tRNA binding30S ribosomal protein S14Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S14Escherichia coli K-12
rRNA binding30S ribosomal protein S14Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S17Escherichia coli K-12
zinc ion binding30S ribosomal protein S17Escherichia coli K-12
rRNA binding30S ribosomal protein S17Escherichia coli K-12
molecular adaptor activity30S ribosomal protein S17Escherichia coli K-12
small ribosomal subunit rRNA binding30S ribosomal protein S17Escherichia coli K-12
RNA binding30S ribosomal protein S1Escherichia coli K-12
single-stranded RNA binding30S ribosomal protein S1Escherichia coli K-12
mRNA binding30S ribosomal protein S1Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S1Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L18Escherichia coli K-12
5S rRNA binding50S ribosomal protein L18Escherichia coli K-12
rRNA binding50S ribosomal protein L18Escherichia coli K-12
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
succinate dehydrogenase activitySuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
protein bindingSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
succinate dehydrogenase (quinone) activitySuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
electron transfer activitySuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
flavin adenine dinucleotide bindingSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
RNA binding50S ribosomal protein L2Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L2Escherichia coli K-12
protein binding50S ribosomal protein L2Escherichia coli K-12
zinc ion binding50S ribosomal protein L2Escherichia coli K-12
transferase activity50S ribosomal protein L2Escherichia coli K-12
rRNA binding50S ribosomal protein L2Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L3Escherichia coli K-12
protein binding50S ribosomal protein L3Escherichia coli K-12
rRNA binding50S ribosomal protein L3Escherichia coli K-12
RNA binding50S ribosomal protein L24Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L24Escherichia coli K-12
protein binding50S ribosomal protein L24Escherichia coli K-12
rRNA binding50S ribosomal protein L24Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L24Escherichia coli K-12
RNA-binding transcription regulator activity50S ribosomal protein L4Escherichia coli K-12
DNA binding50S ribosomal protein L4Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L4Escherichia coli K-12
protein binding50S ribosomal protein L4Escherichia coli K-12
rRNA binding50S ribosomal protein L4Escherichia coli K-12
translation repressor activity50S ribosomal protein L4Escherichia coli K-12
mRNA 5'-UTR binding50S ribosomal protein L4Escherichia coli K-12
endoribonuclease inhibitor activity50S ribosomal protein L4Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L22Escherichia coli K-12
protein binding50S ribosomal protein L22Escherichia coli K-12
rRNA binding50S ribosomal protein L22Escherichia coli K-12
large ribosomal subunit rRNA binding50S ribosomal protein L22Escherichia coli K-12
tRNA binding50S ribosomal protein L5Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L5Escherichia coli K-12
5S rRNA binding50S ribosomal protein L5Escherichia coli K-12
rRNA binding50S ribosomal protein L5Escherichia coli K-12
RNA binding50S ribosomal protein L5Escherichia coli K-12
structural constituent of ribosome30S ribosomal protein S21Escherichia coli K-12
rRNA binding30S ribosomal protein S21Escherichia coli K-12
RNA binding50S ribosomal protein L25Escherichia coli K-12
structural constituent of ribosome50S ribosomal protein L25Escherichia coli K-12
5S rRNA binding50S ribosomal protein L25Escherichia coli K-12
rRNA binding50S ribosomal protein L25Escherichia coli K-12
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
structural constituent of ribosome50S ribosomal protein L36 2Escherichia coli K-12
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (64)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytoplasm30S ribosomal protein S6Escherichia coli K-12
cytosol30S ribosomal protein S6Escherichia coli K-12
ribosome30S ribosomal protein S6Escherichia coli K-12
intracellular organelle30S ribosomal protein S6Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S6Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S6Escherichia coli K-12
cytosol30S ribosomal protein S7Escherichia coli K-12
ribosome30S ribosomal protein S7Escherichia coli K-12
membrane30S ribosomal protein S7Escherichia coli K-12
cytoplasm30S ribosomal protein S7Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S7Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S7Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S7Escherichia coli K-12
ribosome30S ribosomal protein S7Escherichia coli K-12
ribosome50S ribosomal protein L15Escherichia coli K-12
cytoplasm50S ribosomal protein L15Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L15Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L15Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L15Escherichia coli K-12
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
cytosol50S ribosomal protein L10Escherichia coli K-12
ribosome50S ribosomal protein L10Escherichia coli K-12
cytoplasm50S ribosomal protein L10Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L10Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L10Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L10Escherichia coli K-12
cytosol50S ribosomal protein L11Escherichia coli K-12
ribosome50S ribosomal protein L11Escherichia coli K-12
cytoplasm50S ribosomal protein L11Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L11Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L11Escherichia coli K-12
cytoplasm50S ribosomal protein L7/L12Escherichia coli K-12
cytosol50S ribosomal protein L7/L12Escherichia coli K-12
ribosome50S ribosomal protein L7/L12Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L7/L12Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L7/L12Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L7/L12Escherichia coli K-12
cytosol50S ribosomal protein L19Escherichia coli K-12
ribosome50S ribosomal protein L19Escherichia coli K-12
cytoplasm50S ribosomal protein L19Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L19Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L19Escherichia coli K-12
cytosol50S ribosomal protein L1Escherichia coli K-12
ribosome50S ribosomal protein L1Escherichia coli K-12
cytoplasm50S ribosomal protein L1Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L1Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L1Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L1Escherichia coli K-12
cytosol50S ribosomal protein L20Escherichia coli K-12
ribosome50S ribosomal protein L20Escherichia coli K-12
cytoplasm50S ribosomal protein L20Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L20Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L20Escherichia coli K-12
ribosome50S ribosomal protein L27Escherichia coli K-12
cytoplasm50S ribosomal protein L27Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L27Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L27Escherichia coli K-12
cytosol50S ribosomal protein L28Escherichia coli K-12
ribosome50S ribosomal protein L28Escherichia coli K-12
cytoplasm50S ribosomal protein L28Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L28Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L28Escherichia coli K-12
ribosome50S ribosomal protein L29Escherichia coli K-12
cytoplasm50S ribosomal protein L29Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L29Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L29Escherichia coli K-12
cytosol50S ribosomal protein L31Escherichia coli K-12
ribosome50S ribosomal protein L31Escherichia coli K-12
cytoplasm50S ribosomal protein L31Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L31Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L31Escherichia coli K-12
ribosome50S ribosomal protein L31 type BEscherichia coli K-12
cytoplasm50S ribosomal protein L31 type BEscherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L31 type BEscherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L31 type BEscherichia coli K-12
cytosol50S ribosomal protein L32Escherichia coli K-12
ribosome50S ribosomal protein L32Escherichia coli K-12
cytoplasm50S ribosomal protein L32Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L32Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L32Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L32Escherichia coli K-12
cytoplasm50S ribosomal protein L33Escherichia coli K-12
cytosol50S ribosomal protein L33Escherichia coli K-12
ribosome50S ribosomal protein L33Escherichia coli K-12
intracellular organelle50S ribosomal protein L33Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L33Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L33Escherichia coli K-12
ribosome50S ribosomal protein L34Escherichia coli K-12
cytoplasm50S ribosomal protein L34Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L34Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L34Escherichia coli K-12
ribosome50S ribosomal protein L35Escherichia coli K-12
cytoplasm50S ribosomal protein L35Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L35Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L35Escherichia coli K-12
cytoplasm50S ribosomal protein L36Escherichia coli K-12
ribosome50S ribosomal protein L36Escherichia coli K-12
intracellular organelle50S ribosomal protein L36Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L36Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L36Escherichia coli K-12
cytosol30S ribosomal protein S10Escherichia coli K-12
ribosome30S ribosomal protein S10Escherichia coli K-12
cytoplasm30S ribosomal protein S10Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S10Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S10Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S10Escherichia coli K-12
cytosol30S ribosomal protein S11Escherichia coli K-12
ribosome30S ribosomal protein S11Escherichia coli K-12
cytoplasm30S ribosomal protein S11Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S11Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S11Escherichia coli K-12
cytosol30S ribosomal protein S12Escherichia coli K-12
ribosome30S ribosomal protein S12Escherichia coli K-12
cytoplasm30S ribosomal protein S12Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S12Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S12Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S12Escherichia coli K-12
ribosome30S ribosomal protein S12Escherichia coli K-12
cytosol30S ribosomal protein S13Escherichia coli K-12
ribosome30S ribosomal protein S13Escherichia coli K-12
cytoplasm30S ribosomal protein S13Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S13Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S13Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S13Escherichia coli K-12
cytosol30S ribosomal protein S13Escherichia coli K-12
cytoplasm30S ribosomal protein S16Escherichia coli K-12
ribosome30S ribosomal protein S16Escherichia coli K-12
intracellular organelle30S ribosomal protein S16Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S16Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S16Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S16Escherichia coli K-12
cytosol30S ribosomal protein S18Escherichia coli K-12
ribosome30S ribosomal protein S18Escherichia coli K-12
cytoplasm30S ribosomal protein S18Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S18Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S18Escherichia coli K-12
cytoplasm30S ribosomal protein S19Escherichia coli K-12
cytosol30S ribosomal protein S19Escherichia coli K-12
ribosome30S ribosomal protein S19Escherichia coli K-12
intracellular organelle30S ribosomal protein S19Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S19Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S19Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S19Escherichia coli K-12
cytosol30S ribosomal protein S20Escherichia coli K-12
ribosome30S ribosomal protein S20Escherichia coli K-12
cytoplasm30S ribosomal protein S20Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S20Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S20Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S20Escherichia coli K-12
cytosol30S ribosomal protein S20Escherichia coli K-12
ribosome30S ribosomal protein S2Escherichia coli K-12
cytoplasm30S ribosomal protein S2Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S2Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S2Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S2Escherichia coli K-12
cytosol30S ribosomal protein S3Escherichia coli K-12
ribosome30S ribosomal protein S3Escherichia coli K-12
cytoplasm30S ribosomal protein S3Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S3Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S3Escherichia coli K-12
cytosol30S ribosomal protein S4Escherichia coli K-12
ribosome30S ribosomal protein S4Escherichia coli K-12
cytoplasm30S ribosomal protein S4Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S4Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S4Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S4Escherichia coli K-12
cytoplasm30S ribosomal protein S5Escherichia coli K-12
cytosol30S ribosomal protein S5Escherichia coli K-12
ribosome30S ribosomal protein S5Escherichia coli K-12
intracellular organelle30S ribosomal protein S5Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S5Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S5Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S5Escherichia coli K-12
cytoplasm30S ribosomal protein S8Escherichia coli K-12
cytosol30S ribosomal protein S8Escherichia coli K-12
ribosome30S ribosomal protein S8Escherichia coli K-12
intracellular organelle30S ribosomal protein S8Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S8Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S8Escherichia coli K-12
cytosol30S ribosomal protein S9Escherichia coli K-12
ribosome30S ribosomal protein S9Escherichia coli K-12
intracellular organelle30S ribosomal protein S9Escherichia coli K-12
cytoplasm30S ribosomal protein S9Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S9Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S9Escherichia coli K-12
cytoplasm50S ribosomal protein L13Escherichia coli K-12
cytosol50S ribosomal protein L13Escherichia coli K-12
ribosome50S ribosomal protein L13Escherichia coli K-12
intracellular organelle50S ribosomal protein L13Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L13Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L13Escherichia coli K-12
ribosome50S ribosomal protein L13Escherichia coli K-12
cytosol50S ribosomal protein L14Escherichia coli K-12
ribosome50S ribosomal protein L14Escherichia coli K-12
cytoplasm50S ribosomal protein L14Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L14Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L14Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L14Escherichia coli K-12
ribosome50S ribosomal protein L16Escherichia coli K-12
cytoplasm50S ribosomal protein L16Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L16Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L16Escherichia coli K-12
ribosome50S ribosomal protein L23Escherichia coli K-12
cytoplasm50S ribosomal protein L23Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L23Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L23Escherichia coli K-12
cytoplasm30S ribosomal protein S15Escherichia coli K-12
cytosol30S ribosomal protein S15Escherichia coli K-12
ribosome30S ribosomal protein S15Escherichia coli K-12
intracellular organelle30S ribosomal protein S15Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S15Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S15Escherichia coli K-12
chromosomeDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
cytosolDNA gyrase subunit AEscherichia coli K-12
membraneDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit AEscherichia coli K-12
chromosomeDNA gyrase subunit BEscherichia coli K-12
cytoplasmDNA gyrase subunit BEscherichia coli K-12
cytosolDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit BEscherichia coli K-12
cytosol50S ribosomal protein L17Escherichia coli K-12
ribosome50S ribosomal protein L17Escherichia coli K-12
cytoplasm50S ribosomal protein L17Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L17Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L17Escherichia coli K-12
cytoplasm50S ribosomal protein L21Escherichia coli K-12
cytosol50S ribosomal protein L21Escherichia coli K-12
ribosome50S ribosomal protein L21Escherichia coli K-12
intracellular organelle50S ribosomal protein L21Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L21Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L21Escherichia coli K-12
ribosome50S ribosomal protein L30Escherichia coli K-12
cytoplasm50S ribosomal protein L30Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L30Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L30Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L30Escherichia coli K-12
cytosol50S ribosomal protein L6Escherichia coli K-12
ribosome50S ribosomal protein L6Escherichia coli K-12
cytoplasm50S ribosomal protein L6Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L6Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L6Escherichia coli K-12
cytoplasm30S ribosomal protein S14Escherichia coli K-12
ribosome30S ribosomal protein S14Escherichia coli K-12
intracellular organelle30S ribosomal protein S14Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S14Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S14Escherichia coli K-12
small ribosomal subunit30S ribosomal protein S14Escherichia coli K-12
ribosome30S ribosomal protein S17Escherichia coli K-12
cytoplasm30S ribosomal protein S17Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S17Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S17Escherichia coli K-12
cytoplasm30S ribosomal protein S1Escherichia coli K-12
ribosome30S ribosomal protein S1Escherichia coli K-12
membrane30S ribosomal protein S1Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S1Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S1Escherichia coli K-12
cytoplasm50S ribosomal protein L18Escherichia coli K-12
cytosol50S ribosomal protein L18Escherichia coli K-12
ribosome50S ribosomal protein L18Escherichia coli K-12
intracellular organelle50S ribosomal protein L18Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L18Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L18Escherichia coli K-12
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
nucleolusSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
mitochondrionSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
mitochondrial inner membraneSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
mitochondrial respiratory chain complex II, succinate dehydrogenase complex (ubiquinone)Succinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
mitochondrial matrixSuccinate dehydrogenase [ubiquinone] flavoprotein subunit, mitochondrialHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
cytosol50S ribosomal protein L2Escherichia coli K-12
ribosome50S ribosomal protein L2Escherichia coli K-12
cytoplasm50S ribosomal protein L2Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L2Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L2Escherichia coli K-12
DnaA-L2 complex50S ribosomal protein L2Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L2Escherichia coli K-12
cytosol50S ribosomal protein L3Escherichia coli K-12
ribosome50S ribosomal protein L3Escherichia coli K-12
cytoplasm50S ribosomal protein L3Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L3Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L3Escherichia coli K-12
cytosol50S ribosomal protein L24Escherichia coli K-12
ribosome50S ribosomal protein L24Escherichia coli K-12
cytoplasm50S ribosomal protein L24Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L24Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L24Escherichia coli K-12
cytosol50S ribosomal protein L4Escherichia coli K-12
ribosome50S ribosomal protein L4Escherichia coli K-12
cytoplasm50S ribosomal protein L4Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L4Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L4Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L4Escherichia coli K-12
cytosol50S ribosomal protein L22Escherichia coli K-12
ribosome50S ribosomal protein L22Escherichia coli K-12
cytoplasm50S ribosomal protein L22Escherichia coli K-12
large ribosomal subunit50S ribosomal protein L22Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L22Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L22Escherichia coli K-12
cytosol50S ribosomal protein L5Escherichia coli K-12
ribosome50S ribosomal protein L5Escherichia coli K-12
cytoplasm50S ribosomal protein L5Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L5Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L5Escherichia coli K-12
cytosol30S ribosomal protein S21Escherichia coli K-12
ribosome30S ribosomal protein S21Escherichia coli K-12
cytoplasm30S ribosomal protein S21Escherichia coli K-12
cytosolic small ribosomal subunit30S ribosomal protein S21Escherichia coli K-12
ribonucleoprotein complex30S ribosomal protein S21Escherichia coli K-12
cytosol50S ribosomal protein L25Escherichia coli K-12
ribosome50S ribosomal protein L25Escherichia coli K-12
cytoplasm50S ribosomal protein L25Escherichia coli K-12
cytosolic large ribosomal subunit50S ribosomal protein L25Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L25Escherichia coli K-12
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
ribosome50S ribosomal protein L36 2Escherichia coli K-12
cytosolic ribosome50S ribosomal protein L36 2Escherichia coli K-12
ribonucleoprotein complex50S ribosomal protein L36 2Escherichia coli K-12
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5731)

Assay IDTitleYearJournalArticle
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID535021Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-18 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1692904Antibacterial activity against vancomycin-resistant Enterococcus faecium2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID406621Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.
AID548473Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega expressing vraSn mutant gene after 48 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID285132Antimicrobial activity against viridans group Streptococcus sanguinis at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID523796Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID308919Antibacterial activity against multidrug resistant Enterococcus faecalis ATCC 700802 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID516167Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolates assessed as resistant isolates by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID429417Antibacterial activity against Staphylococcus aureus ATCC 25923 by agar dilution method in presence of human plasma2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID531561Antibacterial activity against coagulase-negative Staphylococcus sciuri obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID523778Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1167993Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 7079 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID582991Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS08369 harboring MLST sequence type ST18 and pulsotype G expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1852684Antibacterial activity against wild type Pseudomonas aeruginosa assessed as inhibition of bacterial growth
AID369446Antimicrobial activity against Streptococcus group A after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID561245Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID523046Antimicrobial activity against Moraxella catarrhalis by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID571990Antibacterial activity against Ruminococcus torques by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1649290Antibacterial activity against Vancomycin-resistant Enterococcus faecium SRM1101 (c_VanB) assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID520521Oral bioavailability in osteomylitic patient2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID558532Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1265136Inhibition of human recombinant MAO-B using p-tyramine as substrate at 50 to 200 uM measured up to 50 mins by ELISA screening analysis2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID564811Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus haemolyticus assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID285138Antimicrobial activity against viridans group Streptococcus vestibularis at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID523040Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID542919Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing at 800 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID576132Antibacterial activity against 10'4 to 10'5 CFU Haemophilus influenzae after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID244888Minimal inhibitory concentration against Escherichia coli ATCC 259222004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID520025Antimicrobial activity against Enterococcus faecalis A77892008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1680007Induction of outer membrane permeabilization in Escherichia coli ATCC 25922 at 20 ug/ml measured for 12 mins by NPN dye based fluorescence assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID531579Antibacterial activity against Micrococcus spp. obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID284977Antimicrobial activity against Corynebacterium striatum at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1304851Ratio of MIC for methicillin-resistant Staphylococcus aureus clinical isolate 2 in absence and presence of Cu2+2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1390481Antibacterial activity against vancomycin-resistant Enterococcus faecium 03080 DS2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1904916Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS 123 (USA400) incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID576873Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusio2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID283160Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2554 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID289866Antibacterial activity against Enterococcus faecalis ATCC 292122007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
AID576140Antibacterial activity against 10'4 to 10'5 CFU methicillin-susceptible coagulase-negative Staphylococcus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1168018Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 147969 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID519139Antimicrobial activity against community-acquired methicillin resistant Staphylococcus aureus expressing PVL gene and mec type IV gene assessed as susceptible strains by broth microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activities of Ceftaroline and ME1036 tested against clinical strains of community-acquired methicillin-resistant Staphylococcus aureus.
AID267722Antimicrobial activity against Enterococcus faecium UC127122006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings.
AID285376Bactericidal activity against heteroresistant vancomycin-intermediate Staphylococcus aureus Mu3 assessed as reduction of CFU using in vitro PK/PD model with human dosage regimen 600 mg every 12 hrs after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID369675Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 6.25 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1698704Antibacterial activity against Vancomycin-resistant Enterococcus by CLSI method2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors.
AID283639Antimicrobial activity against Staphylococcus aureus ST/02/2121 with 23S rRNA T2504C mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID566569Antimicrobial activity against Bacillus subtilis PTCC 1023 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID571799Antibacterial activity against Clostridium bifermentans by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID583881Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-3 harboring ribosomal protein L3 deltaPhe127-His146 mutant and cfr-containing p42262 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID318352Antibacterial activity against Staphylococcus aureus in presence of serum2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID1778647Antibacterial activity against vancomycin-susceptible Enterococcus faecalis ATCC 29212 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID439889Antibacterial activity against Staphylococcus epidermidis ATCC 12229 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID369441Antibacterial activity against vancomycin-susceptible Enterococcus faecium after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID1770355Bactericidal activity against penicillin-susceptible Bacillus pumilus CMCC63202 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID571803Antibacterial activity against Clostridium glycolicum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1327122Antitubercular activity against dormant stage Mycobacterium bovis BCG ATCC 35734 at 3 ug/ml measured after 12 days by nitrate reductase assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID573143Antibacterial activity against penicillin-susceptible Streptococcus viridans by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID575050AUC (12 hrs) in liver transplant patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID68244In vitro antibacterial activity against vancomycin-resistant Enterococcus faecium C6487 (VRE).1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1312945Bactericidal activity against methicillin-sensitive Staphylococcus aureus NRS72 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID373310Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID575269Antimicrobial activity against vancomycin-susceptible Enterococcus faecium by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID1139109Antimicrobial activity against Staphylococcus aureus in rat thigh assessed as log reduction of CFU at 3 mg/kg, iv after 8 hrs2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID458460Antimicrobial activity against Mycobacterium vaccae IMET 10670 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID533984Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus NRS384 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID585161Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA A2503G mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID561340Antibacterial activity against Methicillin-sensitive Staphylococcus aureus by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1308231Antibacterial activity against Streptococcus oralis ATCC 9811 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID1680054Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 2 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID373995Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 48 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID573868Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in po dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1151777Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0605 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 10 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1400754Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 16 to 18 hrs by broth microdilution method2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID1832945Antibacterial activity against Vanomycin-resistant Enterococcus faecium NCTC 12204 assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID572012Antibacterial activity against Prevotella buccae by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID523039Antimicrobial activity against Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID562251Antibacterial activity against methicillin-resistant Staphylococcus aureus isolated form patient blood measured after 18 to 24 hrs on day 1 post isolation by Etest2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation between vancomycin MIC values and those of other agents against gram-positive bacteria among patients with bloodstream infections caused by methicillin-resistant Staphylococcus aureus.
AID576643Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusi2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID561266Antibacterial activity against Enterococcus faecium assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID304010Antibacterial activity against methicillin-resistant Staphylococcus aureus C203 in po dosed CD1 mouse systemic infection model assessed as mortality after 7 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID609062Antibacterial activity against Staphylococcus aureus ATCC 9144 at 1 mg/ml after 24 hrs by agar-well diffusion technique2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID559784Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID729178Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in po dosed systemic infection mouse model administered 1 hr post infection measured after 48 hrs2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID576417Volume of distribution at steady state in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1596545Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID255572In vitro minimum inhibitory concentration against Staphylococcus aureus ATCC 25923 after incubation in air at 35 degree C for 24 hr using agar dilution method2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID1539456Antibacterial activity against cephalosporin-resistant Streptococcus pneumoniae ATCC 51916 clinical isolates after 18 to 20 hrs by CLSI-based broth microdilution assay
AID555307Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 057 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID562395Antimicrobial activity against Staphylococcus epidermidis clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID730748Antibacterial activity against macrolides, lincosamides, streptogramin B and methicillin-resistant Staphylococcus epidermidis 1105-00 assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID373997Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1390485Antibacterial activity against vancomycin-resistant Enterococcus faecium 1342018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID562386Antimicrobial activity against Enterococcus faecalis expressing VanA gene clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID548255Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega expressing vraSn mutant gene after 24 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID576866Bactericidal activity against 2 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID531571Antibacterial activity against Streptococcus constellatus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID249176Protective dose against Staphylococcus aureus in mice after 8 days of oral b.i.d. administration at 1 and 5 h per interval with water as vehicle (n=10); range is 5-6 mg/kg/day2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Biaryl isoxazolinone antibacterial agents.
AID534791Bactericidal activity against vancomycin-resistant Staphylococcus aureus assessed as antibiotic concentration that reduced the number of viable cells by =>99.9% by colony count method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID571994Antibacterial activity against Finegoldia magna by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1400034Bactericidal activity against replicating Mycobacterium tuberculosis H37Rv incubated for 15 days under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID524723Antibacterial activity against linezolid-resistant Enterococcus faecium 03B1077 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID695443Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 2-FQR2M NY2746 expressing GyrA Ser84Leu mutant and GrlA Ser80Phe mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID475000Antibacterial activity against Enterococcus faecalis LCB0005 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID477372Antibacterial activity against fmethicillin and vancomycin-resistant Staphylococcus aureus ATCC 29213 after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID511384Antibacterial activity against Enterococcus faecium by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID524958Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus haemolyticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1197132Antibacterial activity against Enterococcus faecium NCTC 7171 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1504622Antibacterial activity against Enterococcus faecium 19434 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID1862431Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1663) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID524974Antibacterial activity against Streptococcus sp. Group C clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID533417Antimicrobial activity against Micromonas micros by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID520021Antimicrobial activity against Enterococcus faecalis ATCC 29212-P5 harboring G2576U mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID523037Antimicrobial activity against vancomycin-susceptible Enterococcus faecium by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID1400752Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 after 16 to 18 hrs by broth microdilution method2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID278569Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 292132007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
AID522902Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1003 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID576863Bactericidal activity against 48 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID575270Antimicrobial activity against vancomycin-resistant Enterococcus faecium by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID1374170Antibacterial activity against Staphylococcus aureus ATCC 33591 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID1687307Antimicrobial activity against Escherichia coli JW55031 TolC mutant assessed as reduction in microbial growth incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1852692Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs by twofold serial dilution method
AID207793Compound was evaluated for minimum inhibitory concentration against Staphylococcus aureus 9616 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID1578431Antimicrobial activity against Listeria monocytogenes ATCC 19111 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID285077Antimicrobial activity against viridans group Streptococcus bovis at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID581041Inhibition of mammalian ribosomal activity by coupled transcription/translation assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID524969Antibacterial activity against vancomycin-susceptible Enterococcus faecium clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1421220Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID285150Antimicrobial activity against viridans group Streptococcus oralis at by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID555310Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 225 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID278861Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID566572Antimicrobial activity against Klebsiella pneumoniae ATCC 10031 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID30153Volume distribution in Male Sprague-Dawley Rat (10 mg/kg iv)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID499161Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 1.6 mg/kg/day, po (Rvb = 1.6 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID763952Antibacterial activity against Moraxella catarrhalis clinical isolate 125 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1895487Antibacterial activity against methicillin resistant Staphylococcus aureus incubated for 24 hrs by broth microdilution method2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthetic access to thiolane-based therapeutics and biological activity studies.
AID671561Antibacterial activity against methicillin-resistant Staphylococcus aureus VL-1372012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID1519049Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID520233Antimicrobial activity against Haemophilus influenzae 54A11002008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID548526Antimicrobial activity against Oxacillin-resistant Staphylococcus aureus by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID1852678Antibacterial activity against recombinant OM pore producing Acinetobacter baumannii assessed as inhibition of bacterial growth
AID285122Antimicrobial activity against viridans group Streptococcus parasanguis at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID131894Effective dose required to inhibit Staphylococcus aureus UC9213 in mice subjected to a lethal systemic infection (when administered orally)1998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID304004Effect on hematology in Sprague-Dawley rat assessed as decrease in red blood cells at 200 mg/kg/day, po after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID559554Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP5 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID531565Antibacterial activity against Enterococcus faecalis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID285313Antimicrobial activity against Pediococcus spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID1312944Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID1378018Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID1390470Antibacterial activity against linezolid-resistant Staphylococcus aureus ATCC 13709 SMITH2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID278856Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID523041Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID1151774Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 40 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID523042Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID245560In vitro minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus (ST450, ATCC 15187, ICH 1 and 37)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID285032Antimicrobial activity against Rothia mucilaginosa at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1126485Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus ATCC 259232014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID565004Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1126484Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 137092014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID1390479Antibacterial activity against Enterococcus faecium ATCC 194342018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1680065Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 1 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID561085Antibacterial activity against penicillin-resistant Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID524959Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus hominis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1778657Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51559 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID562234Antibacterial activity against methicillin-resistant Staphylococcus aureus OC2878 assessed as log reduction in bacterial count at 8 times MIC after 24 hrs by time kill study2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID1151628Toxicity in female rat assessed as effect on neutrophil count at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 22.4%)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID519092Antimicrobial activity against Staphylococcus aureus KM187+198 harboring G2576U mutation in 23S rRNA by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID285063Antimicrobial activity against beta hemolytic Streptococci group F at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID326529Antibacterial activity against vancomycin-resistant Enterococcus faecalis UCN41 challenged with 10 times ID90 bacterial size inoculum in Wistar rat assessed as infection at single administration of 600 mg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID396031Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pACYC184 plasmid by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID244816Minimum inhibitory concentration Moraxella catarrhalis2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID244864Minimum inhibitory concentration against Escherichia coli UC66742005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID1879691Antimycobacterial activity against extensively drug resistant Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method2022European journal of medicinal chemistry, Mar-15, Volume: 232Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
AID1117384Antimicrobial activity against Micrococcus luteus ATCC 10240 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID353062Antibacterial activity against vancomycin-resistant Enterococcus 5 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID576405Mean residence time in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1304828Antibiofilm activity against methicillin-resistant Staphylococcus aureus BAA-1707 assessed as biofilm eradication incubated for 24 hrs by CBD assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID383558Antibacterial activity against Staphylococcus epidermidis ATCC 155 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID558517Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1327097Antibacterial activity against Pseudomonas aeruginosa NCIM 2036 measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1778124Antitubercular activity against linezolid resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth incubated for 7 days by MABA
AID261063Antibacterial activity against Enterococcus faecalis MGH-2 EF1-12006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
AID541519Antimicrobial activity against methicillin-susceptible Staphylococcus aureus clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID285135Antimicrobial activity against viridans group Streptococcus sanguinis at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID565011Bactericidal activity against methicillin-susceptible coagulase-negative Staphylococcus haemolyticus after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID583407Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate PA assessed as bacterial count at 4 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1553387Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 43300 measured after 16 hrs by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1504621Antibacterial activity against Enterococcus faecalis ATCC 29212 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID533401Antimicrobial activity against Clostridium subterminale by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID573113Antibacterial activity against methicillin-susceptible Staphylococcus aureus by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1904082Antibacterial activity against Pseudomonas aeruginosa HER 10182022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID558730Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 50 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID576135Antibacterial activity against 10'4 to 10'5 CFU Enterococcus faecium after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID571931Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB-S623N mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID560511Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b5k3578 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID572000Antibacterial activity against Streptococcus intermedius by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID285375Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as reduction of CFU using in vitro PK/PD model with human dosage regimen 600 mg every 12 hrs after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID548474Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega expressing vraSm mutant gene after 48 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID206609In vitro antibacterial activity against methicillin-resistant Staphylococcus aureus 241 (MRSA)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID311479Antimicrobial activity against penicillin-sensitive Streptococcus pneumoniae ATCC 49619 after 14 to 16 hrs by serial microbroth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID531559Antibacterial activity against coagulase-negative Staphylococcus saprophyticus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID353063Antibacterial activity against vancomycin-resistant Enterococcus 6 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID373317Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID574950Antimicrobial activity against Streptococcus pneumoniae serotype 35B by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID428277Antituberculosis activity against linezolid-resistant Mycobacterium tuberculosis by bactec 460 TB method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID523033Antimicrobial activity against Enterococcus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID1151729Antibacterial activity against Streptococcus mitis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1151775Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 80 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1778102Antibacterial activity against Enterococcus faecium ATCC 49624 assessed as bacterial growth inhibition after 18 hrs by broth microdilution method
AID555295Antibacterial activity against Tmp-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1117382Antimicrobial activity against vancomycin-resistant Enterococcus faecalis 1528 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1504620Antibacterial activity against linezolid-resistant Staphylococcus aureus by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID559556Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP6 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID645036Antibacterial activity against erythromycin-sensitive Streptococcus pyogenes 3 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID576420Cmax in healthy human at 600 mg, iv, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1852671Antibacterial activity against multidrug resistant Pseudomonas aeruginosa BAA 2108 assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID206222In vitro antibacterial activity against Staphylococcus epidermis (S.e.1) ATCC 1228.1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1412975Antibacterial activity against methicillin-sensitive Staphylococcus aureus after 16 hrs by agar dilution method2018MedChemComm, May-01, Volume: 9, Issue:5
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
AID533022Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-3 assessed as inhibition of bacterial growth in brain heart infusion broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID125114In vitro minimum inhibitory concentration (MIC) against Moraxella catarrhalis UC306102003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID285516Antibacterial activity against Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID572272Antimicrobial activity against Streptococcus pneumoniae ATCC 6301 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID1308233Antibacterial activity against Bacillus cereus ATCC 13061 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID319168Inhibition of monoamine oxidase A2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID544820Antimicrobial activity against Staphylococcus epidermidis Xen 43 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID565749Antimicrobial activity against Enterococcus faecalis expressing VanA gene clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1428626Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 by broth microdilution method2017European journal of medicinal chemistry, Feb-15, Volume: 127Diaryltriazenes as antibacterial agents against methicillin resistant Staphylococcus aureus (MRSA) and Mycobacterium smegmatis.
AID424760Antibacterial activity against macrolide, methicillin-resistant Staphylococcus aureus CL5705 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID1414206Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as reduction in viable bacterial count at 8 ug/ml after 24 hrs by time-kill assay2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID206607In vitro antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID263968Efficacy against po dosed mouse infected with Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID520228Antimicrobial activity against methicillin-resistant Staphylococcus aureus BK 111182008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID285142Antimicrobial activity against beta hemolytic Streptococcus group F by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID524960Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus saprophyticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID523026Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523045Antimicrobial activity against Listeria monocytogenes by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID520015Antimicrobial activity against Staphylococcus hominis A78282008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1578410Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID268865Antibacterial activity against vancomycin-resistant Enterococcus faecalis NCTC 122012006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis of novel tricyclic oxazolidinones by a tandem SN2 and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid.
AID528737Antibacterial activity against methicillin resistant Staphylococcus epidermidis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID552857Antibacterial activity against Enterococcus faecium infected in po dosed in vivo acute model administered bid for 1 day2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID726197Antibacterial activity against vancomycin-resistant Enterococcus faecium C803 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID1710582Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS483 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1609262Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID575264Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID541042Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 75 mg/kg measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID285507Antibacterial activity against methicillin-resistant Staphylococcus aureus after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID533966Bacteriostatic activity against Legionella pneumophila ATCC 33153 infected in THP1 cells after 48hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID244933Minimal inhibitory concentration against Staphylococcus aureus ATCC 259232004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID572007Antibacterial activity against Bacteroides splanchnicus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID285518Antibacterial activity against Streptococcus pyogenes2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID29723Tmax value in Male Sprague-Dawley Rat at dose 25 (mg/kg po) [tmax (h)]2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID729217Antibacterial activity against linezolid-resistant Staphylococcus epidermidis after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID1167988Antibacterial activity against vancomycin-resistant Enterococcus ATCC 29212 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID326509Tmax in Enterococcus faecalis infected Wistar rat at single administration of 600 mg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID541784Antimicrobial activity against Streptococcus pyogenes clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1861537Clearance in Wistar rat at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID558702Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID522822Antibacterial activity against vancomycin-hetero-intermediate Staphylococcus aureus after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1421230Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolates by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID575268Antimicrobial activity against vancomycin-resistant Enterococcus faecalis by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID270147Antibacterial activity against gram positive vancomycin-susceptible Enterococcus faecalis ATCC 292122006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.
AID1721058Toxicity in Mycobacterium tuberculosis H37Rv infected Balb/c mouse assessed as change in body weight at 100 mg/kg/day, po administered via gavage 5 times per week for 3 weeks starting from 10 days post-infection (Rvb = 21.29 +/- 0.84 g)2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1770345Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC43300 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID534250Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells at pH 7.4 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID559772Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID511393Antibacterial activity against Levofloxacin resistant Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID548257Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega expressing vraSm, graRm mutant gene after 24 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID572019Antibacterial activity against Prevotella loescheii by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID523035Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID528732Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus saprophyticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1197124Antibacterial activity against Streptococcus pyogenes ATCC 49399 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1873947Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 25% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID545602Bacteriostatic activity against stationary-phase methicillin-resistant Staphylococcus aureus ATCC 33591 grown on nutrient-depleted CAMHB medium at 8 ug/ml after 24 hrs by time kill analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID85956Antibacterial activity against Haemophilus influenzae UC30063 (Haemophilus influenzae)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID278572Antimicrobial activity against Streptococcus pyogenes ATCC 196152007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
AID245045Minimal inhibitory concentration against Enterococcus faecalis (VRE) ATCC 346-VRE2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID535256Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-4 expressing SCCmec type 4 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID576125Antibacterial activity against 1 x 10'8 CFU methicillin-resistant Staphylococcus aureus p125 infected in ICR mouse systemic infection model assessed as mouse protection administered orally twice after 1 and 4 hrs post infection measured after 48 hrs2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1873914Antibacterial activity against Pseudomonas aeruginosa LTP-3 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID577119Cmax in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID717212Antimicrobial activity against methicillin-resistant Staphylococcus aureus CCARM 3089 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1304853Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 incubated for 16 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID83804In vitro minimum inhibitory concentration (MIC) against Haemophilus influenzae UC300632003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID311478Antimicrobial activity against Staphylococcus epidermidis ATCC 700582 after 14 to 16 hrs by serial microbroth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID125242The compound was evaluated for its anti-bacterial activity against Moraxella catarrhalis UC 306101998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID530121Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus 152 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID730746Antibacterial activity against methicillin-resistant Staphylococcus aureus 2111-10-USA300 harboring cfr gene assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID524692Antibacterial activity against Listeria monocytogenes clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID571833Antibacterial activity against Ruminococcus flavefaciens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1514450Antitubercular activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID560522Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gz07030 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID571811Antibacterial activity against Clostridium sporogenes by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1168003Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 7/27 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID565016Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus sciuri after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID533969Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS384 infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID640890Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar microdilution method2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID561094Antibacterial activity against Clostridium perfringens by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID523034Antimicrobial activity against vancomycin-resistant Enterococcus faecalis by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID535032Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-76 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID531568Antibacterial activity against Streptococcus pyogenes obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1327119Antitubercular activity against dormant stage Mycobacterium tuberculosis H37Ra at 3 ug/ml measured after 12 days by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID285328Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 512992007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro activity of aurein 1.2 alone and in combination with antibiotics against gram-positive nosocomial cocci.
AID559282Antimicrobial activity against Enterococcus faecalis JH2-2 harboring nucleotides at position 2576 in rrlA 2576T, rrlB 2576G, rrlC 2576G/T and rrlD 2576T after 6, 8 passages under Linezolid selective pressure by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID542713fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID285152Antimicrobial activity against viridans group Streptococcus salivarius by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID574080Ratio of fAUC (24 hrs) for Methicillin-susceptible Staphylococcus aureus ATCC 13709 infected iv dosed mouse to MIC for Methicillin-susceptible Staphylococcus aureus ATCC 13702009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID283628Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4536-0368 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID561078Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1117369Antimicrobial activity against Bacillus subtilis ATCC 6633 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1609269Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID533638Antimicrobial activity against Propionibacterium sp. assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1703716Antibacterial activity against methicillin-resistant Staphylococcus aureus USA700 NRS386 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID575267Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID573149Antibacterial activity against vancomycin-susceptible Enterococcus faecalis by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID207421In vitro antibacterial activity against Staphylococcus aureus ATCC 29213 (S. a. 035)2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID534256Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA238L infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID562177Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 50 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID319156Toxicity in dog at 40 mg/kg, po for 30 days2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID571992Antibacterial activity against Anaerococcus prevotii by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1688277In vivo antibacterial activity against methicillin resistant Staphylococcus aureus clinical isolate 15-1 infected in kunming mouse assessed as animal survival rate at 9 mg/kg, po administered 6 hrs prior to bacterial infection and at 0 and 6 hrs post infe2020European journal of medicinal chemistry, Feb-15, Volume: 188N-thiadiazole-4-hydroxy-2-quinolone-3-carboxamides bearing heteroaromatic rings as novel antibacterial agents: Design, synthesis, biological evaluation and target identification.
AID562162Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1832943Antibacterial activity against Vanomycin-sensitive Enterococcus faecalis NCTC 775 assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID561246Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID562617Antimicrobial activity against methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID284899Antimicrobial activity against heterogeneous glycopeptide-intermediate Staphylococcus aureus by broth microdilution technique after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antimicrobial activities of ceragenins against clinical isolates of resistant Staphylococcus aureus.
AID1350028Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 11 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID671565Antibacterial activity against Moraxella catarrhalis2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID127506Antibacterial activity against Moraxella catarrhalis (MC1002)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID91253Compound was evaluated for metabolic stability via In vitro Human 5E6 cell at 25 uM concentration; ND denotes not determined2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID1877884Antibacterial activity against methicillin-resistant Staphylococcus aureus N315 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID523782Antimicrobial activity against linezolid-resistant Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID532789Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR1 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID576878Bactericidal activity against 13 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1375999Inhibition of Mycobacterium tuberculosis H37Rv cytochrome bc1 oxidase assessed as reduction in ATP level measured up to 24 hrs under anaerobic condition2016MedChemComm, Nov-01, Volume: 7, Issue:11
SAR and identification of 2-(quinolin-4-yloxy)acetamides as
AID1547715Antibacterial activity against Enterococcus faecalis ATCC 29212 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID285349Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20030203 in CCY media2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID370033Antibacterial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus infected in po dosed C3H mouse localized infection model assessed as reduction of number of CFU per gram of thigh administered 2 hrs postinfection thrice daily 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID523043Antimicrobial activity against Streptococcus viridans by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID1197125Antibacterial activity against Bacillus cereus ATCC 13061 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1493811Antibacterial activity against Enterobacter cloacae BAA-1154 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1553369Inhibition of protein synthesis in mitochondria (unknown origin) assessed as [35S]methionine incorporation incubated for 15 to 120 mins by paper disk assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1687317Synergistic antibacterial activity against Pseudomonas aeruginosa ATCC 15442 in presence of 0.25 times MIC of colistin incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1311365Antibacterial activity against Enterococcus faecalis ATCC 19433 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID574551Decrease in delta toxin levels in Staphylococcus aureus Sanger 252 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID533956Antimicrobial activity against Staphylococcus epidermidis infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1151766Antibacterial activity against penicillin-resistant Streptococcus pneumoniae isolate 0613 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1689208Antibacterial activity against Clostridium difficile BAA1870 assessed as reduction in bacterial growth by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID576676Bactericidal activity against 1 hr peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1647978Antibacterial activity against Staphylococcus aureus ATCC 29213 by resazurin dye based microdilution method2020Journal of natural products, 02-28, Volume: 83, Issue:2
The Isolation of Pyrroloformamide Congeners and Characterization of Their Biosynthetic Gene Cluster.
AID283623Antimicrobial activity against Enterococcus faecium 16 with homozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID563324Antibacterial activity against vancomycin-resistant Enterococcus faecalis EF NJ1 assessed as log reduction in bacterial count at 12 mg/l after 24 hrs by time kill assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID1409852Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.1 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 4.52018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID1501361Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 4 after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID303963Inhibition of human recombinant MAOA2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID532788Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR2 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1603257Antibacterial activity against INH-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay
AID323830Antibacterial activity against methicillin-resistant Staphylococcus aureus Xen1 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po after 4 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID533396Antimicrobial activity against Clostridium innocuum assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1167994Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 7846 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID759691Antibacterial activity against methicillin-resistant Staphylococcus aureus F511 assessed as growth inhibition after 18 to 24 hrs by broth microdilution method2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID270148Antibacterial activity against gram positive vancomycin-resistant Enterococcus faecium OC 33122006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.
AID12301Half life of compound (25 mg/kg) after po administration was determined in Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID207680Minimum inhibitory concentration (MIC) against Staphylococcus aureus OC 4172 in the absence of mouse serum2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID561076Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1591542Antibacterial activity against penicillin-resistant Staphylococcus aureus clinical isolate incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID564833Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus hominis after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID439888Antibacterial activity against Staphylococcus aureus ATCC 29737 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID562250Antibacterial activity against methicillin-resistant Staphylococcus aureus isolated form patient blood measured after 18 to 24 hrs on day 1 isolation by Etest2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation between vancomycin MIC values and those of other agents against gram-positive bacteria among patients with bloodstream infections caused by methicillin-resistant Staphylococcus aureus.
AID565483Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth microdilution method in presence of 50% human plasma2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID292671Antibacterial activity against Enterococcus faecalis by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1563585Inhibition of FabB/FabF in methicillin-sensitive Staphylococcus aureus assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID561752Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID697277Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus ARC 3189 after 18 to 24 hrs by CLSI broth microdilution method2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
AID1778093Antibacterial activity against Escherichia coli 25922 assessed as inhibition of bacterial growth incubated for 18 hrs by broth microdilution method
AID533959Antimicrobial activity against Staphylococcus aureus infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID571995Antibacterial activity against Peptoniphilus asaccharolyticus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID532783Antibacterial activity against vancomycin-susceptible Staphylococcus aureus MI after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID584994Antibacterial activity against Staphylococcus aureus XU21-T1 harboring cfr-encoding conjugative pSCFS7 and fexA by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate.
AID1703728Antibacterial activity against Listeria monocytogenes ATCC 19111 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID285379Bactericidal activity against vancomycin-intermediate Staphylococcus aureus Mu50 assessed as reduction of CFU using in vitro PK/PD model with human dosage regimen 120 mg every 12 hrs after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID523802Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1519263Inhibition of human MAO-A at 30 uM relative to control2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID374006Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 16 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID284953Antimicrobial activity against Bacillus cereus at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID528734Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus haemolyticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1539443Antibacterial activity against Methicillin-sensitive Staphylococcus aureus ATCC 6538 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID308912Antibacterial activity against Bacillus subtilis ATCC 6633 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID524954Antibacterial activity against methicillin-susceptible coagulase-negative unspeciated Staphylococcus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID562396Antimicrobial activity against oxacillin-resistant Staphylococcus aureus clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID285113Antimicrobial activity against viridans group Streptococcus oralis at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1710591Antibacterial activity against Listeria monocytogenes ATCC 19111 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1501359Antibacterial activity against methicillin-resistant Staphylococcus aureus USA200 NRS383 after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID283149Antimicrobial susceptibility of Staphylococcus lugdunensis isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1151746Antibacterial activity against Staphylococcus aureus measured after 8 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID373829Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 after 17 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection techniqu2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID560829Ratio of Cmax in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days to MIC for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID520489AUC in New Zealand rabbit at 20 mg/kg, sc administered every 6 hrs for 4 days measured after 1 hr post first dose by RP-HPLC/MS/MS2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID608940Antibacterial activity against Staphylococcus aureus ATCC 9144 after 24 hrs by broth microdilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID1677793Bacteriostatic activity against Staphylococcus aureus clinical isolate assessed as ratio of MBC to MIC2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID308487Antibacterial activity against Streptococcus pneumoniae SV1 SP32007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
AID535016Bactericidal activity against daptomycin-nonsusceptible Staphylococcus aureus assessed as antibiotic concentration that reduced the number of viable cells by =>99.9% by colony count method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID548524Antimicrobial activity against Oxacillin-resistant Staphylococcus aureus assessed as percent resistant isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID576677Bactericidal activity against 2 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID128015Compound was tested against Staphylococcus aureus UC9213 after po administration in mouse1998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID524687Antibacterial activity against vancomycin-susceptible Enterococcus faecium clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID671567Antibacterial activity against methicillin-resistant Staphylococcus aureus VL-137 infected in neutropenic Balb/c mouse assessed as reduction in lung CFU at 50 mg/kg, po administered 2 and 12 hrs post infection measured 24 hrs post treatment2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID525146Antimicrobial activity against Staphylococcus epidermidis isolate 426-3147L expressing cfr gene by Etest method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID775532Inhibition of CYP2C9 in human liver microsomes assessed as tolbutamide hydroxylation after 20 mins by LC/MS/MS analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID1680045Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 1 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1151728Antibacterial activity against Streptococcus equisimilis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID528720Antibacterial activity against vancomycin resistant Enterococcus faecalis VanB clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID564820Bactericidal activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID283399Antimicrobial activity against Nocardia brasiliensis after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID541096Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as cure rate at 75 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID583387Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate MU50 assessed as bacterial count at 4 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID319158Cmin in human at 625 mg, po bid after 14 days2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID561096Antibacterial activity against Peptostreptococcus micros by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1308224Antibacterial activity against mecA-positive multidrug resistant Staphylococcus aureus COL NRS100 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID523780Antimicrobial activity against oxacillin-resistant Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID753115Antibacterial activity against Micrococcus luteus MTCC 2470 assessed as growth inhibition at 20 mg/mL after 24 hrs2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID561084Antibacterial activity against penicillin-intermediate Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID498891Half life in immunocompetent SKH1 mouse plasma at 50 mg/kg, po2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID475002Antibacterial activity against vancomycin and Linezolid resistant Enterococcus faecalis LCB0007 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID541095Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as cure rate at 50 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1409847Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 3.5 days administered 6 hrs post bacterial infection measured 84 hrs post i2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID558480Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1151713Antibacterial activity against methicillin-resistant Staphylococcus epidermidis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID532810Antibacterial activity against vancomycin-susceptible Staphylococcus aureus BR4 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID571993Antibacterial activity against Anaerococcus tetradius by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID637969Antibacterial activity against Streptococcus pneumoniae expressing PenR gene after overnight incubation by twofold broth dilution technique in presence of 2.5% blood2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID390339Antimicrobial activity against Moraxella catarrhalis 5572008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID1390478Antibacterial activity against linezolid-resistant Enterococcus faecalis ATCC 292122018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1873913Antibacterial activity against Escherichia coli incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID573134Antibacterial activity against erythromycin-nonsusceptible Streptococcus pyogenes by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID561080Antibacterial activity against vancomycin-resistant Enterococcus faecalis by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID571800Antibacterial activity against Clostridium butyricum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID388045Antibacterial activity against Staphylococcus aureus EP167 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID456044Antibacterial activity against penicillin-intermediate resistant Streptococcus pneumoniae after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID523031Antimicrobial activity against vancomycin-nonsusceptible Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID467838Antibacterial activity against methicillin and vancomycin-resistant Staphylococcus aureus ATCC 29213 after 24 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
AID519995Antimicrobial activity against Streptococcus pneumoniae harboring erm(B) and mef(A) gene2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID562179Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 48 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID695448Cytotoxicity against human HeLa cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID558088Antimicrobial activity against Ureaplasma urealyticum isolated from human by two fold serial dilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
AID745373Inhibition of MAO-B in rat forebrain using [14C]PEA as substrate at 30 uM incubated for 20 mins prior to substrate addition measured after 10 mins by liquid scintillation counting analysis relative to control2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID223280Dose required to cure 50% of Staphylococcus aureus infected mice when administered orally; value ranges from 2.9-8.52000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID576651Bactericidal activity against 12 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1056338Inhibition of human CYP2C9 assessed as tolbutamide hydroxylation after 20 mins by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID571796Antibacterial activity against Clostridium subterminale by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID575274Antimicrobial activity against Streptococcus agalactiae by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID576412Total clearance in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID576900Ratio of AUC (0 to 24 hrs) to MIC for Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID575948Antimicrobial activity against erythromycin-resistant Streptococcus pneumoniae assessed as resistant isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.
AID368282AUC in rabbit plasma at 58 mg/kg infused every 12 hrs for 4 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID525144Antimicrobial activity against Staphylococcus epidermidis isolate 426-3147L expressing cfr gene by broth microdilution CLSI method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID562252Antibacterial activity against methicillin-resistant Staphylococcus aureus isolated form patient blood measured after 18 to 24 hrs on day 1 isolation stratified with vancomycin MIC < 1.5 mh/L by Etest2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Correlation between vancomycin MIC values and those of other agents against gram-positive bacteria among patients with bloodstream infections caused by methicillin-resistant Staphylococcus aureus.
AID671566Antibacterial activity against Acinetobacter baumannii2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID1904084Antibacterial activity against Acinetobacter baumannii 2208 ATCC 196062022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID245024In vitro minimum inhibitory concentration against Escherichia coli (ATCC 25922)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID283398Antimicrobial activity against Nocardia carnea after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID574951Antimicrobial activity against Streptococcus pneumoniae serotype 7F by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID373747Antimicrobial activity against mupirocin-susceptible methicillin-resistant Staphylococcus aureus by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID1151768Antibacterial activity against vancomycin-resistant Enterococcus faecalis isolate EFL 4041 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID576122Antibacterial activity against 7.5 x 10'8 CFU Haemophilus influenzae hd2 infected in ICR mouse systemic infection model assessed as mouse protection administered orally twice after 1 and 4 hrs post infection measured after 48 hrs2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID373748Antimicrobial activity against mupirocin-resistant methicillin-resistant Staphylococcus aureus by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID532786Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR4 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1151717Antibacterial activity against coagulase-negative Staphylococcus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID209475In vitro antibacterial activity against Streptococcus pyogenes strain UC 1521996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID533961Antimicrobial activity against Listeria monocytogenes infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1168016Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 27/221 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID561736Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as susceptible isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1472609In vivo anti-virulence activity against Staphylococcus aureus Newman infected in BALB/c mouse model assessed as reduction in bacterial load in heart at 0.4 mg bid for 4.5 days administered intraperitoneally 6 hrs post infection by serial dilution method2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID1862427Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1569) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID542893fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 200 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID574948Antimicrobial activity against Streptococcus pneumoniae serotype 19A by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID285043Antimicrobial activity against Corynebacterium striatum by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID571814Antibacterial activity against Clostridium sp. by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1861539Clearance in Beagle dog at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID285036Antimicrobial activity against Aerococcus spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID533963Bacteriostatic activity against Staphylococcus aureus infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID542695fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1591551Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as log reduction in viable bacterial count at 4 ug/ml incubated for 24 hrs by time-kill curve assay2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID297125Antibacterial activity against vancomycin-resistant Enterococcus faecalis NCTC-12201 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID524944Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus capitis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID528703Antibacterial activity against Streptococcus oralis clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID283388Effect on mitochondrial mass in PBMCs from patient during hyperlactemic phase by citrate synthase method relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reversible inhibition of mitochondrial protein synthesis during linezolid-related hyperlactatemia.
AID210352In vitro antibacterial activity against Streptococcus pneumoniae strains ATCC 6305 and 31573 (SPN).2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID1271203Solubility of compound at pH 1.2 by HPLC analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID523049Antimicrobial activity against beta-lactamase positive Haemophilus influenzae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID66578Antibacterial activity was determined against clinically isolated vancomycin-B resistant enterococci (VRE) strains (10 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1151723Bactericidal activity against penicillin intermediate-sensitive Streptococcus pneumoniae2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1367592Antibacterial activity against gram-negative wild type Escherichia coli MG1655 by CLSI broth microdilution method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID571805Antibacterial activity against Clostridium leptum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID520002Antimicrobial activity against Mycoplasma pneumoniae isolated from human respiratory tract by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1549094Antibacterial activity against Staphylococcus aureus ATCC 29213 measured after 16 to 20 hrs by microdilution method2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Exploration of the Structural Space in 4(3
AID524956Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus cohnii clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID591663Antimicrobial activity against multidrug-resistant Streptococcus pneumoniae after 18 hrs by agar dilution method2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
AID1770342Antibacterial activity against erythromycin-susceptible Streptococcus pyogenes assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID573886Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in po dosed CF-1 mouse administered at 24 hrs post infection measured after 48 hrs relative to Linezolid2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID520017Antimicrobial activity against Staphylococcus capitis A89352008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID112686In vivo antibacterial activity against Staphylococcus aures strain UC 9213 administered subcutaneously in mice1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID369435Antimicrobial activity against methicillin-susceptible Staphylococcus aureus after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID1647976Cytotoxicity against human A549 cells by CCK8 assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
The Isolation of Pyrroloformamide Congeners and Characterization of Their Biosynthetic Gene Cluster.
AID565750Antimicrobial activity against vancomycin-nonsusceptible Enterococcus faecalis clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1553379Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by CellTiter-Glo assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1243930Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA700 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1327111Antibacterial activity against Staphylococcus aureus NCIM 2079 at 30 ug/ml measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID285055Antimicrobial activity against beta hemolytic Streptococcus group C at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID525134Antibacterial activity against Staphylococcus aureus KM51 after 18 to 24 hrs by broth microdilution method selected after 16 ug/ml drug exposure for 6 hrs by culture absorbance method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID1395981Bactericidal activity against methicillin-resistant Staphylococcus aureus 2 planktonic cells after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID524718Antibacterial activity against linezolid-resistant Staphylococcus aureus 01A1220 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID572006Antibacterial activity against Bacteroides vulgatus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID558470Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID576426Antibacterial activity against Staphylococcus aureus RN4220 MutS2 by agar dilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID582988Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS07261 harboring MLST sequence type ST78 and pulsotype D expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1591545Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID572017Antibacterial activity against Prevotella intermedia by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1361113Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRS12 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID522934Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 510 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1308226Antibacterial activity against mecA-positive multidrug resistant Staphylococcus aureus NRS120 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID533949Antimicrobial activity against methicillin-resistant, vancomycin intermediate Staphylococcus aureus NRS18 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID532803Antibacterial activity against vancomycin-susceptible Staphylococcus aureus 99/3759-V after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID285325Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 292132007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro activity of aurein 1.2 alone and in combination with antibiotics against gram-positive nosocomial cocci.
AID573123Antibacterial activity against coagulase-negative and oxacillin-resistant Staphylococcus aureus assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1852672Antibacterial activity against multidrug resistant Acinetobacter baumannii Ab5075 assessed as inhibition of bacterial growth incubated for 24 hrs in M9-MOPS medium by twofold serial dilution method
AID1350031Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 2 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID295155Antibacterial activity against methicillin-resistant Staphylococcus aureus by microdilution broth method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID576134Antibacterial activity against 10'4 to 10'5 CFU vancomycin-resistant Enterococcus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID645046Antibacterial activity against Escherichia coli 3350 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID1723492Antibacterial activity against Enterococcus faecium NR-28978 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID571834Antibacterial activity against Ruminococcus luti by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID206146In vitro antibacterial activity against S. a. 035 (Staphylococcus aureus ATCC 29213)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Influence of ethylene-oxy spacer group on the activity of linezolid: synthesis of potent antibacterials possessing a thiocarbonyl group.
AID571795Antibacterial activity against Clostridium ramosum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1272264Antimicrobial activity against methicillin-resistant Staphylococcus aureus MMX 2002 after 18 to 20 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.
AID373841Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 Michigan after 28 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID577103AUBC (0 to 24 hrs) in Staphylococcus aureus RN4220MutS2 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID562630Antimicrobial activity against Group G Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID528968Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID562619Antimicrobial activity against Heterovancomycin-resistant Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID571827Antibacterial activity against Eggerthella lenta by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID533989Bacteriostatic activity against linezolid-resistant Staphylococcus aureus SA238L infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1374172Antibacterial activity against Streptococcus pyogenes ATCC 19615 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID1703720Antibacterial activity against vancomycin-resistant Staphylococcus aureus 12 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1151771Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 5 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1594383Cmax in human at 625 mg, po2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID763949Antibacterial activity against Moraxella catarrhalis clinical isolate 2824 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1390475Antibacterial activity against TolC-deficient Escherichia coli2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID542888fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered as 4 divided doses every 6 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID531570Antibacterial activity against Streptococcus sp. 'group G' obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID542675fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 400 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID576901Ratio of AUC (0 to 24 hrs) to MIC for Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1434680Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3090 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1553385Inhibition of COX1 (unknown origin) by ELISA2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID283613Antimicrobial activity against Enterococcus faecalis 45 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID511303Antibacterial activity against ciprofloxacin susceptible and methicillin resistant Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID524727Antibacterial activity against linezolid-resistant Enterococcus faecium 03B1076 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID1327102Antitubercular activity against dormant stage Mycobacterium tuberculosis H37Ra measured after 12 days by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID528708Antibacterial activity against multidrug-resistant Streptococcus pneumoniae clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID434137Inhibition of MAOB2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Knowledge based identification of MAO-B selective inhibitors using pharmacophore and structure based virtual screening models.
AID283163Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2639 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID573887AUC (0 to 24 hrs) in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID262237Antibacterial activity against Streptococcus pyogenes ATCC 142892006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID532801Antibacterial activity against vancomycin-susceptible Staphylococcus aureus IL after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID522916Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1851 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID535018Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-3 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID630560Antibacterial activity against linezolid-resistant Staphylococcus epidermidis after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID534161Antimicrobial activity against linezolid-resistant Staphylococcus hominis by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID571802Antibacterial activity against Clostridium disporicum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID524691Antibacterial activity against Streptococcus pyogenes clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID262232Antibacterial activity against Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID509631Antimicrobial activity against Staphylococcus aureus RN4220 transformant carrying plasmid pKKS25 and expressing erm(T), dfrK and tet(L) genes by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain.
AID1584837Antibacterial activity against vancomycin-resistant Enterococcus faecalis BM 4390 after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID1877892Antibacterial activity against Mycobacterium smegmatis mc2 155 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID1186428Antimicrobial activity against Staphylococcus aureus ATCC 19636 infected in neutropenic mouse assessed as reduction in colony forming units at 25 mg/kg, iv administered as single dose measured 24 hrs post infection relative to control2014Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
Discovery and in vivo evaluation of alcohol-containing benzothiazoles as potent dual-targeting bacterial DNA supercoiling inhibitors.
AID519091Antimicrobial activity against Staphylococcus aureus KM168 harboring Arg149Ser mutation in rplC gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID285041Antimicrobial activity against Corynebacterium jeikeium by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID520001Antimicrobial activity against Haemophilus influenzae2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID524967Antibacterial activity against vancomycin- and teichoplanin-nonsusceptible Enterococcus faecalis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID133302Minimum inhibitory concentration of the subcutaneously administered compound evaluated against Staphylococcus pneumoniae PW3 strain in mice (SC)2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID576670Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID545804Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 planktonic cells by broth microdilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID535006Bactericidal activity against vancomycin-intermediate Staphylococcus aureus assessed as antibiotic concentration that reduced the number of viable cells by =>99.9% by colony count method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID559774Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID523032Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523781Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID565758Antimicrobial activity against Staphylococcus epidermidis clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID575273Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID577131Mean residence time in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1557277Antitubercular activity against multidrug resistant Mycobacterium tuberculosis2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID245273Minimum inhibitory concentration against Staphylococcus aureus ATCC 13709 (+4% BSA); value ranges from 3-6 uM2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID285136Antimicrobial activity against viridans group Streptococcus vestibularis at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1395704Bactericidal activity against methicillin-sensitive Staphylococcus aureus NRS107 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID311481Antimicrobial activity against vancomycin-sensitive Enterococcus faecalis ATCC 29212 after 14 to 16 hrs by serial microbroth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID577107AUBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1265135Inhibition of human recombinant MAO-A using p-tyramine as substrate at 50 to 200 uM measured up to 50 mins by ELISA screening analysis2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID511434Antimicrobial activity against Clostridium perfringens LFM1 assessed as resistant breakpoint by EUCAST method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID285069Antimicrobial activity against beta hemolytic Streptococci group G at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID517666Antimicrobial activity against Staphylococcus aureus Smith by standard serial-dilution technique2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
AID523029Antimicrobial activity against Staphylococcus sp. by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID165190In vitro antibacterial activity against Pseudomonas aeruginosa strain ATCC 278531996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID524686Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID278930Antibacterial activity against methicillin-resistant Staphylococcus aureus OC 2878 by time kill experiments2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID560832fT>MIC in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID520482Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 30 mg/kg, sc administered every 12 hrs for 4 days measured on week 6 postinfection (Rvb = 2.84 +/- 0.30 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID745375Inhibition of human CYP3A4 assessed as terfenadine hydroxylation after 20 mins by LC/MS/MS analysis2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID571807Antibacterial activity against Clostridium paraputrificum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1474209Bactericidal activity against Enterococcus faecalis clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID206435In vitro antibacterial activity against ciprofloxacin and methicillin resistant Staphylococcus aureus (Sau2CIP) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID373835Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 504 after 50 passages with daptomycin measured after 10 times antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID533428Antimicrobial activity against Peptostreptococcus sp. assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID424756Antibacterial activity against macrolide, imipenem, methicillin-resistant Staphylococcus aureus MB5393 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID558708Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID284974Antimicrobial activity against Corynebacterium pseudodiphtheriticum at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID571816Antibacterial activity against Bifidobacterium adolescentis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID523025Antimicrobial activity against linezolid-resistant Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523047Antimicrobial activity against Haemophilus influenzae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID573155Antibacterial activity against vancomycin-resistant Enterococcus faecium by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID373308Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID1076822Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate 3 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID1677805Antibacterial activity against penicillin-resistant Staphylococcus aureus incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID326499Antibacterial activity against vancomycin-susceptible Enterococcus faecalis JH2-2 after 24 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID533012Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR3 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID571767Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB-M626I mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID561098Antibacterial activity against Prevotella sp. by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID285101Antimicrobial activity against viridans group Streptococcus mitis at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID581655Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient at pH 7.4 after 48 hrs by broth microdilution method in presence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1578433Antimicrobial activity against methicillin-resistant Streptococcus pneumoniae ATCC 700677 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID274227Antibacterial activity against Enterococcus faecalis MGH-2 EF1-12006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID590152Antibacterial activity against methicillin-sensitive Staphylococcus aureus Smith infected iv dosed ICR mouse assessed as protection against mouse mortality administered 1 hr after infection measured up to 7 days2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1076833Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID1680009Induction of inner membrane permeabilization in Staphylococcus aureus ATCC 29213 at 20 ug/ml measured for 12 mins by propidium iodide staining based fluorescence microscopic analysis2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1770348Antibacterial activity against erythromycin-resistant Streptococcus pyogenes assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID285384Antibacterial activity against heteroresistant vancomycin-intermediate Staphylococcus aureus Mu3 using in vitro PK/PD model with 120 mg/24 hr continuous infusion simulated regimen after 72 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID576896Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1076821Antitubercular activity against extensive drug-resistant Mycobacterium tuberculosis clinical isolate 4 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID374003Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID595861Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate after 24 hrs by microdilution method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID1329445Antibacterial activity against linezolid-resistant Mycobacterium tuberculosis H37Rv in hollow-fiber infection model assessed as reduction in bacterial burden at 600 mg, po at 24 hrs dose regimen measured after 3 weeks2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
From lead optimization to NDA approval for a new antimicrobial: Use of pre-clinical effect models and pharmacokinetic/pharmacodynamic mathematical modeling.
AID1361051Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 16 to 18 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Halogenated quinolines bearing polar functionality at the 2-position: Identification of new antibacterial agents with enhanced activity against Staphylococcus epidermidis.
AID278931Antibacterial activity against Enterococcus faecalis ATCC 51922 by time kill experiments2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1367594Antibacterial activity against gram-negative Escherichia coli MG1655 expressing AcrAB-TolC efflux pump deletion mutant by CLSI broth microdilution method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID1390477Antibacterial activity against Enterococcus faecalis ATCC 512992018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID283387Effect on mitochondrial DNA level in PBMCs from patient on a long-term schedule of the drug with hyperlactatemia relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reversible inhibition of mitochondrial protein synthesis during linezolid-related hyperlactatemia.
AID533936Antimicrobial activity against linezolid-resistant Staphylococcus aureus 131-6952X harboring plasmid borne cfr gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID326286Antibacterial activity against methicillin-resistant Staphylococcus aureus 4875 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID323787Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected neutropenic CD1 mouse assessed as mouse survival at 50 mg/kg, sc after 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID528723Antibacterial activity against Streptococcus constellatus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1557278Antitubercular activity against Mycobacterium tuberculosis XDR2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID458458Antimicrobial activity against Escherichia coli ATCC 25922 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID528727Antibacterial activity against Streptococcus agalactiae group B clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID545809Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as inhibition of biofilm formation after 24 hrs by serial dilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID390333Antimicrobial activity against Haemophilus parainfluenzae 23192008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID528839Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1660515Antibacterial activity against Bacillus cereus ATCC 14579 after 16 hrs by CLSI-based broth microdilution method2020Journal of natural products, 06-26, Volume: 83, Issue:6
Synthesis of the Cyanobacterial Antibiotics Anaephenes A and B.
AID511383Antibacterial activity against vancomycin resistant Enterococcus faecalis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID523028Antimicrobial activity against Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID318353Antibacterial activity against methicillin-resistant Staphylococcus aureus2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID1563586Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1853479Bactericidal activity against persister methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as reduction in colony forming unit at 4 x MIC incubated for 18 to 24 hrs by Time-kill analysis2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID530122Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus 149 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID572020Antibacterial activity against Prevotella melaninogenica by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1139113Antimicrobial activity against Streptococcus pneumoniae infected in rat lung infection model assessed as log reduction of bacterial density at 30 mg/kg, po2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID207424In vitro antibacterial activity against Staphylococcus aureus ATCC 49951 (S. a. 213)2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID574952Antimicrobial activity against Streptococcus pneumoniae serotype 11A by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1519050Stability in human liver microsomes assessed as half life at 1.5 uM preincubated for 5 mins with NADPH and measured after 45 mins by LC/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID278916Antibacterial activity against linezolid-resistant Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID555315Antibacterial activity against methicillin-susceptible, vancomycin-intermediate Staphylococcus aureus 505 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID293837Antibacterial activity against methicillin-susceptible Staphylococcus aureus 209P2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
A new class of anti-MRSA and anti-VRE agents: preparation and antibacterial activities of indole-containing compounds.
AID528707Antibacterial activity against Streptococcus pyogenes group A clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID560583Bactericidal activity against vancomycin-resistant Enterococcus faecalis 1058946 expressing vanA gene assessed as change in bacterial count at 4 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID520231Antimicrobial activity against Streptococcus pneumoniae 02J12582008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID541540Antimicrobial activity against vancomycin-resistant Enterococcus faecium clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID572018Antibacterial activity against Prevotella nigrescens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1409845Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid for 3.5 days administered 6 hrs post bacterial infection measured 84 hrs post i2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID428276Antituberculosis activity against Mycobacterium tuberculosis by bactec MGIT 960 method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID424765Antibacterial activity against vancomycin, macrolide-resistant, linezolid-sensitive Enterococcus faecalis CL5246 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID533940Antimicrobial activity against linezolid-resistant Enterococcus faecalis 411 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID370013Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 6.25 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1434681Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3634 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID66098Inhibitory activity against Enterococcus faecium1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1180585Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC2381-2F to MIC for Staphylococcus aureus ARC23812014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID561088Antibacterial activity against Haemophilus influenzae by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID753130Antitubercular activity against Mycobacterium tuberculosis XDR-1 assessed as growth inhibition after 2 to 3 weeks by broth microdilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID1451758Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.1 mg, ip bid for 4.5 days pretreated 24 hrs prior to bacterial infection measured 108 hrs post infection relative 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID562390Antimicrobial activity against oxacillin-resistant Staphylococcus haemolyticus clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID561258Antibacterial activity against Streptococcus agalactiae assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1304843Antibiofilm activity against methicillin-resistant Enterococcus faecium ATCC 700221 assessed as biofilm eradication incubated for 24 hrs by CBD assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1609279Bactericidal activity against methicilline-sensitive Staphylococcus aureus ATCC 6538 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID278571Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 512992007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
AID541516Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID572004Antibacterial activity against Bacteroides ovatus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID528970Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1395711Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRS12 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID523048Antimicrobial activity against beta-lactamase negative Haemophilus influenzae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID548531Antimicrobial activity against Vancomycin-susceptible Enterococcus faecium by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID373833Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection techni2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID524950Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus sciuri clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID671564Antibacterial activity against Streptococcus pyogenes2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID528728Antibacterial activity against Streptococcus pyogenes group A clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID523836Ratio of vancomycin MIC50 to compound MIC50 for linezolid-susceptible Staphylococcus aureus2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID541094Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as cure rate at 25 mg/kg measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1154474Antibacterial activity against of methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in iv dosed mouse administered 1 hr after infection measured after 48 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID571826Antibacterial activity against Coriobacteriumecies by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1151709Myelosuppression activity against human CD34-positive blood stem/progenitor cells assessed as growth inhibition after 9 to 10 days by CellTiter-Glo luminescent assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1877888Antibacterial activity against Enterococcus faecium DSM-20477 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID558487Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID559360Antimicrobial activity against compound-susceptible Coxiella burnetii Nine-Mile obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID573146Antibacterial activity against penicillin-nonsusceptible Streptococcus viridans by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID522917Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1867 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID571790Antibacterial activity against Clostridium clostridioforme by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID207423In vitro antibacterial activity against methicillin resistant Staphylococcus aureus ATCC 33591 (S. a. 019)2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID206629Antibacterial activity was determined against clinically isolated Levofloxacin-methicillin resistant Staphylococcus aureus (LVFX-r MRSA) strains (74 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID585165Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2612A mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID541808Antimicrobial activity against Enterococcus durans clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1760591Antibacterial activity against vancomycin resistant Enterococcus faecalis 51575 assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID304007Effect on hematology in Sprague-Dawley rat assessed as decrease in reticulocytes at 200 mg/kg/day after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID511304Antibacterial activity against ciprofloxacin and methicillin resistant Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID541546Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID275469Antibacterial activity against Staphylococcus aureus ATCC 33591 infected in CD1 mouse at 20 mg/kg, sc2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID1539453Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI-based broth microdilution assay
AID775548Antibacterial activity against Staphylococcus aureus SR20549 clinical isolate assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID1759684Inhibition of protein synthesis in Staphylococcus aureus ATCC 29213 at 8 times MIC measured by liquid scintillation counter2021European journal of medicinal chemistry, Jul-05, Volume: 2194-4-(Anilinomethyl)-3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-ylbenzoic acid derivatives as potent anti-gram-positive bacterial agents.
AID1180570Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC516-1F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID542686fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 700 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID745404Antibacterial activity against Enterococcus faecalis SR1004 clinical isolate assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID548746Antimicrobial activity against viridans group Streptococcus assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID558085Antimicrobial activity against Mycoplasma fermentans isolated from human by two fold serial dilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
AID1167738Antimicrobial activity against methicillin-sensitive Staphylococcus aureus by broth microdilution method in presence of 50% human serum2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID1862423Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID585157Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA A2058G mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID283157Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2414 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID572003Antibacterial activity against Bacteroides fragilis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1271211Metabolic stability in rat liver microsomes after 30 mins by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1474257Toxicity in Caenorhabditis elegans AU37 assessed as worm survival at 20 ug/ml after 24 hrs by microscopic analysis2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1400045Bactericidal activity against Staphylococcus aureus BAA 44 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID311476Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID370034Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected in po dosed DBA/2 mouse localized infection model assessed as log reduction in CFU per gram of thigh at 10 mg/kg, po administered 2 hrs postinfection thrice daily for 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID558705Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1167736Antimicrobial activity against Escherichia coli by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID285544Cmax in mouse at 50 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID387450Antibacterial activity against linezolid-resistant Staphylococcus aureus DRCC 5642008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID573869Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 infected in sc dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID208611Antibacterial activity was determined against clinically isolated penicillin resistant Streptococcus pneumoniae (PRSP) strains (50 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID541091Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 during logarithmic growth phase by macrodilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID125077In vitro antibacterial activity against Moraxella catarrhalis 306072003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID1689205Antibacterial activity against methicillin resistant Staphylococcus aureus subsp. aureus USA300 assessed as reduction in bacterial growth by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID528725Antibacterial activity against Streptococcus intermedius clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1578417Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 10 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID1862415Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID326296Antibacterial activity against methicillin-resistant Staphylococcus aureus 4875 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1446761Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRSA4 after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1553377Stability in gastric pH assessed as compound remaining after 24 hrs relative to control2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID349309Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID1584842Antibacterial activity against community-acquired methicillin and erythromycin resistant Staphylococcus aureus SA 325 after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID285116Antimicrobial activity against viridans group Streptococcus oralis at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID519990Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID555294Antibacterial activity against Tmp-susceptible Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID577127Terminal half-life in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID383564Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID69194Minimum inhibitory concentration (MIC) against Escherichia coli OC 26052004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID1139111Clearance in rat at 2.8 to 9.5 mg/kg, iv2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID524682Antibacterial activity against glycopeptide-intermediate Staphylococcus aureus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID604294Antibacterial activity against Bacillus subtilis BD54 after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID1361097Bacteriostatic activity against methicillin-resistant Staphylococcus aureus NRS119 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID1688278In vivo antibacterial activity against methicillin resistant Staphylococcus aureus clinical isolate 15-1 infected in kunming mouse assessed as animal survival rate at 3 mg/kg, po administered 6 hrs prior to bacterial infection and at 0 and 6 hrs post infe2020European journal of medicinal chemistry, Feb-15, Volume: 188N-thiadiazole-4-hydroxy-2-quinolone-3-carboxamides bearing heteroaromatic rings as novel antibacterial agents: Design, synthesis, biological evaluation and target identification.
AID572556Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar proportion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro activities of linezolid against clinical isolates of Mycobacterium tuberculosis complex isolated in Taiwan over 10 years.
AID318360Antibacterial activity against wild type Escherichia coli2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID1677803Antibacterial activity against Escherichia coli ATCC25922 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1056364Antibacterial activity against Staphylococcus aureus SR20549 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1361109Bactericidal activity against methicillin-resistant Staphylococcus aureus USA500 NRS385 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID285020Antimicrobial activity against Listeria monocytogenes at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1594375Antibacterial activity against Escherichia coli BW25113 after 18 to 24 hrs in absence of colistin by broth microdilution method2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1151758Antibacterial activity against vancomycin-sensitive/high-level gentamycin-resistant Enterococcus faecalis isolate HH222014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID297128Antibacterial activity against Staphylococcus aureus Smith after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID524964Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus xylosus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID717875Antibacterial activity against methicillin-resistant Staphylococcus aureus OM584 by two-fold liquid microdilution method2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Riccardin C derivatives as anti-MRSA agents: structure-activity relationship of a series of hydroxylated bis(bibenzyl)s.
AID285029Antimicrobial activity against Micrococcus luteus at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID558513Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID562587Antimicrobial activity against Enterococcus faecium expressing VanB gene clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID637971Antibacterial activity against Streptococcus pneumoniae expressing PenR gene after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID1680075Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial measured after 20 passages by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID285140Antimicrobial activity against viridans group Streptococcus vestibularis at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID524948Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus hominis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1243929Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA500 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID560584Bactericidal activity against vancomycin-resistant Enterococcus faecium 1119175 expressing vanB gene assessed as change in bacterial count at 4 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1446754Antibacterial activity against methicillin-resistant Staphylococcus aureus USA100 NRS382 clinical isolate after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID295160Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-42 infected po dosed KunMing mouse2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID285099Antimicrobial activity against viridans group Streptococcus intermedius at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID533985Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus NRS18 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID522886Antibacterial activity against vancomycin-hetero-intermediate Staphylococcus aureus isolate 618 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID531638Selectivity ratio of IC50 for rabbit reticulocyte 50S ribosomal subunit to IC50 for Staphylococcus aureus ATCC 29213 50S ribosomal subunit2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID583196Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate NJ992 after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1853451Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID278573Antimicrobial activity against Rhodococcus equi ATCC 69392007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
AID116078Minimum inhibitory concentration in mice against antimicrobial activity in vancomycin-resistant Enterococcus faecalis (VREF 29212).2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids.
AID581029Inhibition of lipid synthesis in Staphylococcus epidermidis ATCC 23760 assessed as incorporation of [14C]acetate at 2 ug/ml after 60 mins by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID1723493Antibacterial activity against Enterococcus faecium NR-31903 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID523812Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1594378Antibacterial activity against AcrAB-TolC deficient Escherichia coli JW25113 after 18 to 24 hrs in presence of colistin by broth microdilution method2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID285380Bactericidal activity against heteroresistant vancomycin-intermediate Staphylococcus aureus Mu3 assessed as reduction of CFU using in vitro PK/PD model with human dosage regimen 120 mg every 12 hrs after 48 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID406622Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae isolates assessed as percent susceptible isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.
AID571791Antibacterial activity against Clostridium difficile by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1414199Selectivity ratio of MBC for methicillin-resistant Staphylococcus aureus ATCC 43300 to MIC for methicillin-resistant Staphylococcus aureus ATCC 433002018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1151770Antibacterial activity against Streptococcus pyogenes isolate 556 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID583892Antibacterial activity against vancomycin-heteroresistant Staphylococcus aureus isolate 443 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID1437032Antimycobacterial activity against isoniazid/rifampicin/streptomycin-resistant Mycobacterium tuberculosis by microplate Alamar Blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis.
AID68389In vitro antibacterial activity against vancomycin-resistant Enterococcus faecium (VRE.1)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID1414200Selectivity ratio of MBC for clinical isolate of penicillin-resistant Staphylococcus aureus to MIC for clinical isolate of penicillin-resistant Staphylococcus aureus2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1609289Antibacterial activity against methicilline-sensitive Staphylococcus aureus NRS-107 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID576678Bactericidal activity against 12 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID498886Antimicrobial activity against Pseudomonas aeruginosa OC 4354 assessed as inhibition of growth by broth microdilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID456046Antibacterial activity against vancomycin-resistant Enterococcus faecium after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID524962Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus simulans clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID558527Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID523030Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID523038Antimicrobial activity against streptococcal sp. by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID562397Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID245165In vitro minimum inhibitory concentration against Staphylococcus epidermidis (ATCC 12228)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID575188Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID729220Antibacterial activity against Enterococcus faecalis after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID1710606Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as reduction in bacterial count at 3 x MIC incubated upto 24 hrs by time kill analysis2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1167737Antimicrobial activity against tolC-deficient Escherichia coli by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID531574Antibacterial activity against Aerococcus viridans obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID573141Antibacterial activity against erythromycin-nonsusceptible Streptococcus agalactiae by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID484702Antimicrobial activity against methicillin-susceptible Staphylococcus aureus2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Potent antimicrobial activity of 3-(4,5-diaryl-1H-imidazol-2-yl)-1H-indole derivatives against methicillin-resistant Staphylococcus aureus.
AID1312939Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID284979Antimicrobial activity against Corynebacterium striatum at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID571813Antibacterial activity against Clostridium tertium by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID383566Antibacterial activity against Staphylococcus aureus ATCC 14154 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID565009Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus haemolyticus assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID283393Antimicrobial activity against Nocardia abscessus after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID531558Antibacterial activity against coagulase-negative Staphylococcus capitis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1596562Bactericidal activity against methicillin resistant Staphylococcus aureus NRS119 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID523036Antimicrobial activity against vancomycin-resistant Enterococcus faecium by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID585158Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA G2032C mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID127508Antibacterial activity against Moraxella catarrhalis UC30610 (M. cat)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID576434Bactericidal activity against 14 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID405618Antibacterial activity against coagulase-negative Staphylococcus2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID523798Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID561087Antibacterial activity against Streptococcus agalactiae by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1710589Antibacterial activity against vancomycin- resistant Enterococcus faecalis ATCC 51299 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID710139Antibacterial activity against methicillin-resistant Staphylococcus aureus2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria.
AID576393Cmax in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID697276Antibacterial activity against hospital acquired methicillin-resistant Staphylococcus aureus ARC 1692 after 18 to 24 hrs by CLSI broth microdilution method2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
AID1409844Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.1 mg, ip bid for 3.5 days administered 6 hrs post bacterial infection measured 84 hrs post i2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID567568Antimicrobial activity against Staphylococcus aureus RN4220 harboring pBS-01multiple resistance gene cfr and phenolic resistance gene fexA obtained from swine feces2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
First report of the multidrug resistance gene cfr and the phenicol resistance gene fexA in a Bacillus strain from swine feces.
AID573114Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1367598Inhibition of protein synthesis in Escherichia coli ribosomes incubated for 1 hr at 37 degC by SDS-PAGE and Gaussia luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID533008Antibacterial activity against vancomycin-intermediate Staphylococcus aureus LIM2 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1327108Antibacterial activity against Pseudomonas aeruginosa NCIM 2036 at 30 ug/ml measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID373845Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 Hershey after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID542912Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing at 400 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID564806Antimicrobial activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1680008Induction of inner membrane permeabilization in Escherichia coli ATCC 25922 at 20 ug/ml measured for 12 mins by propidium iodide staining based fluorescence microscopic analysis2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID548797Antimicrobial activity against Vancomycin-susceptible Enterococcus faecalis assessed as percent resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID775530Inhibition of CYP3A4 in human liver microsomes assessed as terfenadine hydroxylation after 20 mins by LC/MS/MS analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID284946Antimicrobial activity against Bacillus spp. at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID262238Antibacterial activity against penicillin-resistant Streptococcus pneumoniae ATCC 7009042006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID278865Increase in lactate production in primary human osteoblasts at 400 ug/ml by ELISA relative to control2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID560504Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate bd4768 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID577102AUBC (0 to 24 hrs) in Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID285091Antimicrobial activity against viridans group Streptococcus gordonii at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID531560Antibacterial activity against coagulase-negative Staphylococcus cohnii obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID533978Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA040 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID287259Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID1167990Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 7670 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1415070Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 6 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID522925Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 693 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID560520Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate sh07043 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1117378Antimicrobial activity against Staphylococcus aureus Efs4 assessed as partially clear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID207511Minimum inhibitory concentration against Staphylococcus aureus UC92131998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID524966Antibacterial activity against vancomycin-susceptible Enterococcus faecalis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID560364Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 by broth dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID565745Antimicrobial activity against vancomycin-nonsusceptible Enterococcus faecium clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1400041Bactericidal activity against Staphylococcus aureus BAA 2094 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID559788Antimicrobial activity against heterogeneous vancomycin-susceptible Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID278570Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis ATCC 292122007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
AID574954Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19A by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID573116Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID285103Antimicrobial activity against viridans group Streptococcus mitis at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID245147Minimum inhibitory concentration against Haemophilus influenzae (strain A20191) in absence of calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID278568Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 433002007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro activities of the lipopeptides palmitoyl (Pal)-Lys-Lys-NH(2) and Pal-Lys-Lys alone and in combination with antimicrobial agents against multiresistant gram-positive cocci.
AID1778656Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID369444Antibacterial activity against penicillin-intermediate Streptococcus pneumoniae after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID1451772Antibacterial activity against Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid for 4.5 days treated 24 hrs prior to bacterial infection measured 108 hrs post infection relative to 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID245007Antibacterial activity against Staphylococcus epidermidis 56500 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID562191Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1553376Aqueous solubility of compound2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID261061Antibacterial activity against Staphylococcus aureus UC-76 SA-12006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
AID524942Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID278910Antibacterial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1400060Bactericidal activity against Streptococcus salivarius ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID529822Bactericidal activity against hospital-acquired methicillin-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Activities of ceftobiprole, linezolid, vancomycin, and daptomycin against community-associated and hospital-associated methicillin-resistant Staphylococcus aureus.
AID373825Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 after 14 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection techni2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID285059Antimicrobial activity against beta hemolytic Streptococci group C at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID533967Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 25923 infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1271208Metabolic stability in rat plasma by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID263961Antibacterial activity against methicillin-resistant Staphylococcus aureus DRCC 0192006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID583202Antimicrobial activity against vancomycin-heteroresistant Staphylococcus aureus after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID561755Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as resistant isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID541034Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 75 mg/kg after measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1710590Antibacterial activity against vancomycin- resistant Enterococcus faecalis ATCC 700221 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1308266Drug level in uninfected thighs of ICR mouse neutropenic thigh model of methicillin-resistant Staphylococcus aureus NRS70 infection at 10 mg/kg, sc tid administered every 8 hrs starting from 1 hr post infection and measured 7 hrs post last dose by UPLC an2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID326290Antibacterial activity against methicillin-resistant Staphylococcus aureus 4803 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID1609261Bactericidal activity against Listeria monocytogenes ATCC 19111 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID245274Minimum inhibitory concentration against methicillin-resistant Staphylococcus epidermidis UC120842005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID284988Antimicrobial activity against Enterococcus casseliflavus at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1474210Bactericidal activity against vancomycin-resistant Enterococcus faecalis clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID285344Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20040332 in Mueller-Hinton medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID542889fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 200 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID368281Cmax in rabbit plasma at 58 mg/kg infused every 12 hrs for 4 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID509632Antimicrobial activity against Staphylococcus aureus 25 transformant carrying plasmid pKKS25 and expressing erm(T), dfrKtet(L), tet(K), tet(M), mecA and blaZ genes by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain.
AID1414195Bactericidal activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs followed by plating onto tryptic soy agar plates and further incubated for 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID404936Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus sp. by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID499116Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected immunocompromized SKH1 mouse assessed as lesion volume at 25 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1535 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID572014Antibacterial activity against Prevotella P denticola by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1778101Antibacterial activity against linezolid resistant Enterococcus faecalis assessed as bacterial growth inhibition after 18 hrs by broth microdilution method
AID562620Antimicrobial activity against vancomycin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID373815Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID522885Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 1264 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID542683fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 400 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID244902Minimal inhibitory concentration against Enterococcus durans ATCC 5812004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID522894Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1011 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1609276Bactericidal activity against methicilline-resistant Staphylococcus aureus NRS123 USA400 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1180571Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC516-2F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1596564Bactericidal activity against vancomycin resistant Staphylococcus aureus VRS10 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID562622Antimicrobial activity against Coagulase-negative Staphylococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1703730Antibacterial activity against cephalosporin-resistant Streptococcus pneumoniae ATCC 51916 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1710588Antibacterial activity against methicillin- resistant Streptococcus pneumoniae ATCC 700677 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID534156Antimicrobial activity against linezolid-resistant Enterococcus faecium 854 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID581021Inhibition of DNA synthesis in Staphylococcus epidermidis ATCC 23760 assessed as incorporation of [3H]thymidine at 2 ug/ml by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID562394Antimicrobial activity against oxacillin-susceptible Staphylococcus epidermidis clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1151765Antibacterial activity against penicillin-sensitive Streptococcus pneumoniae isolate 0806 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID541781Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID519082Antimicrobial activity against Escherichia coli KM69-73 harboring G2576U mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID244869Minimum inhibitory concentration against Klebsiella pneumoniae ATCC 133832004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID308489Antibacterial activity against Haemophilus influenzae HI35422007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
AID1400027Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC100 for replicating Mycobacterium tuberculosis H37Rv by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID511302Antibacterial activity against methicillin susceptible Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID561248Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as resistant isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1578428Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis NRS101 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID326285Antibacterial activity against methicillin-resistant Staphylococcus aureus 859 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID548525Antimicrobial activity against Oxacillin-susceptible Staphylococcus aureus by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID576431Bactericidal activity against 12 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID604290Antibacterial activity against Enterococcus faecalis ATCC 29212 after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID1852675Antibacterial activity against multidrug resistant Acinetobacter baumannii AYE assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID571806Antibacterial activity against Clostridium orbiscindens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID560804Cmax in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID245123In vitro antibacterial activity against Staphylococcus aureus; value ranges from 3-6 uM2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID519138Antimicrobial activity against community-acquired methicillin resistant Staphylococcus aureus expressing PVL and mec type IV gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Antimicrobial activities of Ceftaroline and ME1036 tested against clinical strains of community-acquired methicillin-resistant Staphylococcus aureus.
AID617501Antibacterial activity against methicillin-resistant Staphylococcus aureus 43300 by CLSI method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents. Part II.
AID245128Minimum inhibitory concentration against Enterococcus faecalis (strain A20688) in absence of calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID245217Minimum inhibitory concentration against Staphylococcus aureus (strain A15090) in presence of 50% calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID1778669Ratio of MBC to MIC against penicillin-resistant Staphylococcus epidermidis2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID577093Ratio of AUC (0 to 24 hrs) to MIC for Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1076825Antitubercular activity against Mycobacterium tuberculosis H37RV ATCC 27294 assessed as growth inhibition after 3 to 11 days by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID1151627Toxicity in female rat assessed as effect on platelet count at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 654.6 x 10'9/L)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1350036Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 7 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID745407Antibacterial activity against Staphylococcus aureus SR20549 clinical isolate assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID285123Antimicrobial activity against viridans group Streptococcus parasanguis at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1395681Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS12 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID326299Antibacterial activity against methicillin-resistant Staphylococcus aureus 789 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID591660Antimicrobial activity against multidrug-resistant Staphylococcus aureus after 18 hrs by agar dilution method2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
AID475001Antibacterial activity against vancomycin-resistant Enterococcus faecalis LCB0006 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID571793Antibacterial activity against Clostridium innocuum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID571828Antibacterial activity against Holdemania filiformis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1649294Antibacterial activity against Escherichia coli JC2 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID319170Protection against methicillin-resistant Staphylococcus aureus infection in pneumonia patient2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID373831Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 after 22 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection techniq2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1312952Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID318369Inhibition of fatty acid synthesis in Streptococcus pneumoniae in whole cell activity assay2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID541528Antimicrobial activity against Staphylococcus haemolyticus clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID561241Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID206863Antibacterial activity against Methicillin-resistant Staphylococcus aureus UC6685 (S. a.)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID285038Antimicrobial activity against Bacillus cereus by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1303419Antibacterial activity against methicillin-resistant Staphylococcus aureus infected in po dosed mouse model assessed as inhibition of systemic infection administered bid for 3 days2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID562193Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1770366Bactericidal activity against Vancomycin-resistant Enterococcus faecium ATCC 51559 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID524963Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus warneri clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1861531Terminal half life in Wistar rat at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID1435926Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRSA4 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID519481Antibacterial activity against Staphylococcus aureus T991 by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID562163Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID534159Antimicrobial activity against linezolid-resistant Enterococcus faecalis by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID1303421Antibacterial activity against Penicillin-resistant Streptococcus pneumoniae yonsei 15 infected in po dosed immunosuppressed mouse model assessed as inhibition of pulmonary infection administered bid for 3 days2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID645044Antibacterial activity against Streptococcus pneumoniae PEN-1 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID583392Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate NJ992 assessed as bacterial count at 8 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1698677Antibacterial activity against Methicillin-resistant Staphylococcus aureus by CLSI method2020Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors.
AID1591562Bactericidal activity against penicillin-resistant Staphylococcus aureus clinical isolate assessed as 3 log reduction in number of colony forming units incubated for 24 hrs followed by aliquots transfer to tryptic soy agar and grown for 24 hrs2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID285061Antimicrobial activity against beta hemolytic Streptococci group F at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID533932Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS121 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID561092Antibacterial activity against Bacteroides thetaiotaomicron by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1414189Antibacterial activity against Bacillus pumilus CMCC63202 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID571989Antibacterial activity against Ruminococcus productus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID533927Antimicrobial activity against Staphylococcus aureus 1651 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID717210Antimicrobial activity against methicillin-sensitive Staphylococcus aureus CCARM 0205 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1421231Antibacterial activity against methicillin-sensitive Staphylococcus aureus clinical isolates by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID1304827Antibiofilm activity against methicillin-resistant Staphylococcus aureus isolate 2 assessed as biofilm eradication incubated for 24 hrs by CBD assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1687308Antibacterial activity against Escherichia coli ATCC 25922 incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1361098Bacteriostatic activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID285351Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20041010 in CCY media2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID369672Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith by dilution susceptibility test2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID576657Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1547719Antibacterial activity against vancomycin-resistant Enterococcus faecium 106 clinical isolate by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID369437Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID542884fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID558083Antimicrobial activity against Mycoplasma pneumoniae isolated from human by two fold serial dilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
AID637979Antibacterial activity against Staphylococcus aureus ATCC 25923 after overnight incubation by twofold broth dilution technique in presence of 10% human serum2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID206238In vitro antibacterial activity against Staphylococcus aures strain UC126731996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1151780Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0605 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 80 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID541534Antimicrobial activity against Enterococcus faecium clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1304836Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID523786Antimicrobial activity against linezolid-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 16 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID519488Antibacterial activity against Staphylococcus aureus T1910 expressing 23S rrn2 G2576T, rrn3 G2576T, rrn4 G2576T and rrn5 G2576T mutants by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID576414Apparent volume of distribution in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1180581Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC516-1F to MIC for Staphylococcus aureus ARC5162014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1594360Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS385 USA500 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID67243In vitro antibacterial activity against Enterococcus faecalis C6291 (E.f.1).1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1474207Bactericidal activity against Vancomycin-resistant Enterococcus faecium clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID297123Antibacterial activity against Linezolid and methicillin-resistant Staphylococcus aureus 06 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID373812Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 48 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID284968Antimicrobial activity against Corynebacterium jeikeium at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID303916Antibacterial activity against Streptococcus pyogenes ATCC 19615 after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID571991Antibacterial activity against Ruminococcus sp. by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID284957Antimicrobial activity against Corynebacterium spp. at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID559367Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP2 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1151624Toxicity in female rat assessed as effect on hematocrit level at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 39.08%)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID645038Antibacterial activity against erythromycin-sensitive Streptococcus pyogenes 12 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID499164Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 100 mg/kg/day, po (Rvb = 1.6 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1367597Permeability index, ratio of MIC for wild type Escherichia coli MG1655 to MIC for Escherichia coli MG1655 membrane permeabilized mutant in presence of polymyxinnonapeptide2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID283386Increase in Cytochrome C oxidase 2 mitochondrial RNA transcripts in PBMCs from patient on a long-term schedule of the drug with hyperlactatemia relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reversible inhibition of mitochondrial protein synthesis during linezolid-related hyperlactatemia.
AID1680050Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 6 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID533119Antimicrobial activity against Staphylococcus aureus 10*3d1-10 by Etest method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Serial daptomycin selection generates daptomycin-nonsusceptible Staphylococcus aureus strains with a heterogeneous vancomycin-intermediate phenotype.
AID528726Antibacterial activity against Streptococcus mitis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1271217Cmax in BALB/c mouse plasma at 10 mg/kg, po by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID662300Antimycobacterial activity against Mycobacterium tuberculosis H37Rv grown in glycerol-alanine-salts media2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Syntheses and biological studies of novel spiropiperazinyl oxazolidinone antibacterial agents using a spirocyclic diene derived acylnitroso Diels-Alder reaction.
AID1056337Inhibition of human CYP2D6 assessed as dextromethorphan O-demethylation after 20 mins by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID573870Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in sc dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1390484Antibacterial activity against Enterococcus faecalis ATCC 292122018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID695450Inhibition of human ERG expressed in mammalian cells at 10 uM by patch clamp method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1591548Ratio of MBC for penicillin-resistant Staphylococcus aureus clinical isolate to MIC for penicillin-resistant Staphylococcus aureus clinical isolate2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1308240Bacteriostatic activity against multidrug resistant Staphylococcus aureus ATCC 276602016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID1501357Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123 (USA400) after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID326500Antibacterial activity against vancomycin-resistant Enterococcus faecalis UCN41 after 24 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID1710576Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS383 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID206439In vitro antibacterial activity against linezolid-resistant Staphylococcus aureus ATCC 29213 (LRSA).2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID1390473Antibacterial activity against linezolid-resistant Staphylococcus epidermidis 11171742018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID323807Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse with peritonitis at 100 mg/kg, po after 4 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID1395989Hemolytic activity in human RBC at 200 uM after 1 hr relative to control2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID533413Antimicrobial activity against Peptoniphilus asaccharolyticus by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID576869Bactericidal activity against 13 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID528738Antibacterial activity against methicillin resistant Staphylococcus aureus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1393962Antibacterial activity against methicillin resistant Staphylococcus aureus ATCC 33591 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID525135Antibacterial activity against Staphylococcus aureus KM50 after 18 to 24 hrs by broth microdilution method selected after 16 ug/ml drug exposure for 6 hrs by culture absorbance method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID572015Antibacterial activity against Prevotella P disiens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1151773Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 20 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID574949Antimicrobial activity against Streptococcus pneumoniae serotype 3 by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1547708Antibacterial activity against Staphylococcus aureus NRS120 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID534158Antimicrobial activity against linezolid-resistant Staphylococcus epidermidis by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID734707Antibacterial activity against Micrococcus luteus MTCC 2470 after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID1710573Antibacterial activity against methicillin-sensitive Staphylococcus aureus NRS 107 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID373652Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1311369Antibacterial activity against Mycobacterium abscessus ATCC 19977 measured after 3 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID285082Antimicrobial activity against viridans group Streptococcus bovis at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1308209Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID1594362Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS11a after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID528722Antibacterial activity against Streptococcus viridans clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID520011Antimicrobial activity against Staphylococcus aureus A8831 harboring U2500A mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID561079Antibacterial activity against vancomycin-susceptible Enterococcus faecalis by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID208756Antibacterial activity against Streptococcus agalactiae2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1329015Antibacterial activity against Streptococcus pneumoniae PBS13992016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic.
AID1710571Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID209895Antibacterial activity against Streptococcus pneumoniae UC9912 (S.p)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID541067Half life in cage fluid of Albino guiena pig at 25 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID576662Bactericidal activity against 13 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID369442Antibacterial activity against vancomycin-resistant Enterococcus faecium after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID348864Antibacterial activity against vancomycin-resistant Enterococcus 5 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID524946Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1539452Antibacterial activity against Staphylococcus epidermidis NRS101 after 18 to 20 hrs in aerobic condition by CLSI-based broth microdilution assay
AID695449Cytotoxicity against human HepG2 cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID429430Antibacterial activity against Moraxella catarrhalis by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID1547738Drug level in mouse thigh infected with linezolid-sensitive Staphylococcus aureus NRS70 at 40 mg/kg, po administered 1 hrs post infection and measured for 48 hrs2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID1151718Antibacterial activity against beta-lactamase-negative Staphylococcus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID428275Antituberculosis activity against Mycobacterium tuberculosis by bactec 460 TB method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID571794Antibacterial activity against Clostridium perfringens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1151749Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 292132014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID522892Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1009 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID523050Antimicrobial activity against ampicillin-nonsusceptible beta-lactamase negative Haemophilus influenzae by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID1151779Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0605 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 40 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1703724Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID572016Antibacterial activity against Prevotella P intermedia by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1390489Antibacterial activity against vancomycin-resistant Enterococcus faecium 31/1322018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1311359Antibacterial activity against Acinetobacter baumannii ATCC 19606 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID1327116Antibacterial activity against Bacillus subtilis NCIM 2010 at 3 ug/ml measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID363435Antibacterial activity against Streptococcus pneumoniae ATCC 6303-infeceted Sprague-Dawley rat assessed as reduction in lung bacterial density at 25 mg/kg, po administered twice at 18 and 26 hrs after bacterial challenge measured at 72 hrs postinfection2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
AID1852686Antibacterial activity against efflux pump lacking Pseudomonas aeruginosa assessed as inhibition of bacterial growth
AID575041AUC (24 hrs) in patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID1374166Antibacterial activity against Escherichia coli ATCC 25922 incubated at 37 degC for 20 hrs by standard broth microdilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID548528Antimicrobial activity against Oxacillin-resistant coagulase-negative Staphylococcus by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID429419Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID528733Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus hominis subsp. novobiosepticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1591544Antibacterial activity against Escherichia coli ATCC 25922 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID326298Antibacterial activity against methicillin-resistant Staphylococcus aureus 293 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID745377Inhibition of human CYP1A2 assessed as ethoxyresorufin O-deethylation after 20 mins by fluorescence plate reader analysis2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID1151705Antibacterial activity against Staphylococcus aureus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID349316Antibacterial activity against vancomycin-sensitive Enterococcus after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID559366Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP1 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID572273Antimicrobial activity against Streptococcus pneumoniae ATCC 6303 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID125097Minimum inhibitory concentration measured against Moraxella catarrhalis2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID278906Antibacterial activity against Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID308486Antibacterial activity against Staphylococcus aureus UC76 SA12007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
AID1770364Bactericidal activity against Vancomycin-susceptible Enterococcus faecalis ATCC 29212 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID370009Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 6.25 mg/kg/day, po administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burd2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID410113Antimicrobial activity against erm (B) expressing Streptococcus pneumoniae 02J1258 + L4 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID477370Antibacterial activity against floxacin and methicillin-resistant Staphylococcus aureus ATCC 25923 after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID285021Antimicrobial activity against Listeria monocytogenes at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID561097Antibacterial activity against Porphyromonas asaccharolytica by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID1862422Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51575 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID525136Antibacterial activity against Staphylococcus aureus KB103 after 18 to 24 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID283400Antimicrobial activity against Nocardia sp. after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID555300Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1076824Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37RV clinical isolate 1 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID528695Antibacterial activity against methicillin resistant Staphylococcus aureus MED 1805 bloodstream isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1167728Inhibition of Escherichia coli DNA gyrase using fluorescence-tagged DNA by fluorescenct polarization assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID533425Antimicrobial activity against Peptostreptococcus sp. by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID370041Antibacterial activity against 10'9 CFU linezolid-resistant methicillin-resistant Staphylococcus aureus by dilution susceptibility test2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID285017Antimicrobial activity against Enterococcus raffinosus at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID284994Antimicrobial activity against Enterococcus durans at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1308232Antibacterial activity against Streptococcus pyogenes ATCC 49399 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID585167Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA G2032A, C2499A mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID1193403Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 measured after overnight incubation2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID1649280Antibacterial activity against Staphylococcus aureus RN4220 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID776671Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 16 to 20 hrs by microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Novel promising linezolid analogues: rational design, synthesis and biological evaluation.
AID564805Antimicrobial activity against methicillin-resistant Staphylococcus aureus after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID745406Antibacterial activity against Staphylococcus aureus Smith assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID303913Antibacterial activity against methicillin-resistant Staphylococcus aureus 33 after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID283629Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4280-0257 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID439894Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 1 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID85783Antibacterial activity against Haemophillia influenzae2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1539447Antibacterial activity against Methicillin-resistant Staphylococcus aureus NRS385-USA500 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID581663Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level per mg of protein at up to 10'5 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID285052Antimicrobial activity against Rothia mucilaginosa by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1327101Antitubercular activity against active stage Mycobacterium tuberculosis H37Ra measured after 8 days by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1400059Antibacterial activity against Streptococcus salivarius ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1861526Cmax in Wistar rat at 30 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID285067Antimicrobial activity against beta hemolytic Streptococci group G at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID428278Antituberculosis activity against linezolid-resistant Mycobacterium tuberculosis by bactec MGIT 960 method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID562636Antimicrobial activity against Listeria monocytogenes by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1390464Antibacterial activity against methicillin-resistant Staphylococcus aureus 5622018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1594357Antibacterial activity against methicillin-sensitive Staphylococcus aureus NRS107 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID326294Antibacterial activity against methicillin-resistant Staphylococcus aureus 5004 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID561253Antibacterial activity against Streptococcus pyogenes by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID529823Bactericidal activity against community-acquired methicillin-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Activities of ceftobiprole, linezolid, vancomycin, and daptomycin against community-associated and hospital-associated methicillin-resistant Staphylococcus aureus.
AID1329018Antibacterial activity against Streptococcus pneumoniae PBS1399 infected in mouse assessed as protection against bacterial infection by measuring mouse survival administered intravenously as single dose after 2 hrs of infection measured on day 72016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Discovery, pharmacology, and clinical profile of omadacycline, a novel aminomethylcycline antibiotic.
AID561515Antibacterial activity against Enterococcus faecium by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID573156Antibacterial activity against vancomycin-resistant Enterococcus faecium assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID278909Antibacterial activity against vancomycin-intermediate methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID285343Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20030203 in Mueller-Hinton medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID1414209Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in mouse assessed as reduction of bacterial burden in blood at 30 mg/kg, ip administered 0.1, 6 hrs postinfection and measured at 24 hrs post last dose2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID370006Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 3.12 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID207681Minimum inhibitory concentration (MIC) against Staphylococcus aureus OC 4172 in the presence of 50% mouse serum2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID499113Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected immunocompromized SKH1 mouse assessed as lesion volume at 100 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1181 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1361111Bactericidal activity against methicillin-resistant Staphylococcus aureus USA800 NRS387 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID373992Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID522924Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 593 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID245440Minimum inhibitory concentration against penicillin-susceptible Streptococcus pneumoniae UC9912; Range is 0.5-1 ug/mL2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID1415069Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 5 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID1778655Antibacterial activity against erythromycin-resistant Streptococcus pyogenes 2 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID1609283Antibacterial activity against methicilline-resistant Staphylococcus aureus NRS385 USA500 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID237336Calculated partition coefficient (clogP)2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID274229Antibacterial activity against Moraxella catarrhalis BC-35312006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID533982Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus ATCC 25923 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID562628Antimicrobial activity against Group C Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1435931Bactericidal activity against methicillin/ciprofloxacin/clindamycin-resistant Staphylococcus aureus USA100 NRS382 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID1308264Drug level in plasma of ICR mouse neutropenic thigh model of methicillin-resistant Staphylococcus aureus NRS70 infection at 10 mg/kg, sc tid administered every 8 hrs starting from 1 hr post infection and measured 7 hrs post last dose by UPLC analysis2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID1151732Antibacterial activity against Streptococcus sanguinis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1609282Antibacterial activity against vancomycin-resistant Staphylococcus aureus 10 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID297958AUC in Streptococcus pneumoniae 548 infected mouse lung infection model at 80 mg/kg/day, po2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.
AID583409Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate PA assessed as bacterial count at 16 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID528717Antibacterial activity against methicillin resistant Staphylococcus aureus clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID542903Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial regrowth at 200 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1151751Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 06052014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID542702fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg /day administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID326505Cmax in Enterococcus faecalis infected Wistar rat at 600 mg, po two consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID383568Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS 119 with G 2576T mutation by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID278929Antibacterial activity against Chlamydophila pneumoniae in HEp2 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID524979Antibacterial activity against Streptococcus intermedius clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID542699fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID555737Antibacterial activity against methicillin-resistant and vancomycin-resistant Staphylococcus aureus VRS1 by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID205679Minimum inhibitory concentration against Staphylococcus aureus MTCC 962004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID285056Antimicrobial activity against beta hemolytic Streptococcus group C at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID542715fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day administered as 6 divided doses every 4 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1427354Antibacterial activity against methicillin-resistant Staphylococcus aureus RKI 11-02670 after 18 hrs2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis.
AID1151754Antibacterial activity against penicillin-sensitive Streptococcus pneumoniae isolate 08062014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID323823Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, po after 5 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID520772Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 60 mg/kg, po administered every 8 hrs for 4 days measured on week 4 postinfection (Rvb = 2.43 +/- 0.15 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID520009Antimicrobial activity against Staphylococcus aureus A7819 harboring G2576U mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID558515Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID565228Antimicrobial activity against Mycobacterium chelonae ATCC 35752 by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID573138Antibacterial activity against erythromycin-susceptible Streptococcus agalactiae by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID576427Antibacterial activity against Enterococcus faecalis ATCC 29212 by agar dilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID285326Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 433002007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro activity of aurein 1.2 alone and in combination with antibiotics against gram-positive nosocomial cocci.
AID1390463Antibacterial activity against Staphylococcus aureus FDA 209P2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID541549Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID373311Antibacterial activity against Haemophilus influenzae clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID517669Antimicrobial activity against Enterococcus faecium NCTC 12201 by standard serial-dilution technique2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
AID303971Antibacterial activity against Staphylococcus aureus UC76 in po dosed CD1 mouse systemic infection model assessed as mortality after 7 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID511396Antibacterial activity against Streptococcus viridans by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID520004Antimicrobial activity against Ureaplasma urealyticum isolated from human respiratory tract by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID535008Antimicrobial activity against daptomycin-nonsusceptible Staphylococcus aureus by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID562249Antibacterial activity against Staphylococcus aureus NARSA NRS127 harboring rplC T433 to T435 and L3 Ser145 deletion mutant by CLSI broth microdilution assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID495879Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected New Zealand White rabbit aortic valve endocarditis model assessed as decrease in bacterial colony forming unit in spleen at 75 mg/kg, sc dosed every 8 hrs for 4 days (2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ceftobiprole is superior to vancomycin, daptomycin, and linezolid for treatment of experimental endocarditis in rabbits caused by methicillin-resistant Staphylococcus aureus.
AID285100Antimicrobial activity against viridans group Streptococcus mitis at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1676981Antimicrobial activity against Escherichia coli JW55031 harboring TolC mutant assessed as reduction in microbial growth after 48 hrs by CLSI based broth microdilution method
AID499167Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 25 mg/kg/day, po (Rvb = 0.8 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID541525Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID576645Bactericidal activity against 14 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID531569Antibacterial activity against Streptococcus sp. 'group C' obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID542714fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1151630Toxicity in female rat assessed as effect on reticulocyte count at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 1.48%)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID561089Antibacterial activity against Moraxella catarrhalis by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID533020Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-2 assessed as inhibition of bacterial growth in brain heart infusion broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID285053Antimicrobial activity against beta hemolytic Streptococcus group C at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID542707fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID729219Antibacterial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID561075Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID555306Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 051 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1596547Antibacterial activity against vancomycin resistant Staphylococcus aureus VRS10 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID1853455Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 700221 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID370024Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 12.5 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID283156Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2394 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1395987Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 planktonic cells after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID390322Antimicrobial activity against methicillin-resistant Staphylococcus aureus 433002008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID511435Antimicrobial activity against Streptococcus pneumoniae2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID533018Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-1 assessed as inhibition of bacterial growth in brain heart infusion broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1868233Antibacterial activity against Enterococcus faecium ATCC BAA-2317 assessed as inhibition of bacterial growth
AID576424Antibacterial activity against Enterococcus faecalis Ef1497 MutM3 by agar dilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID541805Antimicrobial activity against Enterococcus casseliflavus clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID545603Bacteriostatic activity against stationary-phase vancomycin-resistant Staphylococcus aureus isolate VRS5 grown on nutrient-depleted CAMHB medium at 8 ug/ml after 24 hrs by time kill analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID370035Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected in po dosed DBA/2 mouse localized infection model assessed as log reduction in CFU per gram of thigh at 5 mg/kg, po administered 2 hrs postinfection thrice daily for 12007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID559285Antimicrobial activity against recombination-deficient Enterococcus faecalis JH2-2 recA harboring nucleotides at position 2576 in rrlA 2576G, rrlB 2576G, rrlC 2576G and rrlD 2576T after 5 passages under Linezolid selective pressure by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID558486Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID520732Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid LI50 by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID533945Antimicrobial activity against Linezolid resistant hospital acquired methicillin-resistant Staphylococcus aureus SA238L after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1409843Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.1 mg, ip bid for 3.5 days administered 6 hrs post bacterial infection measured 84 hrs post infection relative to c2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID67752Minimum inhibitory concentration against Enterococcus faecalis ATCC 145062004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID278925Antibacterial activity against Haemophilus influenzae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID522914Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1808 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1684999Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as inhibition of bacterial growth incubated for 16 to 20 hrs by microdilution method2021ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
Enhancing Antimicrobial Peptide Potency through Multivalent Presentation on Coiled-Coil Nanofibrils.
AID726193Antibacterial activity against betalactamase positive Haemophilus influenzae by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID548527Antimicrobial activity against Oxacillin-susceptible coagulase-negative Staphylococcus by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID558722Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID533964Bacteriostatic activity against Staphylococcus epidermidis infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID283630Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4280-0258 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID531552Antibacterial activity against methicillin resistant Staphylococcus aureus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1862414Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID533421Antimicrobial activity against Anaerococcus prevotii by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID561235Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as intermediate isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1174908Antibacterial activity against linezolid-resistant methicillin-resistant Staphylococcus epidermidis by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID285115Antimicrobial activity against viridans group Streptococcus oralis at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID559560Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP7 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID541033Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 50 mg/kg after measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1862424Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1561) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID261064Antibacterial activity against Haemophilus influenzae HI35422006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
AID318361Antibacterial activity against efflux negative-tolC mutant containing Escherichia coli2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID410205Antibacterial activity against Enterococcus faecalis by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID1407930Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID373848Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 Hershey after 14 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID583199Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1760595Antibacterial activity against Methicillin resistant Staphylococcus aureus 43300 assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID209767Minimum inhibitory concentration against Streptococcus pyogenes MTCC 4422004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID1539450Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 12 after 18 to 20 hrs in aerobic condition by CLSI-based broth microdilution assay
AID206236In vitro antibacterial activity against Staphylococcus aures strain ATCC 292131996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID67401In vitro antibacterial activity against vancomycin-resistant Enterococcus faecalis C64872003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1421234Inhibition of recombinant human MAOA expressed in baculovirus infected Sf9 insect cells at 30 uM using luciferin derived substrate pretreated for 15 mins followed by substrate addition and measured after 60 mins by luminescence assay relative to control2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID566575Antimicrobial activity against methicillin-resistant Staphylococcus aureus 5 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID410209Antibacterial activity against vancomycin-resistant Enterococcus faecium by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID474998Antibacterial activity against Staphylococcus epidermidis LCB0003 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID1596568Bactericidal activity against vancomycin resistant Enterococcus faecalis ATCC 51299 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution as2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID323782Antimicrobial activity against bioluminescent methicillin-susceptible Staphylococcus aureus Xen292007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID524722Antibacterial activity against linezolid-resistant Enterococcus faecium 03B1073 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID541531Antimicrobial activity against Enterococcus faecalis clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1519271Antibacterial activity agianst methicillin-resistant Staphylococcus aureus2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID1578432Antimicrobial activity against cephalosporin-resistant Streptococcus pneumoniae ATCC 51916 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID552833Antibacterial activity against penicillin-resistant Streptococcus pneumoniae2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID383559Antibacterial activity against Enterococcus faecalis ATCC 35550 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID498885Antimicrobial activity against Pseudomonas aeruginosa OC 4351 assessed as inhibition of growth by broth microdilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1680071Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID519090Antimicrobial activity against Staphylococcus aureus RN4220 by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID717874Antibacterial activity against methicillin-resistant Staphylococcus aureus OM481 by two-fold liquid microdilution method2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Riccardin C derivatives as anti-MRSA agents: structure-activity relationship of a series of hydroxylated bis(bibenzyl)s.
AID1151743Antibacterial activity against Staphylococcus aureus measured after 5 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID528711Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus saprophyticus clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID555312Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID577097T>MIC in Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID565757Antimicrobial activity against oxacillin-susceptible Staphylococcus epidermidis clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1474196Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 18 to 22 hrs in absence of colistin by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID285000Antimicrobial activity against Enterococcus gallinarum at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID284900Antimicrobial activity against glycopeptide-intermediate Staphylococcus aureus by broth microdilution technique after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antimicrobial activities of ceragenins against clinical isolates of resistant Staphylococcus aureus.
AID1778666Ratio of MBC to MIC against penicillin-resistant Staphylococcus aureus2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID555297Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1703718Antibacterial activity against vancomycin-resistant Staphylococcus aureus 10 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID308917Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID1271227Antibacterial activity against clinical isolate Neisseria meningitidis E-63 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID369440Antimicrobial activity against vancomycin-resistant Enterococcus faecalis after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID572009Antibacterial activity against Fusobacterium mortiferum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1421238Stability in human liver microsomes assessed as parent compound remaining at 1.5 uM pretreated for 5 mins followed by NADPH addition measured after 45 mins by LC-MS analysis2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID285095Antimicrobial activity against viridans group Streptococcus intermedius at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID524972Antibacterial activity against Streptococcus pyogenes clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID283610Antimicrobial activity against Enterococcus faecalis 1 L2 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID583404Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate MI assessed as bacterial count at 8 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID566577Antimicrobial activity against Pseudomonas aeruginosa ATCC 9027 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID1243927Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA200 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID352921Antibacterial activity against Staphylococcus aureus C463 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID522897Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1014 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID522905Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1006 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1271206Solubility of compound at pH 7.4 by HPLC analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1474263Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 after 14 serial passages measured after 18 hrs by broth microdillution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID548739Antimicrobial activity against Oxacillin-susceptible coagulase-negative Staphylococcus assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID558512Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1167735Antimicrobial activity against Haemophilus influenzae by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID1435927Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRSA10 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID1519051Stability in human liver microsomes assessed as intrinsic clearance at 1.5 uM preincubated for 5 mins with NADPH and measured after 45 mins by LC/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID528731Antibacterial activity against penicillin intermediate Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID581025Inhibition of RNA synthesis in Staphylococcus epidermidis ATCC 23760 assessed as incorporation of [3H]uridine at 2 ug/ml by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID67565In vitro minimum inhibitory concentration against Enterococcus faecalis2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID1703707Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID410111Antimicrobial activity against vanA+ expressing Enterococcus faecalis A6349 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID519999Antimicrobial activity against Streptococcus pyogenes harboring mef(A) gene2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID262233Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 7006992006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID1547717Antibacterial activity against vancomycin-resistant Enterococcus faecalis 99 clinical isolate by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID571801Antibacterial activity against Clostridium celerecrescens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID208313Minimum inhibitory concentration measured against Streptococcus pneumoniae2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID565015Bactericidal activity against methicillin-susceptible coagulase-negative Staphylococcus simulans after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID571824Antibacterial activity against Colinsella aerofaciens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1764092Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 assessed as bacterial growth inhibition measured by two-fold serial microdilution method2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Synthesis, optimization, in vitro and in vivo study of bicyclic substituted amine as MenA inhibitor.
AID353058Antibacterial activity against vancomycin-resistant Enterococcus 1 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID283172Effect on biofilm formation of Staphylococcus lugdunensis assessed as percent non-biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID571815Antibacterial activity against Actinomyces naeslundii by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID442574Antibacterial activity against methicillin and vancomycin-resistant Staphylococcus aureus ATCC 29213 after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID429066Antiplasmodial activity after 120 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum.
AID577140Apparent volume of distribution in two-compartment pharmacokinetic/pharmacodynamic model at 400 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1680059Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 9 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID285133Antimicrobial activity against viridans group Streptococcus sanguinis at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1649287Antibacterial activity against Enterococcus faecium SR16972 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID374008Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID575271Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID1879689Antimycobacterial activity against drug susceptible Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method2022European journal of medicinal chemistry, Mar-15, Volume: 232Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
AID1520487Antibacterial activity against methicillin-resistant Staphylococcus aureus infected in Kunming mouse dosed subcutaneously at 0.5 and 4.0 hrs postinfection and measured at 7 to 14 days post treatment by Bliss method
AID210054Compound was evaluated for minimum inhibitory concentration against Streptococcus pneumoniae 9753 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID563320Antibacterial activity against vancomycin-susceptible Enterococcus faecalis EF 12704 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID71095In vitro antibacterial activity against Escherichia coli strain ATCC 259221996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1250833Antibacterial activity against methicillin-resistant Staphylococcus aureus incubated for 18 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent.
AID499165Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 1.6 mg/kg/day, po (Rvb = 0.8 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1591546Ratio of MBC for Staphylococcus aureus ATCC 25923 to MIC for Staphylococcus aureus ATCC 259232019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1269333Apparent permeability from apical to basolateral side in human Caco2 cells2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
AID1493807Antibacterial activity against Staphylococcus aureus VRS12 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1853456Antibacterial activity against Listeria monocytogenes ATCC 19115 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID1862430Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1649) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID1778648Antibacterial activity against vancomycin-susceptible Enterococcus faecalis ATCC19434 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID260739Antibacterial activity against Staphylococcus aureus smith2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID520773Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 60 mg/kg, po administered every 8 hrs for 4 days measured on week 6 postinfection (Rvb = 2.43 +/- 0.15 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID561513Antibacterial activity against Beta-hemolytic Streptococcus group B by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID373654Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 Michigan by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1271214Cmax in BALB/c mouse brain at 10 mg/kg, po by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1904083Antibacterial activity against Klebsiella pneumoniae BAA 21462022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID662301Antimycobacterial activity against Mycobacterium tuberculosis H37Rv grown in iron-deficient glycerol-alanine-salts media2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Syntheses and biological studies of novel spiropiperazinyl oxazolidinone antibacterial agents using a spirocyclic diene derived acylnitroso Diels-Alder reaction.
AID1873945Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 5% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID595022Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 433002011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
AID349308Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus clinical isolate after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID561264Antibacterial activity against Enterococcus faecalis assessed as resistant isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID560516Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 11b091 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID244872In vitro minimum inhibitory concentration against Enterococcus faecalis ATCC 292122005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID28199Plasma clearance in Male Sprague-Dawley Rat (25 mg/kg po); ND denotes not reported2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID303961Antibacterial activity against vancomycin-resistant Enterococcus faecalis MGH2 EF1 by microbroth technology2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID564822Bactericidal activity against methicillin-resistant Staphylococcus aureus after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1887614Synergistic antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as fractional inhibitory concentration incubated for 24 hrs in presence of artocarpin by checkerboard method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID373653Antimicrobial activity against community-acquired vancomycin-intermediate Staphylococcus aureus 504 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1578415Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS 385 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID524726Antibacterial activity against linezolid-resistant Enterococcus faecium 03B1078 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID561081Antibacterial activity against vancomycin-susceptible Enterococcus faecium by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID410107Antimicrobial activity against Haemophilus influenzae parent strain RD1 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID1703710Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS119 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID255574In vitro minimum inhibitory concentration against Streptococcus pneumoniae ATCC 6303 after incubation in air at 35 degree C for 24 hr using agar dilution method2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID571822Antibacterial activity against Bifidobacterium pseudolongum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1680037Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 10 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1873946Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 10% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID533975Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 33591 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1194832Antibacterial activity against methicillin-sensitive Staphylococcus aureus incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID511381Antibacterial activity against methicillin resistant coagulase negative Staphylococcus epidermidis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID533416Antimicrobial activity against Peptoniphilus asaccharolyticus assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID559286Antimicrobial activity against recombination-deficient Enterococcus faecalis JH2-2 recA harboring nucleotides at position 2576 in rrlA 2576G, rrlB 2576G, rrlC 2576G/T and rrlD 2576T after 6 passages under Linezolid selective pressure by agar dilution meth2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID533947Antimicrobial activity against community acquired methicillin-resistant Staphylococcus aureus NRS384 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID585160Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2499U mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID245403In vitro minimum inhibitory concentration against methicillin-resistant Staphylococcus epidermidis (ATCC 23760)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID308922Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS 119 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID245182Minimal inhibitory concentration against methicillin resistant Staphylococcus aureus ST4502004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID572011Antibacterial activity against Prevotella bivia by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1519038Antibacterial activity against linezolid-resistant Enterococcus faecalis assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID524945Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus cohnii clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID533941Antimicrobial activity against linezolid-resistant Enterococcus faecalis 412 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID520005Antimicrobial activity against Mycoplasma hominis isolated from human respiratory tract by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID373650Antimicrobial activity against methicillin-resistant Staphylococcus aureus by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID560213Antimicrobial activity against methicillin-resistant Staphylococcus aureus in mouse systemic infection model2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Molecular basis and phenotype of methicillin resistance in Staphylococcus aureus and insights into new beta-lactams that meet the challenge.
AID1308230Antibacterial activity against Staphylococcus haemolyticus ATCC 29970 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID542706fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1424067Antibiotic activity against methicillin-resistant Staphylococcus aureus isolate CAIRD142 by broth microdilution assay or Alamar blue dye based colorimetric assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
The Berkeleylactones, Antibiotic Macrolides from Fungal Coculture.
AID1898415Antibiofilm activity against methicillin-resistant vancomycin-resistant Enterococcus faecium ATCC 700221 biofilms assessed as biofilm eradication incubated for 24 hrs followed by incubation for 24 hrs in fresh medium by Calgary biofilm device assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
A Modular Synthetic Route Involving
AID368276Bactericidal activity against methicillin-resistant Staphylococcus aureus SA2 by microdilution technique2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID522903Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1004 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID583197Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate PA after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1393960Antibacterial activity against methicillin resistant Staphylococcus aureus BAA-1685 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID523027Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID196689tmax was evaluated in male Dawley rats at a dose of 25 mg/kg when taken perorally1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID582987Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0761 harboring MLST sequence type ST78 and pulsotype C expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1904921Antibacterial activity against Vancomycin-resistant Staphylococcus aureus 10 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1139107Antimicrobial activity against Staphylococcus aureus ATCC 29213 infected in Sprague-Dawley rat cyclophosphamide-induced neutropenic sepsis model assessed as host survival at 25 mg/kg, iv administered 1 hr before bacterial infection measured up to 120 hrs2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID561267Antibacterial activity against Enterococcus faecium assessed as intermediate isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID565078Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus 156 by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
AID474999Antibacterial activity against methicillin-resistant Staphylococcus epidermidis LCB0004 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID285145Antimicrobial activity against viridans group Streptococcus bovis by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID134122Protective dose of subcutaneously administered compound against intraperitoneally-induced septicaemia model (Staphylococcus aureus HT-17) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID574955Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19F by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1151703Antibacterial activity against Staphylococcus aureus by agar dilution method2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1167995Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 21/235 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID687494Cmax in rat at 10 mg/kg, iv2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID285081Antimicrobial activity against viridans group Streptococcus bovis at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID392201Antibacterial activity against Staphylococcus aureus UC-76 SA-1 by micro broth method2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents.
AID531557Antibacterial activity against coagulase-negative Staphylococcus hominis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID560574Bactericidal activity against vancomycin-susceptible Enterococcus faecalis ATCC 29212 assessed as change in bacterial count at 16 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID575042Cmax in patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID591665Antimicrobial activity against multidrug-resistant Moraxella catarrhalis after 18 hrs by agar dilution method2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
AID637970Antibacterial activity against Haemophilus influenzae ATCC 31517 after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID268866Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 122022006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis of novel tricyclic oxazolidinones by a tandem SN2 and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid.
AID571792Antibacterial activity against Clostridium hathewayi by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID516161Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolates assessed as resistant isolates by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID1862432Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1665) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID562387Antimicrobial activity against vancomycin-nonsusceptible Enterococcus faecalis clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID293551Antibacterial activity against Salmonella typhi MTCC 733 after 24 hrs by agar dilution assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Organoiodine(III) mediated synthesis of 3,9-diaryl- and 3,9-difuryl-bis-1,2,4-triazolo[4,3-a][4,3-c]pyrimidines as antibacterial agents.
AID1151722Bacteriostatic activity against vancomycin-resistant Enterococcus faecium2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID405631Toxicity in rabbit liver mitochondria assessed as inhibition of mitochondrial protein synthesis2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID583410Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate PA assessed as bacterial count at 32 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID318364Toxicity in human RBC assessed as drug level causing hemolysis2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID533408Antimicrobial activity against Clostridium tertium assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID542923Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial killing at 600 mg administered once every 24 hrs for 15 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID132092Tested for the dose to protect the mice from infection with Staphylococcus aureus OC 4172, by subcutaneous administration2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID519086Antimicrobial activity against Escherichia coli KM87-88 harboring Arg141Ser mutation in rplC gene by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID67386In vitro antibacterial activity against vancomycin-susceptible E. f. 034 (Enterococcus faecalis ATCC 29212)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Influence of ethylene-oxy spacer group on the activity of linezolid: synthesis of potent antibacterials possessing a thiocarbonyl group.
AID1151756Antibacterial activity against vancomycin-sensitive Enterococcus faecalis ATCC 292122014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID308914Antibacterial activity against Enterococcus faecalis ATCC 29212 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID562638Antimicrobial activity against Streptococcus mitis by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID575047Cmin in human intensive care unit patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID533970Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS18 infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID562248Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by CLSI broth microdilution assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID1574835Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID1390469Antibacterial activity against linezolid-resistant Staphylococcus aureus O-1282018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID565482Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method in presence of 50% human plasma2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID285315Antimicrobial activity against Leuconostoc spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID1168020Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 30/48 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1594377Antibacterial activity against AcrAB-TolC deficient Escherichia coli JW25113 after 18 to 24 hrs in absence of colistin by broth microdilution method2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID458450Antimicrobial activity against Bacillus subtilis ATCC 6633 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID278908Antibacterial activity against methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID577117ABBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID531572Antibacterial activity against Streptococcus mitis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID562168Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID405619Antibacterial activity against Enterococcus2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID1350035Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 6 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID533971Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA040 infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID278920Antibacterial activity against macrolide-resistant Streptococcus pyogenes2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID534786Antimicrobial activity against community-acquired methicillin-resistant Staphylococcus aureus by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID206449In vitro antibacterial activity against methicillin-resistant S. a. 019 (Staphylococcus aureus ATCC 33591 )2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Influence of ethylene-oxy spacer group on the activity of linezolid: synthesis of potent antibacterials possessing a thiocarbonyl group.
AID285048Antimicrobial activity against Enterococcus hirae by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID205584Compound was evaluated for minimum inhibitory concentration against Staphylococcus epidermidis 975 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID511305Antibacterial activity against methicillin resistant coagulase negative Staphylococcus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID1117387Antimicrobial activity against Pseudomonas aeruginosa K799/WT assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1269329Antimicrobial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 7 days by microbroth dilution method2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
AID519083Antimicrobial activity against Escherichia coli KM74 harboring U2500A mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID1861530AUC in Beagle dog at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID541090Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 during stationary growth phase by macrodilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID697274Antibacterial activity against linezolid-resistant Staphylococcus aureus ARC 3583 after 18 to 24 hrs by CLSI broth microdilution method2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
AID1117394Antimicrobial activity against Escherichia coli SG458 assessed as partially clear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID567489Antimicrobial activity against linezolid pretreated vancomycin-intermediate Staphylococcus aureus isolate 4 obtained from wound of patient by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Clinical outcomes by methicillin-resistant Staphylococcus aureus staphylococcal cassette chromosome mec type: isolates recovered from a phase IV clinical trial of linezolid and vancomycin for complicated skin and skin structure infections.
AID583195Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate NY after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID263963Antibacterial activity against vancomycin-susceptible Enterococcus faecalis DRCC 0342006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID206281In vitro antibacterial activity against Staphylococcus aureus (S. a.) ATCC 29213.1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1578414Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS384 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID285154Antimicrobial activity against viridans group Streptococcus vestibularis by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID572555Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis harboring gyrA D94A mutation by agar proportion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro activities of linezolid against clinical isolates of Mycobacterium tuberculosis complex isolated in Taiwan over 10 years.
AID1350030Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 1 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID569340Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by broth micro dilution technique2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID524982Antibacterial activity against Streptococcus sanguinis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID565007Bactericidal activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID571809Antibacterial activity against Clostridium sordellii by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID260743Antibacterial activity against Vancomycin resistant Enterococcus faecium VRE 7008022006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID285162Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID1400057Antibacterial activity against Escherichia coli ATCC 10798 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID303970Antibacterial activity against Streptococcus pyogenes C203 by micro-broth technology2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID565761Antimicrobial activity against Staphylococcus aureus clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1578418Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 12 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID558496Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID763953Antibacterial activity against Moraxella catarrhalis clinical isolate 112 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID319153Toxicity in rat at 20 mg/kg for 30 days2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID430948Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of protein synthesis at 8 times MIC treated 5 mins before [3H]leucine challenge measured after 30 mins by [3H]leucine incorporation assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Design, synthesis, and structure-activity relationships of benzophenone-based tetraamides as novel antibacterial agents.
AID571818Antibacterial activity against Bifidobacterium breve by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID208732Compound was evaluated for minimum inhibitory concentration against Streptococcus A 29 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID210361In vitro antibacterial activity against penicillin susceptible Streptococcus pneumoniae UC19912 (PSSP)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID523784Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID559558Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP6 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID562188Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 after 28 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1180574Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC1692-2F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID428279Antituberculosis activity against linezolid-resistant Mycobacterium tuberculosis having mutation in 23S rRNA with identical G to T base pair exchange at position 20612008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID373839Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 Michigan after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID575170Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose at 200 uM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID1421224Antibacterial activity against vancomycin-resistant Enterococcus faecium by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID558728Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 50 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID284973Antimicrobial activity against Corynebacterium pseudodiphtheriticum at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1304850Ratio of MIC for methicillin-resistant Staphylococcus aureus clinical isolate 2 in absence and presence of tiron2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID571797Antibacterial activity against Clostridium bartlettii by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID519991Antimicrobial activity against vancomycin-resistant Enterococcus faecalis nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1167992Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 7077 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID244887Minimal inhibitory concentration against Enterococcus faecium 6A-VRE2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID525131Antibacterial activity against Staphylococcus aureus KM183 after 18 to 24 hrs by broth microdilution method selected after 16 ug/ml drug exposure for 6 hrs by culture absorbance method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID560589Free fraction in healthy human male at 600 mg, po every 12 hrs by LC/MS/MS analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID410115Antimicrobial activity against Haemophilus influenzae 1100 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID1151712Antibacterial activity against methicillin-sensitive Staphylococcus aureus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID698976Antimycobacterial activity against Mycobacterium tuberculosis2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1180583Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC1692-1F to MIC for Staphylococcus aureus ARC16922014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID255748In vivo effective dose (on day 7-post-infection) against methicillin-resistant Staphylococcus aureus 562 infected mice upon peroral administration at 30 min and 4 hr post-infection2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID558488Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1161218Antimicrobial activity against Staphylococcus aureus ATCC 33591 in septicemia mouse model assessed as mortality of host at 5 mg/kg administered intragastrically measured after 14 days relative to control2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID209292Compound was evaluated for minimum inhibitory concentration against Streptococcus pyogenes 102 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID1596553Antibacterial activity against vancomycin resistant Staphylococcus aureus VRS11a assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID1616124Antimicrobial activity against Staphylococcus aureus ATCC 292132019European journal of medicinal chemistry, Nov-15, Volume: 182Recent advancements in mechanistic studies and structure activity relationship of F
AID260736Binding affinity to Bacillus subtilis DNA polymerase3C2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID244931Minimal inhibitory concentration against Enterococcus faecalis ATCC 292122004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID541543Antimicrobial activity against Enterococcus avium clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1596550Antibacterial activity against Staphylococcus aureus ATCC 6538 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID285040Antimicrobial activity against Corynebacterium amycolatum by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID387448Antibacterial activity against methicillin-susceptible Staphylococcus aureus DRCC 0352008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID531563Antibacterial activity against methicillin-resistant, oxacillin-susceptible, coagulase-negative, mecA-positive Staphylococcus lugdunensis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID262235Antibacterial activity against Enterococcus faecalis ATCC 145062006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID560812Apparent oral clearance in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID572001Antibacterial activity against Parabacteroides distasonis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID533014Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR5-1 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1168019Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 29/203 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID391591Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae IID553 by agar dilution method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials.
AID564825Antimicrobial activity against methicillin-susceptible Staphylococcus aureus assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID17942Absolute bioavailability was evaluated in male Dawley rats at a dose of 25 mg/kg when taken perorally1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID1861528AUC in Wistar rat at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID583408Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate PA assessed as bacterial count at 8 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID559555Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP5 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID565746Antimicrobial activity against vancomycin-susceptible Enterococcus faecium clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID278913Antibacterial activity against methicillin-susceptible coagulase-negative staphylococci2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID205559Minimum inhibitory concentration against Staphylococcus aureus ATCC 141542004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID575103Antimicrobial activity against Streptococcus pneumoniae serotype 23A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1553371Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 8235-4 measured after 16 hrs by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1243925Antimicrobial activity against methicillin-sensitive Staphylococcus aureus NRS72 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID759681Cytotoxicity against human HaCaT cells assessed as cell death at 200 to 400 ug/ml by MTT assay relative to control2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID1390482Antibacterial activity against Enterococcus faecium ATCC 356672018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID373313Antibacterial activity against vancomycin-resistant Enterococcus clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID531566Antibacterial activity against Enterococcus faecium obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID561233Antibacterial activity against methicillin-susceptible Staphylococcus aureus by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID645045Antibacterial activity against Escherichia coli ATCC 25922 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID83641The compound was evaluated for its anti-bacterial activity against Haemophilus influenzae UC 300631998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID520023Antimicrobial activity against Enterococcus faecalis A63432008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID564816Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID577138Total clearance in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID565484Bactericidal activity against methicillin-resistant Staphylococcus aureus after 24 hrs by M26-A method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID1852689Antibacterial activity against efflux pump lacking/recombinant OM pore producing Escherichia coli incubated for 24 hrs by twofold serial dilution method
AID303959Antibacterial activity against levofloxacin-oxacillin-resistant Staphylococcus aureus UC76 SA1 by micro-broth technology2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID576325Antibacterial activity against 10'4 to 10'5 CFU methicillin-resistant Staphylococcus aureus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID585169Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA G2032A, U2504G mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID1609287Antibacterial activity against methicilline-resistant Staphylococcus aureus NRS-119 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID573125Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID575266Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID519997Antimicrobial activity against Streptococcus pneumoniae ribosomal mutant2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID285352Decrease in Panton-Valentine leukocidin level in Staphylococcus aureus LUG855 in CCY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID571988Antibacterial activity against Ruminococcus lactaris by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1677784In-vivo antibacterial activity against Staphylococcus aureus infected in KM mouse model assessed as reduction in bacterial load in blood at 10 mg/kg, iv administered thrice daily and measured after 48 hrs2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID374011Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 18 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1327098Antibacterial activity against Staphylococcus aureus NCIM 2079 measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID533943Antimicrobial activity against linezolid-resistant Enterococcus faecalis 414 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID206463In vitro antibacterial activity against Staphylococcus aureus2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and antibacterial activity of oxazolidinone containing sulphonyl group.
AID571810Antibacterial activity against Clostridium spiroforme by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1327104Antitubercular activity against dormant stage Mycobacterium bovis BCG ATCC 35734 measured after 12 days by nitrate reductase assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID564812Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus haemolyticus after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID560820AUC (0 to 12 hrs) in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1547707Antibacterial activity against Staphylococcus aureus NRS119 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID1161217Antimicrobial activity against Staphylococcus aureus ATCC 33591 in septicemia mouse model assessed as mortality of host at 10 mg/kg administered intragastrically measured after 14 days relative to control2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID1205591Equilibrium solubility of the compound in phosphate buffer by LC-MS analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID572005Antibacterial activity against Bacteroides thetaiotaomicron by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID68067Antibacterial activity against ciprofloxacin resistant and linezolid-resistant Enterococcus faecium (EF4011 LinR;CipR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID523828Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 16 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID529681Antimicrobial activity against community-acquired methicillin-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Activities of ceftobiprole, linezolid, vancomycin, and daptomycin against community-associated and hospital-associated methicillin-resistant Staphylococcus aureus.
AID1430401Antibacterial activity against Staphylococcus epidermidis 209E after 24 to 48 hrs by macro-broth dilution method2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Methylsulfonyl benzothiazoles (MSBT) derivatives: Search for new potential antimicrobial and anticancer agents.
AID303960Antibacterial activity against levofloxacin-penicillin-resistant Streptococcus pneumoniae SV1 SP3 by microbroth technology2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID542886fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1193399Inhibition of recombinant Bacillus anthracis PurE assessed as change in melting temperature at 100 uM after 10 to 30 mins by high-throughput thermal shift screening2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID1883848Antibacterial activity against Mycobacterium tuberculosis Erdman in acute Mtb infection BALB/c mouse model assessed as reduction in log10 CFU in lungs at 100 mg/kg, po qd via gavage for 4 weeks2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID572021Antibacterial activity against Prevotella oralis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID528715Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus auricularis clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID208630Inhibitory activity against Streptococcus pneumoniae1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1770349Antibacterial activity against penicillin-resistant Staphylococcus epidermidis assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID637967Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID1584840Antibacterial activity against methicillin and vancomycin intermediate resistant Staphylococcus aureus MU50 after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID429422Antibacterial activity against Streptococcus pneumoniae by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID68242In vitro antibacterial activity against Enterococcus faecium C6301 (E.f.2).1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1390459Antibacterial activity against vancomycin-resistant Enterococcus faecium R12018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID289867Antibacterial activity against Enterococcus faecalis NCTC 122012007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
AID533397Antimicrobial activity against Clostridium paraputrificum by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID573867Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in po dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID583198Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate MI after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID531575Antibacterial activity against Bacillus spp. obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1151720Bacteriostatic activity against vancomycin-sensitive Enterococcus faecium2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1311364Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID1907630Antibacterial activity against Escherichia coli incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID1161138Antimicrobial activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID519989Antimicrobial activity against coagulase-negative Staphylococcus nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID523806Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID284978Antimicrobial activity against Corynebacterium striatum at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285148Antimicrobial activity against viridans group Streptococcus intermedius by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID561237Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID206305In vitro antibacterial activity against Staphylococcus aureus UC12673 (SA2)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID558711Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1304849Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 incubated for 16 hrs by broth microdilution method in presence of Fe2+2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1680006Induction of cytoplasmic membrane depolarization in Escherichia coli ATCC 25922 at 20 ug/ml measured for 12 mins by DiSC35 dye-based fluorescence assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID374590Antimicrobial activity against Bacillus pumilus MTCC 1456 after 24 hrs by agar dilution assay2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.
AID1174907Antibacterial activity against linezolid-sensitive methicillin-resistant Staphylococcus aureus by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID574078Ratio of fAUC (24 hrs) for Methicillin-susceptible Staphylococcus aureus ATCC 13709 infected po dosed mouse to MIC for Methicillin-susceptible Staphylococcus aureus ATCC 13702009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID520003Antimicrobial activity against Legionella pneumophila isolated from human respiratory tract by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID429426Antibacterial activity against Haemophilus influenzae isolate 280 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID529885Antibacterial activity against Staphylococcus aureus RN4220 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID1151714Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID558087Antimicrobial activity against Ureaplasma parvum isolated from human by two fold serial dilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
AID516165Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolates by CLSi method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID284986Antimicrobial activity against Enterococcus avium at 4 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID585171Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2055A, U2504G mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID1852699Selectivity ratio of IC50 for efflux pump lacking Pseudomonas aeruginosa to IC50 for efflux pump lacking/OM pore producing Pseudomonas aeruginosa
AID370017Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 6.25 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID566574Antimicrobial activity against methicillin-resistant Staphylococcus aureus 3 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID405139Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate assessed as percent susceptible isolates by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID533405Antimicrobial activity against Clostridium tertium by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID562165Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID368285AUC in rabbit plasma at 58 mg/kg after 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID524968Antibacterial activity against vancomycin-resistant and teichoplanin-susceptible Enterococcus faecalis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID255573In vitro minimum inhibitory concentration against Streptococcus pyogenes ATCC 19615 after incubation in air at 35 degree C for 24 hr using agar dilution method2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID542916Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial killing at 800 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID548740Antimicrobial activity against Oxacillin-resistant coagulase-negative Staphylococcus assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID13097Tmax of compound (25 mg/kg) after po administration was determined in Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID562623Antimicrobial activity against Coagulase-negative Staphylococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1327106Antibacterial activity against Escherichia coli NCIM 2688 at 10 ug/ml measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID387459Tmax in Swiss albino mouse at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID522888Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 555 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID548743Antimicrobial activity against Vancomycin-susceptible Enterococcus faecium assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID583886Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus isolate 156 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID1451769Antibacterial activity against Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 4.5 days treated 24 hrs prior to bacterial infection measured 108 hrs post infection relative to co2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID561243Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as intermediate isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID284939Antimicrobial activity against Aerococcus spp. at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID524984Antibacterial activity against penicillin susceptible Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID69612Antibacterial activity against Escherichia coli (OC 2530) (HS)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID1883681Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1312937Antimicrobial activity against methicillin-sensitive Staphylococcus aureus NRS72 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID283155Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL856 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1151767Antibacterial activity against vancomycin-sensitive Enterococcus faecalis ATCC 29212 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID717209Antimicrobial activity against methicillin-sensitive Staphylococcus aureus CCARM 0204 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID533635Antimicrobial activity against Propionibacterium sp. by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID572023Antibacterial activity against Sutterella wadsworthensis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1609266Antibacterial activity against Listeria monocytogenes ATCC 19111 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID558495Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1853459Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as reduction in colony forming unit incubated for 20 hrs2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID562626Antimicrobial activity against Group B Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID552832Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID1329447Antibacterial activity against linezolid-resistant Mycobacterium tuberculosis H37Rv in hollow-fiber infection model assessed as reduction in bacterial burden at 1116 mg, po at 24 hrs dose regimen measured after 3 weeks2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
From lead optimization to NDA approval for a new antimicrobial: Use of pre-clinical effect models and pharmacokinetic/pharmacodynamic mathematical modeling.
AID542691fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 400 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID562616Antimicrobial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID283392Antimicrobial activity against Nocardia otitidiscaviarum after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID573872Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 infected in iv dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID340858Antimicrobial activity against wild type vancomycin-intermediate resistant Staphylococcus aureus Mu50 by microdilution assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus.
AID373840Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 Michigan after 20 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID528842Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID571823Antibacterial activity against Catenibacterium mitsuokai by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID285327Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis ATCC 292122007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro activity of aurein 1.2 alone and in combination with antibiotics against gram-positive nosocomial cocci.
AID558519Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID565481Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID387460Cmax in Swiss albino mouse at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID573131Antibacterial activity against erythromycin-susceptible Streptococcus pyogenes by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1076830Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID555298Antibacterial activity against Tmp-susceptible coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID525127Suppression of drug resistance development in recA-deficient Staphylococcus aureus KB103 assessed as prolonged length of subculture to develop Linezolid resistance at 4 times MIC and 0.25 times IC50 after 20 days2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID206098In vitro antibacterial activity against Streptococcus2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and antibacterial activity of oxazolidinone containing sulphonyl group.
AID575272Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID541037Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 50 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID565752Antimicrobial activity against Enterococcus faecalis clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID352927Antibacterial activity against Streptococcus agalactiae ATCC 2901 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID565754Antimicrobial activity against oxacillin-susceptible Staphylococcus haemolyticus clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID520030Antimicrobial activity against Enterococcus faecium A6349 harboring G2576U mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1493801Antibacterial activity against Staphylococcus aureus RN4220 NRS107 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID555296Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1680069Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 1 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID285064Antimicrobial activity against beta hemolytic Streptococci group F at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID552831Antibacterial activity against glycopeptide-intermediate Staphylococcus aureus2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID558485Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID571998Antibacterial activity against Streptococcus anginosus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID560499Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 5zjsau3 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID449616Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID528729Antibacterial activity against multidrug-resistant Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID303911Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID583201Antimicrobial activity against vancomycin-intermediate Staphylococcus haemolyticus after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1151752Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 152014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1375988Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured after 1 week2016MedChemComm, Nov-01, Volume: 7, Issue:11
SAR and identification of 2-(quinolin-4-yloxy)acetamides as
AID523776Antimicrobial activity against linezolid-susceptible Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID519088Antimicrobial activity against Staphylococcus aureus KM164-165 harboring Gly155Arg mutation in rplC gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID583878Antibacterial activity against laboratory-derived Staphylococcus aureus ATCC 29213 harboring cfr-containing p42262 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID717211Antimicrobial activity against methicillin-sensitive Staphylococcus aureus CCARM 3640 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1151716Antibacterial activity against Staphylococcus saprophyticus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID353061Antibacterial activity against vancomycin-resistant Enterococcus 4 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID541835Antimicrobial activity against Streptococcus agalactiae clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1778654Antibacterial activity against penicillin-resistant Staphylococcus epidermidis assessed as inhibition of bacterial growth measured by broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID753122Antibacterial activity against Bacillus subtilis MTCC 121 assessed as growth inhibition after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID577123Tmax in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID30967Harmonic mean apparent terminal disposition half-life [t1/2beta (h)] in Male Sprague-Dawley Rat at dose 10 (mg/kg iv)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID326504Cmax in Enterococcus faecalis infected Wistar rat at single administration of 600 mg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID558719Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID584116Ratio of MIC for Escherichia coli KAM32 harboring cloned pSP72 lmrS to MIC for Escherichia coli KAM32 harboring pSP722010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.
AID763979Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1193405Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 measured after overnight incubation2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID1519053Inhibition of recombinant human MAO-A (active motif 31502) at 30 uM using luciferin as substrate incubated for 15 mins followed by substrate addition and measured after 60 mins by luminescence based method relative to control2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID531555Antibacterial activity against coagulase-negative Staphylococcus haemolyticus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1151719Bacteriostatic activity against vancomycin-sensitive Enterococcus faecalis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1337721Antibacterial activity against Staphylococcus aureus ATCC 29213 after 18 to 24 hrs by broth microdilution method2016European journal of medicinal chemistry, Nov-29, Volume: 124New isoxazolidinone and 3,4-dehydro-β-proline derivatives as antibacterial agents and MAO-inhibitors: A complex balance between two activities.
AID1778664Ratio of MBC to MIC against erythromycin-susceptible Staphylococcus aureus ATCC 259232021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID1193404Antimicrobial activity against Yersinia pestis BEI/ATCC A1122 measured after overnight incubation2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID1591543Antibacterial activity against Staphylococcus aureus clinical isolate incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID524955Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus capitis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID278915Antibacterial activity against linezolid-susceptible Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID523794Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID542917Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing at 800 mg administered as 4 divided doses every 6 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID576136Antibacterial activity against 10'4 to 10'5 CFU Enterococcus faecalis after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID207015Antibacterial activity against linezolid-resistant Staphylococcus aureus (SA1012 LinR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID1879692Antimycobacterial activity against PAS resistant Mycobacterium tuberculosis H37Rv harboring E153A mutant assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method2022European journal of medicinal chemistry, Mar-15, Volume: 232Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
AID533942Antimicrobial activity against linezolid-resistant Enterococcus faecalis 413 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID284969Antimicrobial activity against Corynebacterium jeikeium at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1434679Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3089 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID576860Bactericidal activity against 13 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID572013Antibacterial activity against Prevotella corporis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID576879Bactericidal activity against 14 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1367595Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by CLSI broth microdilution method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID533659Antimicrobial activity against Staphylococcus aureus RN42202008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID244929Antibacterial activity against Streptococcus pyogenes G-36 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID458451Antimicrobial activity against Micrococcus luteus ATCC 10240 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID542701fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day administered as 6 divided doses every 4 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID404937Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus sp. by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID1446760Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRSA4 after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1594373Antibacterial activity against Klebsiella pneumoniae ATCC BAA-1705 after 18 to 24 hrs in presence of colistin by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID244815Minimum inhibitory concentration against Staphylococcus aureus A150902005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
AID775549Antibacterial activity against Staphylococcus aureus Smith assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID206312In vitro antibacterial activity against Staphylococcus aureus strains UC12673, UC9213, ATCC 29213, and UC9271 (SA); range is 2-42003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID524985Antibacterial activity against penicillin intermediate Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID637980Antibacterial activity against Staphylococcus aureus ATCC 13709 after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID409582Antimicrobial activity against Enterococcus faecalis after 16 to 18 hrs by agar dilution method2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID560498Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at 16 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID285159Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID370037Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected in po dosed DBA/2 mouse localized infection model assessed as log reduction in CFU per gram of thigh at 5 mg/kg, iv administered 2 hrs postinfection thrice daily for 12007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1852690Antibacterial activity against efflux pump lacking/recombinant OM pore producing Pseudomonas aeruginosa incubated for 24 hrs by twofold serial dilution method
AID285006Antimicrobial activity against Enterococcus gallinarum at 4 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID535257Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-5 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1687311Antibacterial activity against wild type Escherichia coli BW25113 incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID373649Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID734687Antibacterial activity against Escherichia coli MTCC 739 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID1395972Antibacterial activity against methicillin-resistant Staphylococcus aureus 2 after 16 to 18 hrs by broth microdilution method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID560828AUC (0 to 24 hrs) in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID581019Inhibition of DNA synthesis in Staphylococcus aureus ATCC 25923 assessed as incorporation of [3H]thymidine at 2 ug/ml by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID564097Bactericidal activity against stationary-phase methicillin-resistant Staphylococcus aureus HUSA 304 after 24 hrs by time kill analysis in presence of 50 mg/L calcium ions2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID409579Antimicrobial activity against methicillin-susceptible Staphylococcus aureus after 16 to 18 hrs by agar dilution method2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID1311368Antibacterial activity against Mycobacterium tuberculosis 124R measured after 14 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID499163Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 25 mg/kg/day, po (Rvb = 1.6 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID558469Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID303967Bacteriostatic activity against Enterococcus after 48 hrs by time kill study2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID524951Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus simulans clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID555301Antibacterial activity against methicillin-susceptible Staphylococcus aureus 505 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1879690Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method2022European journal of medicinal chemistry, Mar-15, Volume: 232Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
AID283394Antimicrobial activity against Nocardia beijingensis after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID410202Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID524685Antibacterial activity against vancomycin-susceptible Enterococcus faecalis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID285342Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20020488 in Mueller-Hinton medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID429063Antiplasmodial activity after 48 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum.
AID571832Antibacterial activity against Ruminococcus albus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1904085Antibacterial activity against Escherichia coli MG16552022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID558477Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID522910Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1751 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID576885Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1327099Antibacterial activity against Escherichia coli NCIM 2688 measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID532782Antibacterial activity against vancomycin-susceptible Staphylococcus aureus NJ after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID572008Antibacterial activity against Bilophila wadsworthia by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID524683Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID548741Antimicrobial activity against Vancomycin-susceptible Enterococcus faecalis assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID285355Decrease in Panton-Valentine leukocidin level in community acquired methicillin-resistant Staphylococcus aureus HT20030203 in CYY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID528847Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID535773Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K carrying the luxAB gene under the hsp60 promoter agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID590153Antibacterial activity against methicillin-sensitive Staphylococcus aureus Smith infected po dosed ICR mouse assessed as protection against mouse mortality administered 1 hr after infection measured up to 7 days2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID561086Antibacterial activity against Streptococcus pyogenes by CLSI M7-A7 broth microdilution broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID542685fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID581042Ratio of IC50 for mammalian ribosomal activity to ribosomal activity in Escherichia coli S30 by coupled transcription/translation assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID533755Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus SA238 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID577112ABBC (0 to 24 hrs) in Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID558511Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID308727Antibacterial activity against Streptococcus pneumoniae SV1 SP3 by micro-broth method2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID576133Antibacterial activity against 10'4 to 10'5 CFU Moraxella catarrhalis after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID565019Bactericidal activity against methicillin-susceptible coagulase-negative Staphylococcus sciuri after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID630564Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 infected in NSA mouse neutropenic model administered orally 1 hour after infection measured 48 hrs post-treatment2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID285060Antimicrobial activity against beta hemolytic Streptococci group F at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1139108Antimicrobial activity against Staphylococcus aureus in rat thigh assessed as log reduction of CFU at 30 mg/kg, iv after 8 hrs2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID1312950Bactericidal activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID1710586Antibacterial activity against Staphylococcus epidermidis NRS101 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID565003Bactericidal activity against methicillin-susceptible coagulase-negative Staphylococcus hominis after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1778653Antibacterial activity against Staphylococcus aureus assessed as inhibition of bacterial growth measured by broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID285147Antimicrobial activity against viridans group Streptococcus gordonii by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1154476Antibacterial activity against of methicillin-resistant Staphylococcus aureus ATCC 33591 infected in iv dosed neutropenic mouse administered 1 hr after infection measured after 24 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID1873892Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^3 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID584114Antibacterial activity against Escherichia coli KAM32 harboring Staphylococcus aureus cloned pSP72 lmrS by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.
AID561090Antibacterial activity against Bacteroides fragilis by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID406623Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae isolates assessed as percent resistant isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.
AID1677798Bactericidal activity against penicillin-resistant Staphylococcus aureus assessed as reduction in number of colony forming units incubated for 24 hrs followed by re-plating and reincubation on tryptic soy agar plate for 24 hrs2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID528735Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus capitis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1197120Antibacterial activity against vancomycin/methicillin-resistant Staphylococcus aureus VRS2 clinical isolate after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID687496Half life in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID531551Antibacterial activity against Staphylococcus aureus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1603254Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay
AID449619Antibacterial activity against Streptococcus pneumoniae by agar dilution method2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID499168Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 100 mg/kg/day, po (Rvb = 0.8 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID262229Antibacterial activity against Staphylococcus aureus ATCC 259232006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID756095Antibacterial activity against methicillin-sensitive Staphylococcus aureus assessed as growth inhibition after 16 hrs by agar dilution method2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
AID542703fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1151724Bactericidal activity against penicillin-sensitive Streptococcus pneumoniae2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1873908Antibacterial activity against Cronobacter sakazakii ATCC 29544 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID545813Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate VRS5 assessed as inhibition of biofilm formation after 24 hrs by by serial dilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID285118Antimicrobial activity against viridans group Streptococcus oralis with G2576T rRNA mutation at 4 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID523801Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1770341Antibacterial activity against erythromycin-susceptible Staphylococcus aureus ATCC 25923 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID519986Antimicrobial activity against Streptococcus pneumoniae nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID519996Antimicrobial activity against Streptococcus pneumoniae harboring mef(A) gene2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1687316Antibacterial activity against Pseudomonas aeruginosa ATCC 15442 incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1446756Antibacterial activity against methicillin-resistant Staphylococcus aureus USA200 NRS383 clinical isolate after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1879693Antimycobacterial activity against PAS resistant Mycobacterium tuberculosis H37Rv harboring S150G mutant assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method2022European journal of medicinal chemistry, Mar-15, Volume: 232Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
AID285374Half life for simulated intermittent-dosage regimen at 120 mg every 12 hrs using in vitro PK/PD model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID41245Antibacterial activity against Bacteroides fragilis UC121991998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID528973Antimicrobial activity against methicillin-resistant Staphylococcus aureus assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID573119Antibacterial activity against coagulase-negative and oxacillin-susceptible Staphylococcus aureus by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1710574Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS 119 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID560797Absorption rate constant in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1437031Antimycobacterial activity against isoniazid/rifampicin/kanamycin/streptomycin/ofloxacin/moxifloxacin/levofloxacin-resistant Mycobacterium tuberculosis by microplate Alamar Blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis.
AID326284Antibacterial activity against methicillin-resistant Staphylococcus aureus 5004 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID373996Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 21 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1400028Inhibition of protein translation/transcription in Escherichia coli S30 cell extract at 0.1 ug/ml using circular DNA with pBESTluc after 60 mins by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID571997Antibacterial activity against Peptostreptococcus micros by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID467835Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 70069 after 24 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
AID520006Antimicrobial activity against Chlamydia trachomatis isolated from human respiratory tract by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID555293Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID524978Antibacterial activity against Streptococcus constellatus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID565759Antimicrobial activity against oxacillin-resistant Staphylococcus aureus clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID574953Antimicrobial activity against Streptococcus pneumoniae serotype 6C by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID520770Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as bacterial count per gram of tibial marrow at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 8 pos2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID522909Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1743 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID533954Antimicrobial activity against Legionella pneumophila ATCC 33153 after 48 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID561257Antibacterial activity against Streptococcus agalactiae by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1692899Antibacterial activity against hospital acquired methicillin-resistant Staphylococcus aureus clinical isolates2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID1168006Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 28/211 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1437033Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis by microplate Alamar Blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis.
AID318356Antibacterial activity against vancomycin-intermediate resistant Staphylococcus aureus2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID558492Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID285072Antimicrobial activity against viridans group Streptococcus anginosus at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID559287Antimicrobial activity against recombination-deficient Enterococcus faecalis JH2-2 recA harboring nucleotides at position 2576 in rrlA 2576G, rrlB 2576G, rrlC 2576T and rrlD 2576T after 7, 8, 9 passages under Linezolid selective pressure by agar dilution 2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID285085Antimicrobial activity against viridans group Streptococcus constellatus at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1361100Bacteriostatic activity against methicillin-resistant Staphylococcus aureus USA500 NRS385 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID1056341AUC (infinity) in ICR mouse at 67.7 mg/kg, po by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1519269Antibacterial activity agianst methicillin-resistant Staphylococcus aureus clinical isolates2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID1547710Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS2 clinical isolate by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID28087Cmax value in Male Sprague-Dawley Rat at dose 25 (mg/kg po)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID542711fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1721015Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID562382Antimicrobial activity against vancomycin-nonsusceptible Enterococcus faecium clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1578413Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS123 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID245095In vitro minimum inhibitory concentration against Pseudomonas aeruginosa (ATCC 27853)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID283609Antimicrobial activity against Enterococcus faecalis Ho 4450-0446 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID285508Antibacterial activity against Streptococcus pneumoniae by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID519087Antimicrobial activity against Escherichia coli KM89-94 harboring G2576U mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID528976Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID246859Antibacterial activity against Staphylococcus aureus was evaluated in infected mice2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
AID285319Antimicrobial activity against Nocardis brasiliensis by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID528701Antibacterial activity against Streptococcus viridans clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID573147Antibacterial activity against penicillin-nonsusceptible Streptococcus viridans assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID533983Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus ATCC 33591 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1167996Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 5642 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1361101Bacteriostatic activity against methicillin-resistant Staphylococcus aureus USA700 NRS386 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID630554Antibacterial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID429425Antibacterial activity against Haemophilus influenzae ATCC 49247 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID576418Volume of distribution at steady state in two-compartment pharmacokinetic/pharmacodynamic model at 400 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID323821Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, po after 3 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID571830Antibacterial activity against Ruminococcus gnavus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID571798Antibacterial activity against Clostridium beijerinckii by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID566581Antimicrobial activity against Staphylococcus saprophyticus ATCC 15305 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID511394Antibacterial activity against Streptococcus pyogenes by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID528719Antibacterial activity against vancomycin resistant Enterococcus faecium VanA clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID564834Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus hominis assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID576889Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1692907Antibacterial activity against hospital acquired linezolid-resistant Enterococcus faecalis clinical isolates2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID558471Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1852668Antibacterial activity against multidrug resistant Pseudomonas aeruginosa BAA 2109 assessed as inhibition of bacterial growth incubated for 24 hrs in MP-MOPS medium by twofold serial dilution method
AID373750Antimicrobial activity against mupirocin-resistant methicillin-resistant Staphylococcus aureus assessed as resistant rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID1361108Bactericidal activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID292901Antimicrobial activity against staphylococcus aureus by broth dilution method2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.
AID442653Antibacterial activity against Streptococcus pyogenes after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID522889Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1287 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1852667Antibacterial activity against multidrug resistant Klebsiella pneumoniae ATCC13883 assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID285039Antimicrobial activity against Corynebacterium spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID348595Antibacterial activity against coagulase negative Staphylococcus after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID1151727Antibacterial activity against Streptococcus agalactiae2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID283620Antimicrobial activity against Enterococcus faecium 31 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID373842Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 Michigan after 18 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID558510Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID671562Antibacterial activity against Streptococcus pneumoniae SPN1602012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID516168Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolates assessed as susceptible isolates by EUCAST method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID1337722Antibacterial activity against Enterococcus faecalis ATCC 29212 after 18 to 24 hrs by broth microdilution method2016European journal of medicinal chemistry, Nov-29, Volume: 124New isoxazolidinone and 3,4-dehydro-β-proline derivatives as antibacterial agents and MAO-inhibitors: A complex balance between two activities.
AID1616125Antimicrobial activity against Streptococcus pneumoniae ATCC 496192019European journal of medicinal chemistry, Nov-15, Volume: 182Recent advancements in mechanistic studies and structure activity relationship of F
AID561342Antibacterial activity against Beta-hemolytic Streptococcus group A by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1904086Antibacterial activity against Enterobacter cloacae ATCC 130472022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID532784Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1151730Antibacterial activity against Streptococcus constellatus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID559371Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP3 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID571825Antibacterial activity against Coprobacillus cateniformis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID561239Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as intermediate isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID576138Antibacterial activity against 10'4 to 10'5 CFU methicillin-resistant coagulase-negative Staphylococcus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1151715Antibacterial activity against Staphylococcus haemolyticus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID285329Antimicrobial activity against Streptococcus pyogenes ATCC 196152007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro activity of aurein 1.2 alone and in combination with antibiotics against gram-positive nosocomial cocci.
AID267721Antimicrobial activity against Streptococcus pneumoniae2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings.
AID1649284Antibacterial activity against Enterococcus faecalis SR1004 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID278914Antibacterial activity against methicillin-resistant coagulase-negative staphylococci2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID555308Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 074 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID285546AUC (0-24 hrs) in mouse at 50 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID1744562Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID511395Antibacterial activity against Streptococcus agalactiae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID560515Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 13b16 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID206234Minimum inhibitory concentration against Staphylococcus epidermis UC120841998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID555507Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 197 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID567488Antimicrobial activity against vancomycin pretreated vancomycin-intermediate Staphylococcus aureus isolate 3 obtained from wound of patient by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Clinical outcomes by methicillin-resistant Staphylococcus aureus staphylococcal cassette chromosome mec type: isolates recovered from a phase IV clinical trial of linezolid and vancomycin for complicated skin and skin structure infections.
AID573128Antibacterial activity against penicillin-resistant Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1603311Antimicrobial activity against Acinetobacter baumannii ATCC 19606 measured after 16 hrs by broth microdilution method2019ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3
Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics.
AID555513Antibacterial activity against methicillin-resistant, Linezolid non-susceptible coagulase-negative Staphylococcus epidermidis 345 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID308924Antibacterial activity against methicillin-resistant Streptococcus pyogenes ATCC 14289 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID523785Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID645040Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID1778651Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth by broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID424759Antibacterial activity against macrolide-sensitive, Linezolid, methicillin-resistant Staphylococcus aureus CL5814 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID577139Apparent volume of distribution in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1594371Antibacterial activity against Acinetobacter baumannii BAA1605 after 18 to 24 hrs in presence of colistin by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID245286Minimum inhibition concentration against Staphylococcus aureus strains in presence of 2% calf serum2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Biaryl isoxazolinone antibacterial agents.
AID1272263Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 after 18 to 20 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.
AID558086Antimicrobial activity against Mycoplasma hominis isolated from human by two fold serial dilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
AID717215Antimicrobial activity against methicillin-resistant Staphylococcus aureus CCARM 3635 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID576137Antibacterial activity against 10'4 to 10'5 CFU Streptococcus pyogenes after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1197123Antibacterial activity against Streptococcus oralis ATCC 9811 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1435922Antibacterial activity against methicillin/ciprofloxacin/gentamicin/clindamycin-resistant Staphylococcus aureus USA200 NRS383 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID1770358Bactericidal activity against penicillin-resistant Staphylococcus aureus ATCC 31007 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID519486Antibacterial activity against Staphylococcus aureus T1888 expressing 23S rrn 3 G2576T and rrn 5 G2576T mutants by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID558505Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID763950Antibacterial activity against Moraxella catarrhalis clinical isolate 255 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID535036Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-403 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1547704Antibacterial activity against Staphylococcus aureus ATCC 27660 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID292614Antimicrobial activity against Haemophilus influenzae ATCC 49247 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID1519052Stability in human liver microsomes assessed as compound remaining at 1.5 uM preincubated for 5 mins with NADPH and measured after 45 mins by LC/MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID532809Antibacterial activity against vancomycin-susceptible Staphylococcus aureus BR3 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID697275Antibacterial activity against vancomycin-resistant Staphylococcus aureus ARC 3186 after 18 to 24 hrs by CLSI broth microdilution method2012Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
AID1407931Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs in presence of 2% human albumin by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID383567Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID520484Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 30 mg/kg, sc administered every 12 hrs for 4 days measured on week 2 postinfection (Rvb = 2.84 +/- 0.30 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID533409Antimicrobial activity against Finegoldia magna by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID278857Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID520512Cmin in New Zealand rabbit osteomyelitis model at 40 mg/kg, sc administered every 6 hrs for 4 days2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID633447Bacteriostatic activity against Staphylococcus aureus ATCC 01001 infected in thigh of CD1 mouse assessed as prevention of colony formation at 80 mg/kg, po administered 2 hrs post infection measured after 12 hrs2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.
AID524693Antibacterial activity against Corynebacterium sp. by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID571817Antibacterial activity against Bifidobacterium bifidum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1407937Antifungal activity against Candida albicans ATCC 90028 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID1493808Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID405617Antibacterial activity against Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID68065Antibacterial activity against ciprofloxacin resistant Enterococcus faecium (EF4016 CipR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID577115ABBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID94375In vitro antibacterial activity against Klebsiella pneumoniae strain UC 120811996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID319165Nonrenal clearance in human2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1501358Antibacterial activity against methicillin-resistant Staphylococcus aureus USA100 NRS382 after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID207796Compound was evaluated for minimum inhibitory concentration against Staphylococcus aureus 975 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID763986Antibacterial activity against methicillin-susceptible Staphylococcus aureus after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1692402Antibacterial activity against methicillin and linezolid resistant Staphylococcus aureus NRS119 assessed as reduction in bacterial growth incubated for 18 to 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Aug-15, Volume: 200Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting d-alanyl-d-alanine ligase in bacterio.
AID1877890Antibacterial activity against wild type Escherichia coli DSM-11116 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID559283Antimicrobial activity against Enterococcus faecalis JH2-2 harboring nucleotides at position 2576 in rrlA 2576T, rrlB 2576G, rrlC 2576T and rrlD 2576T after 9, 10, 11 passages under Linezolid selective pressure by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID1400758Bactericidal activity against methicillin-resistant Staphylococcus aureus isolate 2 after 24 hrs by calgary biofilm device-based assay2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID1680002Resistance ratio of compound MIC for methicillin-resistant Staphylococcus aureus after 20 passages to compound MIC for methicillin-resistant Staphylococcus aureus after 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1303406Antibacterial activity against Escherichia coli after 24 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID519489Antibacterial activity against Staphylococcus aureus T2019 expressing 23S rrn1 G2576T, rrn2 G2576T, rrn3 G2576T, rrn4 G2576T and rrn5 G2576T mutants by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID559281Antimicrobial activity against Enterococcus faecalis JH2-2 harboring nucleotides at position 2576 in rrlA 2576T, rrlB 2576G, rrlC 2576G and rrlD 2576T after 5 passages under Linezolid selective pressure by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID525148Antimicrobial activity against Staphylococcus epidermidis isolate 426-3147L expressing cfr gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID1680063Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 3 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID560507Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b2k3421 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID424769Antibacterial activity against penicillin-resistant Streptococcus pneumoniae CL5771 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID531556Antibacterial activity against coagulase-negative Staphylococcus lugdunensis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1649295Antibacterial activity against Klebsiella pneumoniae SR1 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID275461Antibacterial activity against vancomycin-sensitive Staphylococcus aureus F9886332007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID531554Antibacterial activity against coagulase-negative Staphylococcus epidermidis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1241208Inhibition of pre-miR-21 (unknown origin) cleavage assessed as reduction of oncogenic microRNAs biogenesis by measuring fluorescence every minute for 5 hrs using 5'-FAM,3'-dabcyl-pre-miRNA beacons by FRET assay in presence of recombinant Dicer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID532813Antibacterial activity against vancomycin-intermediate Staphylococcus aureus MI phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID283177Increase in biofilm formation of Staphylococcus epidermidis RP62A at 0.25 times MIC2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID562381Antimicrobial activity against Enterococcus faecium expressing VanA gene clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID590151Antibacterial activity against methicillin-resistant Staphylococcus aureus Smith infected po dosed ICR mouse assessed as protection against mouse mortality administered 1 hr after infection measured up to 7 days2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1861518Antibacterial activity against methicillin-sensitive Staphylococcus aureus Sta-001 incubated for 18 hrs by CLSI protocol based two-fold serial agar dilution method2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID571996Antibacterial activity against Peptostreptococcus anaerobius by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID278927Antibacterial activity against Legionella pneumophila2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1862426Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1568) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID524983Antibacterial activity against Streptococcus sp. clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1852691Antibacterial activity against Escherichia coli SQ110 DTC G2032A incubated for 24 hrs by twofold serial dilution method
AID206224In vitro antibacterial activity against methicillin resistant Staphylococcus epidermis US 12084 (MRSE)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID410105Antimicrobial activity against erm (B) expressing Streptococcus pyogenes Msr 610 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID523803Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 4 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1139114Antimicrobial activity against Streptococcus pneumoniae infected in rat lung infection model assessed as log reduction of bacterial density at 3 mg/kg, po2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID577111ABBC (0 to 24 hrs) in Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1703726Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1721061Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in Balb/c mouse assessed as reduction in lung bacterial burden at 50 to 100 mg/kg/day, po administered via gavage 5 times per week for 3 weeks starting from 10 days post-infection a2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID523809Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID726196Antibacterial activity against penicillin-resistant Streptococcus pneumoniae C402 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID1421233Antibacterial activity against linezolid-resistant Enterococcus faecalis clinical isolates by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID284954Antimicrobial activity against Bacillus cereus at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1611120Antibacterial activity against methicillin-sensitive Staphylococcus aureus CLSI-based double dilution method2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
AID319149Oral bioavailability in rat at 25 mg/kg2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1117377Antimicrobial activity against Staphylococcus aureus Efs4 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID370012Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 12.5 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID583883Antibacterial activity against laboratory-generated cfr-transformed Staphylococcus aureus by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID1126487Antimicrobial activity against methicillin-resistant Staphylococcus aureus2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID1400030Inhibition of protein translation/transcription in Escherichia coli S30 cell extract using circular DNA with pBESTluc after 60 mins by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID576898Ratio of AUC (0 to 24 hrs) to MIC for Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1853458Bactericidal activity against methicillin-resistant Staphylococcus aureus USA300 assessed as reduction in colony forming unit incubated for 20 hrs2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID528696Antibacterial activity against methicillin resistant Staphylococcus aureus MED 2028 osteomyelitis isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID531644Displacement of [3H]chloramphenicol from 70S ribosomal complex in Staphylococcus aureus ATCC 29213 by competitive binding assay2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID1400044Antibacterial activity against Staphylococcus aureus BAA 44 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID541522Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1327100Antibacterial activity against Bacillus subtilis NCIM 2010 measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID103859Inhibitory activity against Moraxella catarrhalis UC306102000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID577090Ratio of AUC (0 to 24 hrs) to MIC for Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1056339Inhibition of human CYP1A2 assessed as ethoxyresorufin O-deethylation after 20 mins by fluorescence plate reader2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID287267Antimicrobial activity against Escherichia coli ATCC 259222007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID285090Antimicrobial activity against viridans group Streptococcus gordonii at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1151759Antibacterial activity against Streptococcus pyogenes isolate 5562014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID520733Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid MS2 by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID1519273Antibacterial activity agianst Staphylococcus aureus ATCC 292132019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID410224Antibacterial activity against Haemophilus influenzae by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID535019Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-4 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1451776Antibacterial activity against Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 4.5 days treated 24 hrs prior to bacterial infection measured 108 hrs post infection relative to 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID245296In vitro minimum inhibitory concentration of compound against Methicillin-sensitive Staphylococcus aureus ATCC 292132005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID542709fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg /day administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1721018Stability in CD-1 mouse liver microsome at 1 uM measured after 30 mins in absence of NADPH by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1174904Antibacterial activity against methicillin-resistant Staphylococcus aureus MRSA M923 by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID285117Antimicrobial activity against viridans group Streptococcus oralis at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID562385Antimicrobial activity against Enterococcus faecalis expressing VanB gene clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID541038Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 75 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID577106AUBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID284984Antimicrobial activity against Enterococcus avium at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1151725Bactericidal activity against penicillin-resistant Streptococcus pneumoniae2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID552829Antibacterial activity against methicillin-sensitive Staphylococcus aureus2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID581038Induction of bacterial membrane damage in Staphylococcus aureus ATCC 25923 at 4 ug/mL by BacLight assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID533965Bacteriostatic activity against Listeria monocytogenes EGD infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1778663Bactericidal activity against penicillin-resistant Staphylococcus epidermidis measured after 24 hrs by CLSI protocol based method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID532806Antibacterial activity against vancomycin-susceptible Staphylococcus aureus 28160 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1233142Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID424421Antibacterial activity against Enterococcus faecalis HIP14333 isolated from patients rectum by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID523779Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID245238In vitro minimum inhibitory concentration against Enterococcus faecalis (ATCC 29212 and 21777)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID349307Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus clinical isolate after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID542906Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial regrowth at 500 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1539457Antibacterial activity against methicillin-resistant Streptococcus pneumoniae ATCC 700677 clinical isolates after 18 to 20 hrs by CLSI-based broth microdilution assay
AID285051Antimicrobial activity against Micrococcus luteus by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID304003Toxicity in Sprague-Dawley rat at 1000 mg/kg/day, po after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID373319Antibacterial activity against Haemophilus influenzae ATCC 49247 after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID1862420Antibacterial activity against Listeria monocytogenes ATCC 19115 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID581666Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU level after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID541081Cmax in cage fluid of Albino guiena pig at 50 mg/kg, ip after 3 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID558484Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID520007Antimicrobial activity against Chlamydophila pneumoniae isolated from human respiratory tract by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID576640Bactericidal activity against 1 hr peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID565012Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus simulans after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID561261Antibacterial activity against Enterococcus faecalis by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1474217Bacteriostatic activity against vancomycin-resistant Enterococcus faecium ATCC 700221 assessed as reduction in CFU at 4 times MIC after 24 hrs2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID560371Antimicrobial activity against vancomycin-resistant Enterococcus faecalis 1058946 by broth dilution method in presence of 4% HSA2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1853452Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID1390471Antibacterial activity against Staphylococcus epidermidis ATCC 122282018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID278921Antibacterial activity against Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID528692Antibacterial activity against Streptococcus agalactiae MED 2038 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1311360Antibacterial activity against Acinetobacter baumannii ACBA measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID285120Antimicrobial activity against viridans group Streptococcus parasanguis at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID572022Antibacterial activity against Prevotella oris by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID207510Minimum inhibitory concentration against Staphylococcus aureus UC66851998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID591664Antimicrobial activity against multidrug-resistant Haemophilus influenzae after 18 hrs by agar dilution method2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
AID524986Antibacterial activity against penicillin resistant Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID262231Antibacterial activity against Staphylococcus aureus ATCC 141542006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID370028Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in iv dosed C3H mouse localized infection model assessed as reduction of number of CFU per gram of kidney administered 15 mins after infection measured after 48 hr2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID535024Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-23 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID534793Bactericidal activity against community-acquired methicillin-resistant Staphylococcus aureus assessed as antibiotic concentration that reduced the number of viable cells by =>99.9% by colony count method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1861536Volume of distribution in Beagle dog at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID345135Antimicrobial activity against Streptococcus pneumoniae 02J1175 expressing mef(A) gene by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
AID285151Antimicrobial activity against viridans group Streptococcus parasanguis by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID201444Inhibitory activity against Methicillin-resistant Staphylococcus epidermidis UC120842000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID559280Antimicrobial activity against Enterococcus faecalis JH2-2 harboring nucleotides at position 2576 in rrlA 2576G, rrlB 2576G, rrlC 2576G and rrlD 2576T after 4 passages under Linezolid selective pressure by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID535255Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-3 expressing SCCmec type 4 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID583388Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate MU50 assessed as bacterial count at 8 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID285506Antibacterial activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID283612Antimicrobial activity against Enterococcus faecalis 37 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID285387Area under population analysis profile for vancomycin-intermediate Staphylococcus aureus Mu50 using in vitro PK/PD model relative to growth control with 120 mg/24 hrs continuous infusion regimen after 72 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID531577Antibacterial activity against Gemella spp. obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID576139Antibacterial activity against 10'4 to 10'5 CFU Streptococcus pneumoniae after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID524943Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID311484Antimicrobial activity against Haemophilus influenzae ATCC 49766 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID373800Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 504 after 22 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID511392Antibacterial activity against Levofloxacin susceptible Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID559797Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at 0.125 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID645041Antibacterial activity against Staphylococcus aureus ATCC 43300 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID1400750Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 2 after 16 to 18 hrs by broth microdilution method2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID318358Antibacterial activity against vancomycin-resistant Enterococcus faecium2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID524949Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus saprophyticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID571831Antibacterial activity against Ruminococcus obeum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID206610In vitro antibacterial against methicillin-susceptible Staphylococcus aureus (MSSA)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1407936Antibacterial activity against Enterococcus faecalis ATCC 29212 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID531641Antimicrobial activity against Enterococcus faecalis ATCC 292122008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID210051Antibacterial activity against Streptococcus pneumoniae UC99121998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID1898409Antibiofilm activity against methicillin-resistant Staphylococcus aureus BAA-1707 biofilms assessed as biofilm eradication incubated for 24 hrs followed by incubation for 24 hrs in fresh medium by Calgary biofilm device assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
A Modular Synthetic Route Involving
AID561077Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID542913Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing followed by emergence of resistance between 4 to 8 days at 500 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID575045Nonrenal clearance in healthy human at 600 mg, po2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID424757Antibacterial activity against methicillin-sensitive Staphylococcus aureus MB2865 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID555305Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS1 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1861532Terminal half life in Wistar rat at 30 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID283171Decrease in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1594069Antibacterial activity against Staphylococcus aureus assessed as reduction in bacterial cell viability incubated for 20 to 24 hrs by REMA method2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Design, synthesis, in-silico studies and biological screening of quinazolinone analogues as potential antibacterial agents against MRSA.
AID524970Antibacterial activity against vancomycin- and teichoplanin-nonsusceptible Enterococcus faecium clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID587297Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 4 weeks by microplate alamar blue assay2011European journal of medicinal chemistry, Mar, Volume: 46, Issue:3
Anti-tubercular agents. Part 6: synthesis and antimycobacterial activity of novel arylsulfonamido conjugated oxazolidinones.
AID1361110Bactericidal activity against methicillin-resistant Staphylococcus aureus USA700 NRS386 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID1168007Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 151495 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1687314Antibacterial activity against Acinetobacter baumannii ATCC 19606 incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1873888Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^7 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID581015Inhibition of protein synthesis in Staphylococcus aureus ATCC 25923 assessed as incorporation of [14C]isoleucine at 2 ug/ml by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID1056343Cmax in ICR mouse at 67.7 mg/kg, po by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1271225Antibacterial activity against linezolid-resistant Streptococcus pneumoniae 6303 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID285323Antimicrobial activity against Nocardia spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID559783Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at 0.125 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1395680Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS10 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID564095Bactericidal activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 after 24 hrs by time kill analysis in presence of 50 mg/L calcium ions2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID326280Antibacterial activity against methicillin-resistant Staphylococcus aureus 4803 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID283618Antimicrobial activity against Enterococcus faecium Ho 4418-0062 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID285037Antimicrobial activity against Bacillus spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID83806In vitro antibacterial activity against Haemophilus influenzae 11 (Hin) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID541811Antimicrobial activity against Enterococcus gallinarum clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID519994Antimicrobial activity against Streptococcus pneumoniae harboring erm(B) gene by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID126688Compound was evaluated for inhibition of Mono aminoxidase B in rat primary hepatocytes2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID533013Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR4 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1594361Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS10 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID558522Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID583394Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate NJ992 assessed as bacterial count at 32 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1390466Antibacterial activity against methicillin-resistant Staphylococcus aureus DB-000262018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID516160Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolates assessed as susceptible isolates by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID1400050Bactericidal activity against Clostridium difficile ATCC 700057 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID285013Antimicrobial activity against Enterococcus raffinosus at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID522901Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 511 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1680036Hemolytic activity in sheep RBC incubated for 1 hr2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID246828Efficacy against mice infected with MRSA-32 upon s.c. administration2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID483195Antibacterial activity against Escherichia coli ATCC 25922 by microbroth dilution technique2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID531567Antibacterial activity against Streptococcus agalactiae obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID383740Cmax in Sprague-Dawley rat at 25 mg/kg, po2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID410207Antibacterial activity against vancomycin and linezolid-resistant Enterococcus faecalis by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID555304Antibacterial activity against methicillin-resistant Staphylococcus aureus 507 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID560798Elimination rate constant in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID285156Antimicrobial activity against Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Clonal diversity and resistance mechanisms in tetracycline-nonsusceptible Streptococcus pneumoniae isolates in Poland.
AID573152Antibacterial activity against vancomycin-resistant Enterococcus faecalis by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID559551Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP4 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID558729Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 50 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID511436Antimicrobial activity against multidrug-resistant flogene-deficient Clostridium perfringens LFM1 harboring single C>T at bp 404 of rplD gene2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID524681Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID1578416Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS 386 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID574075Clearance in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID576401Residual concentration at the end of the administration interval in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID561249Antibacterial activity against Streptococcus pneumoniae by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID575265Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Comparative in vitro activity profiles of novel bis-indole antibacterials against gram-positive and gram-negative clinical isolates.
AID1680057Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 8 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1770359Ratio of MBC to MIC against penicillin-susceptible Bacillus subtilis ATCC 93722021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID404948Antibacterial activity against methicillin-susceptible Staphylococcus aureus isolate assessed as susceptible resistant isolates by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID352929Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID1241210Binding affinity to 5'-FAM-pre-miR-17 (unknown origin) after 4 hrs by fluorescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID555292Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1167733Antimicrobial activity against methicillin-sensitive Staphylococcus aureus by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID323791Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po within 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID369438Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID542672fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 100 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID582811Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS05446 harboring MLST sequence type ST17 and pulsotype B expressing vanA gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID637975Antibacterial activity against Staphylococcus aureus after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID645034Antibacterial activity against erythromycin-resistant Streptococcus pyogenes 24 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID533424Antimicrobial activity against Anaerococcus prevotii assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID533389Antimicrobial activity against Clostridium perfringens by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1596565Bactericidal activity against vancomycin resistant Staphylococcus aureus VRS11a assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID353059Antibacterial activity against vancomycin-resistant Enterococcus 2 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID442573Antibacterial activity against methicillin resistant Staphylococcus aureus ATCC 70069 after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID561082Antibacterial activity against vancomycin-resistant Enterococcus faecium by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID574956Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 6B by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1241209Binding affinity to 5'-FAM-pre-miR-372 (unknown origin) after 4 hrs by fluorescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID391590Antibacterial activity against methicillin-resistant Staphylococcus aureus TK7 by agar dilution method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials.
AID534160Antimicrobial activity against linezolid-resistant Enterococcus faecium by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID283164Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2640 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID285378Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 assessed as reduction of CFU using in vitro PK/PD model with human dosage regimen 600 mg every 12 hrs at 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID278919Antibacterial activity against linezolid-resistant Enterococcus gallinarum2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID567487Antimicrobial activity against linezolid pretreated vancomycin-intermediate Staphylococcus aureus isolate 2 obtained from blood of patient by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Clinical outcomes by methicillin-resistant Staphylococcus aureus staphylococcal cassette chromosome mec type: isolates recovered from a phase IV clinical trial of linezolid and vancomycin for complicated skin and skin structure infections.
AID404952Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus sp. assessed as percent susceptible isolates by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID284989Antimicrobial activity against Enterococcus casseliflavus at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID373312Antibacterial activity against Streptococcus pneumoniae clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID1308223Antibacterial activity against mecA-positive methicillin/oxacillin/tetracycline-resistant Staphylococcus aureus ATCC 27660 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID1451775Antibacterial activity against Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 4.5 days administered 6 hrs post bacterial infection measured 108 hrs post infection relative to 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID1504626Antibacterial activity against Haemophilus influenzae ATCC 49247 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID1557269Antitubercular activity against resistant Mycobacterium tuberculosis harboring rplC Cys154Arg mutant2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID405620Antibacterial activity against Streptococcus2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID319155Toxicity in rat at 50 mg/kg, po for 30 days2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1421237Intrinsic clearance in human liver microsomes at 1.5 uM pretreated for 5 mins followed by NADPH addition measured after 5 to 45 mins by LC-MS analysis2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID534251Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells at pH 5.5 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID583877Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-3 harboring ribosomal protein L3 deltaPhe127-His146 mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID1271204Solubility of compound at pH 2.2 by HPLC analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1390487Antibacterial activity against linezolid-resistant Enterococcus faecium 3032018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1409842Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 4.5 days relative to co2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID561093Antibacterial activity against Bacteroides ovatus by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID575944Antimicrobial activity against erythromycin-resistant Streptococcus pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.
AID1584844Antibacterial activity against hospital-acquired methicillin and vacomycin resistant Staphylococcus aureus VRS-1 after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID1168015Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 12875 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID583890Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus isolate 412 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID533958Antimicrobial activity against Legionella pneumophila ATCC 33153 infected in THP1 cells assessed as log reduction in bacterial count after 48 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID520769Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as bacterial count per gram of tibial matrix at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 8 pos2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID542389Antimicrobial activity against Staphylococcus aureus RN4220 transformed with Staphylococcus aureus ST9 plasmid pSCFS3 carrying cfr and fexA genes2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr.
AID1907631Antibacterial activity against Pseudomonas aeruginosa incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID563329Antibacterial activity against vancomycin-resistant Enterococcus faecalis EF NJ1 infected in New Zealand White rabbit assessed as reduction of bacterial count in aortic valve vegetations at 10 mg/kg, administered through ear vein every 12 hrs for 4 days (2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID1151755Antibacterial activity against penicillin-resistant Streptococcus pneumoniae isolate 06132014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID560808Elimination rate constant in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID520616Antimicrobial activity against Nocardia brasiliensis HUJEG-1 infected in BALB/c mouse assessed as decrease in number of lesions on foot-pad at 25 mg/kg, sc TID for 4 weeks2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vivo therapeutic effect of gatifloxacin on BALB/c mice infected with Nocardia brasiliensis.
AID1241206Inhibition of pre-miR-17 (unknown origin) cleavage assessed as reduction of oncogenic microRNAs biogenesis by measuring fluorescence every minute for 5 hrs using 5'-FAM,3'-dabcyl-pre-miRNA beacons by FRET assay in presence of recombinant Dicer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID1493809Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1350038Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 9 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID263966Antibacterial activity against beta lactamase negative Moraxella catarrhalis DRCC 3002006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID424616Antibacterial activity against Enterococcus avium AIS2007004 isolated from patients rectum by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID529682Antimicrobial activity against hospital-acquired methicillin-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Activities of ceftobiprole, linezolid, vancomycin, and daptomycin against community-associated and hospital-associated methicillin-resistant Staphylococcus aureus.
AID524981Antibacterial activity against Streptococcus oralis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1760590Antibacterial activity against Escherichia coli 29212 assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID1852670Antibacterial activity against multidrug resistant Pseudomonas aeruginosa BAA 2108 assessed as inhibition of bacterial growth incubated for 24 hrs in M9-MOPS medium by twofold serial dilution method
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID326501Antibacterial activity against vancomycin-susceptible Enterococcus faecalis 309 after 24 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID373651Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID565744Antimicrobial activity against Enterococcus faecium expressing VanA gene clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID584972Antibacterial activity against wild type Mycobacterium smegmatis after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID1168021Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 16475 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID285146Antimicrobial activity against viridans group Streptococcus constellatus by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID519485Antibacterial activity against Staphylococcus aureus T1887 expressing 23S rrn3 G2576T mutant by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID348863Antibacterial activity against vancomycin-resistant Enterococcus 4 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID524977Antibacterial activity against Streptococcus bovis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID531578Antibacterial activity against Lactococcus lactis obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID630556Antibacterial activity against methicillin-resistant Staphylococcus epidermidis after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID326289Antibacterial activity against methicillin-resistant Staphylococcus aureus 789 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID326297Antibacterial activity against methicillin-resistant Staphylococcus aureus 4342 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID373659Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID519093Antimicrobial activity against Staphylococcus aureus NRS119 clinical isolate harboring G2576U mutation in 23S rRNA by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID566582Antimicrobial activity against Staphylococcus warneri ATCC 27836 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID67753Minimum inhibitory concentration against Enterococcus faecalis ATTCC 292122003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
AID1393951Antibacterial activity against methicillin resistant Staphylococcus epidermidis ATCC 51625 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID442572Antibacterial activity against floxacin and methicillin-resistant Staphylococcus aureus ATCC 25923 after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID1197127Antibacterial activity against Enterococcus faecalis ATCC 29212 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1390468Antibacterial activity against Staphylococcus aureus Mu50 ATCC 7006992018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID560508Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b3k5923 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1350039Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 10 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID373999Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey after 50 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1400055Antibacterial activity against Acinetobacter baumannii ATCC 19606 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID285370Antibacterial activity against heteroresistant vancomycin-intermediate Staphylococcus aureus Mu3 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID1304854Aqueous solubility of compound in media after 16 hrs2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID561095Antibacterial activity against Peptostreptococcus anaerobius by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID530124Antimicrobial activity against community acquired methicillin-resistant Staphylococcus aureus 147 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID576422AUC in healthy human at 600 mg, iv, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID528718Antibacterial activity against vancomycin resistant Enterococcus faecium VanB clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID474996Antibacterial activity against Staphylococcus aureus LCB0001 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID528736Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus auricularis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID561268Antibacterial activity against Enterococcus faecium assessed as resistant isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1327120Antitubercular activity against dormant stage Mycobacterium bovis BCG ATCC 35734 at 30 ug/ml measured after 12 days by nitrate reductase assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID278926Antibacterial activity against Moraxella catarrhalis2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID374017Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1680013Antibiofilm activity against 24 hrs preformed biofilm of Staphylococcus aureus ATCC 29213 assessed as eradication of preformed biofilm incubated for 24 hrs by crystal violet staining assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1161139Antimicrobial activity against methicillin-resistant Staphylococcus aureus after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID303972Antibacterial activity against methicillin-resistant Staphylococcus aureus SA1417 in po dosed CD1 mouse systemic infection model assessed as mortality after 7 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID1684998Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth incubated for 16 to 20 hrs by microdilution method2021ACS medicinal chemistry letters, Jan-14, Volume: 12, Issue:1
Enhancing Antimicrobial Peptide Potency through Multivalent Presentation on Coiled-Coil Nanofibrils.
AID1904919Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS 386 (USA700) incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1659809Antimycobacterial activity against Mycobacterium tuberculosis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Molecule Property Analyses of Active Compounds for
AID522907Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1007 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID562634Antimicrobial activity against Corynebacterium spp. by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1594365Antibacterial activity against penicillin-resistant Streptococcus pneumoniae ATCC 700677 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID424761Antibacterial activity against vancomycin-intermediate, macrolide, methicillin-resistant Staphylococcus aureus CL5706 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID558701Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID562618Antimicrobial activity against Heterovancomycin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1374165Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated at 37 degC for 20 hrs by standard broth microdilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID369439Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID1151745Antibacterial activity against Staphylococcus aureus measured after 7 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1770365Bactericidal activity against Vancomycin-susceptible Enterococcus faecium ATCC 19434 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID524947Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus haemolyticus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1866043Antibacterial activity against methicillin-resistant Staphylococcus aureus in in-vivo systemic infection model2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
AID549537Apparent permeability from basolateral to apical side of MDCK cells2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
MDCK cell permeability characteristics of a sulfenamide prodrug: strategic implications in considering sulfenamide prodrugs for oral delivery of NH-acids.
AID428280Antituberculosis activity against linezolid-resistant Mycobacterium tuberculosis having mutation in 23S rRNA with G to T base pair exchange at position 25762008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID562185Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 15 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID524721Antibacterial activity against linezolid-resistant Enterococcus faecalis 03A1128 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID533007Antibacterial activity against vancomycin-intermediate Staphylococcus aureus 99/3700-W phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID558501Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1304837Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID564821Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus hominis after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1060727Antibacterial activity against Staphylococcus aureus harboring FtsZ G196A mutant by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ.
AID326291Antibacterial activity against methicillin-resistant Staphylococcus aureus 4913 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID534157Antimicrobial activity against linezolid-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID67579Minimum inhibitory concentration against Enterococcus faecalis UC92171998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID1609285Antibacterial activity against methicilline-resistant Staphylococcus aureus NRS384 USA300 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1504624Antibacterial activity against Streptococcus pyogenes ATCC 19615 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID548256Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega expressing vraSm mutant gene after 24 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID559365Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP1 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1677796Bacteriostatic activity against Staphylococcus aureus ATCC25923 assessed as ratio of MBC to MIC2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID528698Antibacterial activity against vancomycin resistant Enterococcus faecium VanA clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID67242In vitro antibacterial activity against Enterococcus faecalis ATCC 29212 (Efs) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID1862429Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1644) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID1852696Inhibition of CALML3 (unknown origin) assessed as apparent protein translation inhibition constant incubated for 5 hrs by SDS gel electrophoresis
AID133991Protective dose of orally administered compound against intraperitoneally-induced septicaemia model ( vancomycin resistant Enterococci faecium D3HM3 strain) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID352925Antibacterial activity against Streptococcus pneumoniae C402 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID729224Antibacterial activity against methicillin-resistant Staphylococcus aureus after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID1409851Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 4.52018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID1180577Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC2381-3F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID373827Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 after 16 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance s2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1327103Antitubercular activity against active stage Mycobacterium bovis BCG ATCC 35734 measured after 8 days by nitrate reductase assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID83808Antibacterial activity against Haemophilus influenzae (HI1008)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID524976Antibacterial activity against Streptococcus sp. Group G clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID577142Volume of distribution at steady state in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1680062Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 4 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID571927Ratio of MIC for Escherichia coli K-12 3-AG300 harboring acrB::rpsLneo mutant gene to MIC for Escherichia coli K-12 3-AG3002009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID561091Antibacterial activity against Bacteroides vulgatus by CLSI M11-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID369436Antimicrobial activity against methicillin-resistant Staphylococcus aureus after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID319167Drug level in human lung epithelial lining fluid at 600 mg, po bid after 4 hrs2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID285004Antimicrobial activity against Enterococcus gallinarum at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID523819Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID275471Antibacterial activity against Staphylococcus aureus2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID522015Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID533950Antimicrobial activity against hospital acquired methicillin-resistant, vancomycin resistant Staphylococcus aureus VRS1 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID567453Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK5 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID581013Antimicrobial activity against Staphylococcus epidermidis ATCC 23760 by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID542716fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg /day administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID535261Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-9 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1744565Inhibition of Staphylococcus aureus FabH A81V/A111T mutant assessed as bacterial growth inhibition measured after 18 hrs by resazurin dye based broth dilution assay2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID561254Antibacterial activity against Streptococcus pyogenes assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID528697Antibacterial activity against vancomycin resistant Enterococcus faecium VanB clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID535013Antimicrobial activity against vancomycin-resistant Staphylococcus aureus by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID284963Antimicrobial activity against Corynebacterium amycolatum at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID590063Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected po dosed ICR mouse assessed as protection against mouse mortality administered 1 hr after infection measured up to 7 days2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID524975Antibacterial activity against Streptococcus sp. Group F clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID535259Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-7 expressing SCCmec element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID244814Minimum inhibitory concentration against Enterococcus faecalis A206882005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
AID261065Antibacterial activity against Moraxella catarrhalis BC-35312006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
AID756093Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis assessed as growth inhibition after 16 hrs by agar dilution method2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
AID387456Antibacterial activity against beta-lactamase deficient Haemophilus influenzae DRCC 4332008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID1578429Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID1609265Antibacterial activity against methicillin-resistant Streptococcus pneumoniae ATCC 700677 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID542896fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID188644In vivo activity against Staphylococcus aureus when administered orally for 1 hr in rat at a dose of 15 mg/kg2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID262227Antibacterial activity against Staphylococcus epidermidis ATCC 1552006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID519094Antimicrobial activity against Staphylococcus aureus NRS120 clinical isolate harboring G2576U mutation in 23S rRNA by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID583896Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 454 (NRS404) by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID303966Bacteriostatic activity against Staphylococcus after 48 hrs by time kill study2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID1676982Antimicrobial activity against Escherichia coli BW25113 harboring TolC mutant assessed as reduction in microbial growth after 48 hrs by CLSI based broth microdilution method
AID285110Antimicrobial activity against viridans group Streptococcus mutans at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1594367Antibacterial activity against Acinetobacter baumannii BAA1605 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID562624Antimicrobial activity against Group A Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1180579Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC2398-1F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID671569Antibacterial activity against Streptococcus pneumoniae SPN160 infected in neutropenic Balb/c mouse infection model assessed as reduction in lung CFU at 30 mg/kg, po administered 2 and 12 hrs post infection measured 24 hrs post treatment2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID1243931Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS119 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID131687Effective dose of compound after oral administration in murine model infected with Staphylococcus aureus OC4172 (Smith) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
AID523829Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 32 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID564809Bactericidal activity against methicillin-resistant coagulase-negative Staphylococcus haemolyticus after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID283621Antimicrobial activity against Enterococcus faecium 2 L1 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID1611132Aqueous solubility of compound2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
AID1400042Antibacterial activity against Staphylococcus aureus BAA 1683 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID285044Antimicrobial activity against Enterococcus avium by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285383Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 using in vitro PK/PD model with 120 mg/24 hr continuous infusion simulated regimen after 72 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID1853457Bactericidal activity against Staphylococcus aureus ATCC 25923 assessed as reduction in colony forming unit incubated for 20 hrs2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID571999Antibacterial activity against Streptococcus constellatus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1609290Antibacterial activity against Staphylococcus aureus ATCC BAA42 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1168001Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 5648 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID541057Ratio of Cmax to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 50 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID584995Antibacterial activity against pSCFS7-deficient methicillin-resistant Staphylococcus aureus M05/0060-C1 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate.
AID1168024Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 12/266 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID308921Antibacterial activity against Staphylococcus aureus ATCC 25923 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID573385Antibacterial activity against beta lactamase-positive Moraxella catarrhalis by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1151711Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID574086Ratio of fAUC (24 hrs) for penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected iv dosed mouse to MIC for penicillin-susceptible Streptococcus pneumoniae ATCC 63012009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID561514Antibacterial activity against Enterococcus faecalis by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID383571Tmax in Sprague-Dawley rat at 10 mg/kg, iv2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID1721014Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID584115Antibacterial activity against Escherichia coli KAM32 harboring pSP72 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.
AID326295Antibacterial activity against methicillin-resistant Staphylococcus aureus 859 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID573890fAUC (0 to 24 hrs) in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID560822Ratio of Cmax in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days to MIC for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID562171Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 after 50 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID562389Antimicrobial activity against Enterococcus faecalis clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1451768Antibacterial activity against Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 4.5 days administered 6 hrs post bacterial infection measured 108 hrs post infection relative to co2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID561074Antibacterial activity against methicillin-susceptible Staphylococcus aureus by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID524689Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID1205590Fraction unbound (%) in human plasma at 10 uM by LC/MS-MS analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1271212Metabolic stability in human liver microsomes after 30 mins by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID561083Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of TR-700, the active ingredient of the antibacterial prodrug TR-701, a novel oxazolidinone antibacterial agent.
AID776672Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 after 16 to 20 hrs by microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Novel promising linezolid analogues: rational design, synthesis and biological evaluation.
AID763954Antibacterial activity against Moraxella catarrhalis clinical isolate 36 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1553374Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 measured after 16 hrs by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID370022Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 3.12 mg/kg/day, iv administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burd2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID374588Antimicrobial activity against Staphylococcus aureus MTCC 3160 after 24 hrs by agar dilution assay2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.
AID576660Bactericidal activity against 12 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1161215Antimicrobial activity against Staphylococcus aureus ATCC 33591 in septicemia mouse model administered intragastrically measured after 14 days2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID522896Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1013 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1415068Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 4 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID522906Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1984 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1907628Antibacterial activity against Staphylococcus aureus ATCC6538 incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID210360In vitro antibacterial activity against penicillin sensitive Streptococcus pneumoniae UC 9912; range is 0.5-12003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID577108AUBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1361107Bactericidal activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID522884Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 1263 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID558482Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID545806Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate VRS5 planktonic cells by broth microdilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID687497Clearance in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID373315Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID1710570Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1873944Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in absence of foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID244852Minimum inhibitory concentration against Enterococcus faecium ATCC 65692004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID576891Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID541056Ratio of Cmax to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 75 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID535015Antimicrobial activity against vancomycin-resistant Staphylococcus aureus assessed as susceptible isolates by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID10637In vivo activity against Staphylococcus aureus when administered orally for 1 hr in rat at a dose of 15 mg/kg2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1233135Antibacterial activity against patient-derived methicillin-resistant Staphylococcus aureus 7419 after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID576326Antibacterial activity against 10'4 to 10'5 CFU methicillin-susceptible Staphylococcus aureus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID206816In vitro antibacterial activity against Staphylococcus pyogenes ATTCC86682003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID285369Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID1126486Antimicrobial activity against Staphylococcus aureus Oxford2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID424764Antibacterial activity against vancomycin-sensitive Enterococcus faecalis CL8516 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID533976Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS384 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID576895Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID369448Antimicrobial activity against Streptococcus viridans after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID533412Antimicrobial activity against Finegoldia magna assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID442577Antibacterial activity against Klebsiella pneumoniae ATCC 27736 after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID542385Antimicrobial activity against methicillin-resistant Staphylococcus aureus ST398 expressing cfr, fexA, erm(A), tet(M) and mecA genes2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr.
AID558497Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID284945Antimicrobial activity against Bacillus spp. at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID311482Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 29212 after 14 to 16 hrs by serial microbroth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID528730Antibacterial activity against penicillin resistant Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1308238Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS70 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID567490Antimicrobial activity against linezolid pretreated vancomycin-intermediate Staphylococcus aureus isolate 5 obtained from wound of patient by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Clinical outcomes by methicillin-resistant Staphylococcus aureus staphylococcal cassette chromosome mec type: isolates recovered from a phase IV clinical trial of linezolid and vancomycin for complicated skin and skin structure infections.
AID1472758In vivo anti-virulence activity against methicillin-resistant Staphylococcus aureus LRSA202 infected in BALB/c mouse model assessed as reduction in bacterial load in heart at 0.1 mg bid for 3.5 days administered intraperitoneally 6 hrs post infection by s2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID572002Antibacterial activity against Parabacteroides merdae by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1574839Antibacterial activity against vancomycin-resistant Enterococcus faecium by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID284987Antimicrobial activity against Enterococcus casseliflavus at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285047Antimicrobial activity against Enterococcus gallinarum by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1151742Antibacterial activity against Staphylococcus aureus measured after 4 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID531642Antimicrobial activity against linezolid-resistant Enterococcus faecalis P52008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID562383Antimicrobial activity against vancomycin-susceptible Enterococcus faecium clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID348600Antibacterial activity against Streptococcus agalactiae ATCC 2901 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID582992Antimicrobial activity against rifampin-, fusidic acid-resistant Enterococcus faecium BM-4105 by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID428282Antituberculosis activity against linezolid-resistant Mycobacterium smegmatis without mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID560512Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b6k1642 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1832944Antibacterial activity against Vanomycin-resistant Enterococcus faecalis NCTC 12201 assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID285127Antimicrobial activity against viridans group Streptococcus salivarius at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID284996Antimicrobial activity against Enterococcus durans at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID345136Antimicrobial activity against Streptococcus pyogenes Msr 610 expressing erm(B) gene by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
AID1265126Reversible inhibition of human MAO-A2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID1862419Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID244813Minimum inhibitory concentration against Enterococcus faecium A248852005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
AID1151726Antibacterial activity against Streptococcus pyogenes2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID270150Antibacterial activity against gram positive methicillin-susceptible Staphylococcus aureus Smith OC 4172 by broth microdilution assay2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.
AID565743Antimicrobial activity against Enterococcus faecium expressing VanB gene clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID604289Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 1094 after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID285381Bactericidal activity against vancomycin-intermediate Staphylococcus aureus Mu50 assessed as reduction of CFU using in vitro PK/PD model with 120 mg/24 hr continuous infusion simulated regimen after 48 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID581656Antibacterial activity against revertant Staphylococcus aureus at pH 7.4 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1409841Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 4.5 days relative to co2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID293550Antibacterial activity against Staphylococcus aureus MTCC 3160 after 24 hrs by agar dilution assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Organoiodine(III) mediated synthesis of 3,9-diaryl- and 3,9-difuryl-bis-1,2,4-triazolo[4,3-a][4,3-c]pyrimidines as antibacterial agents.
AID285388Area under population analysis profile for vancomycin-resistant Enterococcus faecium ATCC 700221 using in vitro PK/PD model relative to growth control with 120 mg/24 hrs continuous infusion regimen after 72 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID388044Antibacterial activity against methicillin-resistant Staphylococcus aureus MB5393 containing COL plasmid after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID1472764In vivo anti-virulence activity against Staphylococcus aureus NRS271 infected in BALB/c mouse model assessed as reduction in bacterial load in kidney at 0.4 mg bid for 4.5 days administered orally 6 hrs post infection by serial dilution method relative to2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID373316Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID531576Antibacterial activity against Gemella morbillorum obtained from complicated skin and skin structure infections by RapID ANA system2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1400040Antibacterial activity against Staphylococcus aureus BAA 2094 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID522900Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1017 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1744555Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID206993The compound was evaluated for its anti-bacterial activity against methicillin resistant Staphylococcus epidermidis1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID1596560Bactericidal activity against Staphylococcus aureus ATCC 6538 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID524973Antibacterial activity against Streptococcus agalactiae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID577135AUC in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1451771Antibacterial activity against Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid for 4.5 days administered 6 hrs post bacterial infection measured 108 hrs post infection relative to 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID573117Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID565486Bactericidal activity against methicillin-resistant Staphylococcus aureus after 24 hrs by M26-A method in presence of 50% human plasma2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID207216In vitro minimum inhibitory concentration against Staphylococcus aureus Oxford2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID585159Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA A2453U mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID565491Ratio of MBC to MIC for methicillin-susceptible Staphylococcus aureus in presence of 50% human plasma2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID1446758Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID561238Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID560824Ratio of AUC (0 to 24 hrs) in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days to MIC for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID260742Antibacterial activity against Enterococcus faecium 194342006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID285321Antimicrobial activity against Nocardia asteroides by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID424770Antibacterial activity against Streptococcus pyogenes CL10440 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID571808Antibacterial activity against Clostridium scindens by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID370027Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in po dosed C3H mouse localized infection model assessed as reduction of number of CFU per gram of kidney administered 15 mins after infection measured after 48 hr2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID263962Antibacterial activity against methicillin-resistant Staphylococcus aureus DRCC 4462006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID285382Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 assessed as reduction of CFU using in vitro PK/PD model with 120 mg/24 hr continuous infusion simulated regimen after 48 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID558498Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID456045Antibacterial activity against vancomycin-resistant Enterococcus faecalis after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID555742Antibacterial activity against methicillin-resistant, Linezolid non-susceptible coagulase-negative Staphylococcus epidermidis 345 by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1609264Bactericidal activity against methicillin-resistant Staphylococcus epidermidis NRS101 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1721021Ratio of MIC for antitubercular activity against linezolid-resistant Mycobacterium tuberculosis to MIC for antitubercular activity against Mycobacterium tuberculosis H37Rv2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID560802Apparent oral clearance in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID542909Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as prevention of bacterial regrowth at 800 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID574071Tmax in CF-1 mouse serum at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID292667Inhibition of mitochondrial protein synthesis in Escherichia coli assessed as [35S]methionine incorporation method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials.
AID562192Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID548530Antimicrobial activity against Vancomycin-nonsusceptible Enterococcus faecalis by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID572557Antibacterial activity against Mycobacterium tuberculosis H37Rv by agar proportion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
In vitro activities of linezolid against clinical isolates of Mycobacterium tuberculosis complex isolated in Taiwan over 10 years.
AID516163Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolates assessed as resistant isolates by EUCAST method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID1312949Bactericidal activity against methicillin-resistant Staphylococcus aureus USA200 NRS383 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID390338Antimicrobial activity against ampC beta-lactamase producing multidrug-resistant Klebsiella pneumoniae 22622008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID524980Antibacterial activity against Streptococcus mitis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID285035Antimicrobial activity against Rothia mucilaginosa at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1117393Antimicrobial activity against Escherichia coli SG458 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID511382Antibacterial activity against Enterococcus faecalis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID1304848Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 incubated for 16 hrs by broth microdilution method in presence of Cu2+2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1547711Antibacterial activity against Staphylococcus epidermidis ATCC 35547 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID523805Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID323783Antimicrobial activity against bioluminescent methicillin-resistant Staphylococcus aureus Xen12007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID68385In vitro antibacterial activity against Enterococcus faecium strain UC127121996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID278911Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID520614Cmax in BALB/c mouse serum at 25 mg/kg, sc TID for 4 weeks by HPLC method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vivo therapeutic effect of gatifloxacin on BALB/c mice infected with Nocardia brasiliensis.
AID370020Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 12.5 mg/kg/day, iv administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burd2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID562393Antimicrobial activity against oxacillin-resistant Staphylococcus epidermidis clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID278922Antibacterial activity against penicillin-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID245414Minimum inhibitory concentration against methicillin-susceptible Staphylococcus aureus UC9213; Range is 2-4 ug/mL2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID534155Antimicrobial activity against linezolid-resistant Enterococcus faecalis 3128 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID495878Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected New Zealand White rabbit aortic valve endocarditis model assessed as decrease in bacterial colony forming unit in vegetation at 75 mg/kg, sc dosed every 8 hrs for 4 da2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ceftobiprole is superior to vancomycin, daptomycin, and linezolid for treatment of experimental endocarditis in rabbits caused by methicillin-resistant Staphylococcus aureus.
AID511431Antimicrobial activity against Clostridium perfringens LFM1 assessed as susceptibility breakpoint by EUCAST method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID372667Antimicrobial activity against Pseudomonas aeruginosa MTCC 3541 after 24 hrs by agar dilution assay2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.
AID565756Antimicrobial activity against oxacillin-resistant Staphylococcus epidermidis clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID542921Antimicrobial activity against mutant Bacillus anthracis2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID410114Antimicrobial activity against erm (B) Streptococcus pyogenes msr610 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID287268Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID390337Antimicrobial activity against Klebsiella pneumoniae 22392008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID581657Antibacterial activity against normal phenotype Staphylococcus aureus at pH 7.4 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID565747Antimicrobial activity against Enterococcus faecium clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID640892Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by agar microdilution method2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID1327105Antibacterial activity against Escherichia coli NCIM 2688 at 30 ug/ml measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1395673Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1482581Antibacterial activity against methicillin-sensitive Staphylococcus aureus A-1178 infected in neutropenic murine thigh infection model assessed as decrease in bacterial load in thighs administered po 22 hrs post infection measured 24 hrs post infection2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents.
AID442576Antibacterial activity against Enterococcus faecalis MTCC439 after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID524957Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1680048Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 8 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1862421Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID576411Total clearance in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID519993Antimicrobial activity against vancomycin-resistant Enterococcus faecium nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID572010Antibacterial activity against Fusobacterium varium by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1117380Antimicrobial activity against methicillin-resistant Staphylococcus aureus 134/93 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID363434Antibacterial activity against Streptococcus pneumoniae ATCC 63032008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
AID284952Antimicrobial activity against Bacillus cereus at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285028Antimicrobial activity against Micrococcus luteus at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID565077Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus 144 by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
AID390324Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 292132008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID206864Antibacterial activity against Methicillin-suceptible Staphylococcus aureus UC92182003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID532794Antibacterial activity against vancomycin-intermediate Staphylococcus aureus AMC11094 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID210369In vitro antibacterial activity against Streptococcus pneumoniae2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and antibacterial activity of oxazolidinone containing sulphonyl group.
AID297130Antibacterial activity against Klebsiella pneumoniae NCTN9632 by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID520513AUC in New Zealand rabbit osteomyelitis model at 40 mg/kg, sc administered every 6 hrs for 4 days2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID565748Antimicrobial activity against Enterococcus faecalis expressing VanB gene clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID278924Antibacterial activity against fluoroquinolone-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID370023Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 25 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay re2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID560374Selectivity ratio of MIC for Enterococcus faecalis ATCC 29212 in presence of 4% HSA to MIC for Enterococcus faecalis ATCC 292122009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID524684Antibacterial activity against coagulase-negative Staphylococcus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID559561Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP7 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID373990Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 50 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID278907Antibacterial activity against methicillin-susceptible Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1778661Bactericidal activity against penicillin-susceptible Bacillus subtilis ATCC 9372 measured after 24 hrs by CLSI protocol based method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID532808Antibacterial activity against vancomycin-susceptible Staphylococcus aureus BR2 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1400035Antibacterial activity against Mycobacterium smegmatis ATCC 607 incubated for 48 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID532812Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1584839Antibacterial activity against vancomycin-resistant Enterococcus faecalis BM 4575 clinical isolate after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID439890Antibacterial activity against Escherichia coli ATCC 8739 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID1056355Antibacterial activity against Haemophilus influenzae SR27914 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID583393Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate NJ992 assessed as bacterial count at 16 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID244925Minimum inhibition concentration against Haemophilus influenzae strains2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Biaryl isoxazolinone antibacterial agents.
AID285311Antimicrobial activity against Listeria monocytogenes by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID573388Antibacterial activity against Pasteurella multocida by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID574074Half life in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID132755In vivo antibacterial activity in a murine systemic infection model2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID404934Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID562167Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID516159Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolates by CLSi method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID524961Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus sciuri clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID562160Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1056348Inhibition of rat forebrain MAO-A using [14C]5-HT as substrate at 30 uM preincubated for 20 mins followed by substrate addition measured after 5 mins by liquid scintillation counting analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1311370Antibacterial activity against Mycobacterium avium 104 measured after 7 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID206592In vitro antibacterial activity against Staphylococcus aureus2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID520768Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as improvement in extent of bone remodeling at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 8 post2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID390325Antimicrobial activity against methicillin-resistant Staphylococcus aureus 11372008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID206872Antibacterial activity against Staphylococcus aureus (SA1011)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID370021Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 6.25 mg/kg/day, iv administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burd2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1603314Antimicrobial activity against Escherichia coli SQ110 LPTD measured after 16 hrs by broth microdilution method2019ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3
Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics.
AID1504966Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by second incubation under aerobic condition for 28 hrs by LORA2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID730747Antibacterial activity against methicillin-resistant Staphylococcus aureus 1279-07-USA300 assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID1197129Antibacterial activity against vancomycin-resistant Enterococcus faecalis 99 clinical isolate after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1139118Half life in rat at 2.8 to 9.5 mg/kg, iv2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID1435925Antibacterial activity against methicillin/erythromycin/tetracycline-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID671563Antibacterial activity against Haemophilus influenzae 5512012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID1308236Antibacterial activity against vancomycin-resistant Enterococcus faecalis 99 clinical isolate incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID245023In vitro minimum inhibitory concentration against Enterococcus faecium (6A-VRE)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID1395709Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS386 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
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AID245167Minimum inhibitory concentration against homogeneously methicillin-resistant Staphylococcus aureus A272232005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
AID548533Antimicrobial activity against Beta-hemolytic Streptococcus by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID65385Inhibitory activity against Enterococcus faecalis UC92172000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID133299Minimum inhibitory concentration of the subcutaneously administered compound evaluated against Staphylococcus aureus HT-17 strain in mice (SC)2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID23015Steady-state volume distribution was evaluated in male Dawley rats at a dose of 10 mg/kg when taken intravenously1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID1609260Bactericidal activity against cephalosporin-resistant Streptococcus pneumoniae ATCC 51916 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID571763Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-F628F mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID1151733Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID645039Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID370031Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected in po dosed DBA/2 mouse localized infection model assessed as reduction of number of CFU per gram of thigh administered 2 hrs postinfection thrice daily for 1 day and 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID533955Antimicrobial activity against Staphylococcus aureus infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID581654Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient at pH 7.4 after 48 hrs by broth microdilution method in absence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID571789Antibacterial activity against Clostridium bolteae by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID576865Bactericidal activity against 1 hr peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1778650Antibacterial activity against penicillin-susceptible Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured by broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID520617Antimicrobial activity against Nocardia brasiliensis HUJEG-1 by broth macrodilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vivo therapeutic effect of gatifloxacin on BALB/c mice infected with Nocardia brasiliensis.
AID1151764Antibacterial activity against penicillin intermediate-sensitive Streptococcus pneumoniae ATCC 49619 clinical isolate in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID206599In vitro antibacterial activity against ciprofloxacin-resistant Staphylococcus aureus (CRSA)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID523818Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID560514Antimicrobial activity against SCCmec type IV vancomycin-intermediate Staphylococcus aureus isolate 06b41 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID244819Minimum inhibitory concentration against Streptococcus pneumoniae A95852005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
AID1265131Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis ATCC 122282015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID1424068Antibiotic activity against methicillin-resistant Staphylococcus aureus isolate CAIRD148 by broth microdilution assay or Alamar blue dye based colorimetric assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
The Berkeleylactones, Antibiotic Macrolides from Fungal Coculture.
AID475006Antibacterial activity against Escherichia coli LCB0011 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID1058370Antimicrobial activity against methicillin-resistant Staphylococcus aureus after 24 hrs by microdilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Anti-tubercular agents. Part 8: synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles.
AID730743Antibacterial activity against macrolides, lincosamides, streptogramin B and methicillin-resistant Staphylococcus aureus 1609-09 harboring cfr gene assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID584993Antibacterial activity against Staphylococcus aureus XU21 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate.
AID1649292Antibacterial activity against Streptococcus pneumoniae SR11031 (PRSP) assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID1853454Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51575 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID1553378Half life in mouse liver microsomes2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID520031Antimicrobial activity against Enterococcus faecium A81302008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID542680fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 100 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID388046Antibacterial activity against Haemophilus influenzae MSD2261 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID285050Antimicrobial activity against Listeria monocytogenes by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID370011Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 25 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay re2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID565480Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID562632Antimicrobial activity against Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1723499Antibacterial activity against Enterococcus faecalis HM-335 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID1703712Antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID566579Antimicrobial activity against Staphylococcus epidermidis ATCC 12228 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID1327113Antibacterial activity against Staphylococcus aureus NCIM 2079 at 3 ug/ml measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID477373Antibacterial activity against Bacillus cereus MTCC 430 after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID348603Antibacterial activity against vancomycin-resistant Enterococcus faecium 1 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID573122Antibacterial activity against coagulase-negative and oxacillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID285106Antimicrobial activity against viridans group Streptococcus mutans at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1361102Bacteriostatic activity against methicillin-resistant Staphylococcus aureus USA800 NRS387 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID11797Maximum plasma concentration (Cmax) of compound (25 mg/kg) after po administration was determined Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID1770346Antibacterial activity against penicillin-resistant Staphylococcus aureus ATCC 31007 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID392208Antibacterial activity against Staphylococcus aureus ATCC 292132009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Antibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ.
AID533962Antimicrobial activity against Legionella pneumophila ATCC 33153 infected in THP1 cells after 48hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID561747Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as resistant isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID274226Antibacterial activity against Streptococcus pyogenes C-2032006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID1303405Antibacterial activity against Penicillin-resistant Streptococcus pneumoniae after 24 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID1687315Synergistic antibacterial activity against Acinetobacter baumannii ATCC 19606 in presence of 0.25 times MIC of colistin incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1680052Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 4 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID284991Antimicrobial activity against Enterococcus casseliflavus at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID542894fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 400 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID285509Antibacterial activity against Streptococcus viridans after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID373843Antimicrobial activity against methicillin and vancomycin-resistant Staphylococcus aureus 510 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1472760In vivo anti-virulence activity against methicillin-resistant Staphylococcus aureus LRSA202 infected in BALB/c mouse model assessed as reduction in bacterial load in heart at 0.4 mg bid for 3.5 days administered intraperitoneally 6 hrs post infection by s2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID285119Antimicrobial activity against viridans group Streptococcus parasanguis at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID374014Antimicrobial activity against methicillin-resistant vancomycin-intermediate Staphylococcus aureus 504 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID369447Antimicrobial activity against Streptococcus group B after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID545811Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as inhibition of biofilm formation after 24 hrs by serial dilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID573132Antibacterial activity against erythromycin-susceptible Streptococcus pyogenes assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID534162Antimicrobial activity against linezolid-resistant Staphylococcus sciuri by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID564829Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus sciuri after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID535772Antimicrobial activity against Mycobacterium ulcerans 1059 agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID528836Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1181168Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID541041Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 50 mg/kg measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID581653Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU after 5 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID318365Antifungal activity against Candida albicans2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID66572Antibacterial activity was determined against clinically isolated vancomycin-A resistant enterococci (VRE) strains (33 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID559787Antimicrobial activity against heterogeneous vancomycin-susceptible Staphylococcus aureus assessed as intermediate isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1904913Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID576421Elimination half-life in healthy human at 600 mg, iv, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID424766Antibacterial activity against vancomycin, linezolid-resistant Enterococcus faecium CL5791 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID206127In vitro antibacterial activity against ciprofloxacin-resistant Staphylococcus aureus (CRSA) C6043.1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID524688Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID524690Antibacterial activity against penicillin-nonsusceptible Streptococcus pneumoniae clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID576881Bactericidal activity against 48 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1271221Ratio of AUC (0 to t) in brain to plasma in BALB/c mouse at 10 mg/kg, po2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1862425Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1567) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID1194837Antibacterial activity against Enterococcus faecalis incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID278912Antibacterial activity against coagulase-negative staphylococci2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID444265Antibacterial activity against Streptococcus pneumoniae ATCC 6303 by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID571766Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB-N616 mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID524971Antibacterial activity against vancomycin-resistant and teichoplanin-susceptible Enterococcus faecium clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID1853460Bactericidal activity against Enterococcus faecalis ATCC 29212 assessed as reduction in colony forming unit incubated for 20 hrs2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID548529Antimicrobial activity against Vancomycin-susceptible Enterococcus faecalis by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID1056356Antibacterial activity against penicillin-resistant Streptococcus pneumoniae SR11031 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID528705Antibacterial activity against Streptococcus mitis clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1250832Antibacterial activity against Staphylococcus aureus incubated for 18 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent.
AID1400056Bactericidal activity against Acinetobacter baumannii ATCC 19606 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID297131Antibacterial activity against Proteus mirabilis IFO3849 by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID560579Bactericidal activity against vancomycin-resistant Enterococcus faecium 1059060 expressing vanA gene assessed as change in bacterial count at 16 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID534252Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1303404Antibacterial activity against vancomycin-resistant Enterococcus faecalis after 24 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID1853462Bactericidal activity against vancomycin-resistant Enterococcus faecalis ATCC 700221 assessed as reduction in colony forming unit incubated for 20 hrs2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID534253Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus SA238 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID560523Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gs07022 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID405628AUC in human at 600 mg administered every 12 hrs measured after 24 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID533968Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 33591 infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1432977Inhibition of mitochondrial protein synthesis in rat H9c2 cells after 5 days by In-Cell ELISA
AID534508Drug level in human THP1 cells at 10 mg/L after 2 hrs in presence of 50 uM proton inophore monesin relative to control2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
AID517667Antimicrobial activity against methicillin-resistant Staphylococcus aureus HH1 by standard serial-dilution technique2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
AID562391Antimicrobial activity against oxacillin-susceptible Staphylococcus haemolyticus clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID562614Antimicrobial activity against methicillin-sensitive Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID569348Antibacterial activity against Haemophilus influenzae by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID575101Antimicrobial activity against Streptococcus pneumoniae serotype 23B assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1361104Bacteriostatic activity against vancomycin-resistant Staphylococcus aureus VRS12 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID456043Antibacterial activity against ciprofloxacin, methicillin-resistant Staphylococcus aureus after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID1151721Bacteriostatic activity against vancomycin-sensitive Enterococcus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID593963Antibacterial activity Staphylococcus epidermidis ATCC 122282011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
AID1434675Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 0027 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID585174Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA A2572U1 mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID1873891Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^4 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID207016Antibacterial activity against methicillin - resistant Staphylococcus aureus (MRSA OC2878)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID522895Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1012 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID541089Antibacterial activity against 1 x10'6 to 5 x10'6 CFU/ml methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as effect on bacterial count at MIC after 24 hrs by time kill study2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID410104Antimicrobial activity against mef (A) expressing Streptococcus pneumoniae 02J1175 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID571829Antibacterial activity against Propionibacterium propionicus by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1770343Antibacterial activity against penicillin-susceptible Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID542907Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial regrowth at 600 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1076826Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID1168009Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 14643 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID284982Antimicrobial activity against Enterococcus avium at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID467839Antibacterial activity against Enterococcus faecalis MTCC 439 after 24 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
AID297129Antibacterial activity against Escherichia coli NIHJ JC2 by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1465594Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6J mouse assessed as bacterial load in lungs at 100 mg/kg qd administered for 8 consecutive weeks starting from 6 weeks post infection measured 24 hrs post last dose (Rvb = 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656).
AID558473Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID548532Antimicrobial activity against Vancomycin-nonsusceptible Enterococcus faecium by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID574065Cmax in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID284971Antimicrobial activity against Corynebacterium pseudodiphtheriticum at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1852683Antibacterial activity against efflux pump lacking/recombinant OM pore producing Escherichia coli assessed as inhibition of bacterial growth
AID285033Antimicrobial activity against Rothia mucilaginosa at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1327121Antitubercular activity against dormant stage Mycobacterium bovis BCG ATCC 35734 at 10 ug/ml measured after 12 days by nitrate reductase assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID541047Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 50 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1271229Antibacterial activity against clinical isolate Neisseria meningitidis 306 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1395710Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRS10 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1547706Antibacterial activity against Staphylococcus aureus NRS100 (COL) by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID1677786Inhibition of ftsZ in Bacillus subtilis assessed as increase in enzyme polymerization kinetics at 10 ug/ml measured for 30 mins by microtiter plate-based light scattering assay2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1241207Inhibition of pre-miR-373 (unknown origin) cleavage assessed as reduction of oncogenic microRNAs biogenesis by measuring fluorescence every minute for 5 hrs using 5'-FAM,3'-dabcyl-pre-miRNA beacons by FRET assay in presence of recombinant Dicer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID520227Antimicrobial activity against methicillin resistant Staphylococcus aureus 67-02008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID560811Apparent volume of distribution with respect to the bioavailability in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID575946Antimicrobial activity against erythromycin-resistant Streptococcus pneumoniae assessed as susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.
AID245199Minimum inhibitory concentration against Streptococcus pyogenes ATCC 49399; value ranges from 1.5-3 uM2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID285124Antimicrobial activity against viridans group Streptococcus salivarius at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1574850Inhibition of recombinant human full length N-terminal FLAG-tagged MAO-A expressed in sf9 cells at 30 uM preincubated for 15 mins followed by substrate addition and measured after 60 mins by luminescence assay relative to control2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID559369Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP2 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID285079Antimicrobial activity against viridans group Streptococcus bovis at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID348602Antibacterial activity against methicillin-resistant Staphylococcus aureus 1 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID483192Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by microbroth dilution technique2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID348599Antibacterial activity against Streptococcus pyogenes ATCC 8736 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID763980Antibacterial activity against Haemophilus influenzae ATCC 49247 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID533004Antibacterial activity against vancomycin-intermediate Staphylococcus aureus IL phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID555320Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1651639Antibacterial activity against Staphylococcus aureus NCTC 8325 assessed as reduction in microbial growth2020Journal of natural products, 03-27, Volume: 83, Issue:3
Natural Products as Sources of New Drugs over the Nearly Four Decades from 01/1981 to 09/2019.
AID373837Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 504 after 16 passages with quinupristin-dalfopristin measured after 10 times antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID429431Antibacterial activity against Escherichia coli ATCC 25922 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID520480Antimicrobial activity against Staphylococcus aureus 168-1 isolated from osteomyelitis patient by broth macrodilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID1680073Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID404935Antibacterial activity against methicillin-susceptible Staphylococcus aureus isolate by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID522823Antibacterial activity against vancomycin-resistant Staphylococcus aureus after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID541077Cmin in cage fluid of Albino guiena pig at 75 mg/kg, ip after 12 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID535253Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-1 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID533972Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID125127In vivo antibacterial activity against Staphylococcus aureus after intramuscular administration (5 mg/kg) in mice using (MTT) mouse thigh test2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID519988Antimicrobial activity against methicillin-resistant Staphylococcus aureus nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID528838Antimicrobial activity against vancomycin-resistant Enterococcus sp. assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID534795Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID560372Antimicrobial activity against vancomycin-resistant Enterococcus faecium 1119175 by broth dilution method in presence of 4% HSA2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID555299Antibacterial activity against Tmp-resistant coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID83650Inhibitory activity against Haemophilus influenzae1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1361124Bacteriostatic activity against AcrAB-tolC deficient Escherichia coli JW5503-1 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID1609280Bactericidal activity against Staphylococcus aureus ATCC BAA42 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID292900Antimicrobial activity against Haemophilus influenzae by broth dilution method2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID68560Minimum inhibitory concentration against vancomycin resistant Enterococcus faecium OC 33122003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
AID1852665Antibacterial activity against multidrug resistant Klebsiella aerogenes ATCC43816 assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID1151622Toxicity in female rat assessed as effect on RBC count at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 7.28 x 10'12/L)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID424420Antibacterial activity against vancomycin-resistant Staphylococcus aureus HIP14300 isolated from patients foot wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID27799Volume distribution in Male Sprague-Dawley Rat (25 mg/kg po); NC denotes not calculated2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID275450Antibacterial activity against methicillin-resistant Staphylococcus aureus2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID520014Antimicrobial activity against Staphylococcus aureus A87272008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID284943Antimicrobial activity against Aerococcus spp. at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID519073Antimicrobial activity against wild type Staphylococcus aureus RN4220 measured after 21 days of subculturing by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID1056336Inhibition of human CYP3A4 assessed as terfenadine hydroxylation after 20 mins by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID562159Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID533928Antimicrobial activity against linezolid-resistant Staphylococcus aureus 1652 harboring U2500A mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID561263Antibacterial activity against Enterococcus faecalis assessed as intermediate isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID571819Antibacterial activity against Bifidobacterium dentium by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1591539Antibacterial activity against Bacillus pumilus CMCC63202 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1174905Antibacterial activity against methicillin-resistant Staphylococcus aureus MRSA 433 by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID561265Antibacterial activity against Enterococcus faecium by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID566573Antimicrobial activity against Micrococcus luteus ATCC 9341 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID11315Steady state volume distribution (Vss) of compound (10 mg/kg) after iv administration was determined in Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID569338Antibacterial activity against Staphylococcus aureus ATCC 25923 by broth micro dilution technique2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID1853453Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID562596Antimicrobial activity against Enterococcus faecalis clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID560505Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate b2k4781 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID318357Antibacterial activity against macrolide-resistant Enterococcus faecalis2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID1547713Antibacterial activity against Bacillus cereus ATCC 13061 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID387452Antibacterial activity against vancomycin-resistant Enterococcus faecalis DRCC 1532008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID410229Antibacterial activity against Klebsiella pneumoniae at 128 ug/mL by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID134113Protective dose of orally administered compound against intraperitoneally-induced septicaemia model ( vancomycin resistant Enterococci faecium D3HT12 strain) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID285030Antimicrobial activity against Rothia mucilaginosa at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID68390In vitro antibacterial activity against vancomycin-resistant Enterococcus faecium 2006 (VRE.2)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID284944Antimicrobial activity against Aerococcus spp. at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID525137Antibacterial activity against Staphylococcus aureus EMRSA-15 after 18 to 24 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID562398Antimicrobial activity against Staphylococcus aureus clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1056360Antibacterial activity against Enterococcus faecalis SR1004 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID532793Antibacterial activity against vancomycin-intermediate Staphylococcus aureus 99/3759-V after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID583889Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus isolate 360 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID523044Antimicrobial activity against Corynebacterium jeikeium by broth dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges.
AID573873Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in iv dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1167998Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 22/203 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1197160Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 27660 in po dosed ICR mouse peritonitis infection model assessed as survival rate administered at 1 hr post infection2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID559279Antimicrobial activity against Enterococcus faecalis JH2-2 harboring nucleotides at position 2576 in rrlA 2576G, rrlB 2576G, rrlC 2576G and rrlD 2576G by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID560817Antimicrobial activity against Mycobacterium tuberculosis in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID542891fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID561341Antibacterial activity against Methicillin-resistant Staphylococcus aureus by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1852688Antibacterial activity against efflux pump lacking/recombinant OM pore producing Acinetobacter baumannii incubated for 24 hrs by twofold serial dilution method
AID511385Antibacterial activity against vancomycin resistant Enterococcus faecium by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID348594Antibacterial activity against Staphylococcus aureus C463 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID571820Antibacterial activity against Bifidobacterium infantis by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1591561Bactericidal activity against Staphylococcus aureus ATCC 43300 assessed as 3 log reduction in number of colony forming units incubated for 24 hrs followed by aliquots transfer to tryptic soy agar and grown for 24 hrs2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID206451In vitro antibacterial activity against methicillin-susceptible Staphylococcus aureus (MSSA) C2214.1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID523791Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID197767Compound was evaluated for metabolic stability via In vitro Rat 5E6 cell at 50 uM concentration2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID519487Antibacterial activity against Staphylococcus aureus T1900 expressing 23S rrn3 G2576T, rrn4 G2576T and rrn5 G2576T mutants by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID1412976Antibacterial activity against methicillin-resistant Staphylococcus aureus after 16 hrs by agar dilution method2018MedChemComm, May-01, Volume: 9, Issue:5
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
AID284955Antimicrobial activity against Bacillus cereus at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID326511Tmax in Enterococcus faecalis infected Wistar rat at 600 mg, po four consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID560500Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate sh06024 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID565008Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus haemolyticus after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID533665Antimicrobial activity against Staphylococcus aureus ATCC 292132008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID284990Antimicrobial activity against Enterococcus casseliflavus at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID576877Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusi2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID340859Antimicrobial activity against vancomycin-intermediate resistant Staphylococcus aureus Mu50 graR mutant microdilution assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus.
AID1117374Antimicrobial activity against Staphylococcus aureus Efs1 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID27809Cmax value in Male Sprague-Dawley Rat at dose 10 (mg/kg iv); ND denotes not reported2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID524952Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus warneri clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID326281Antibacterial activity against methicillin-resistant Staphylococcus aureus 4913 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID522912Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1776 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1723494Antibacterial activity against Enterococcus faecium NR-32065 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID173097Cmax was evaluated in male Dawley rats at a dose of 25 mg/kg when taken perorally1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID533005Antibacterial activity against vancomycin-intermediate Staphylococcus aureus AMC11094 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID533933Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS271 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID1578412Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS119 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID1594070Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as reduction in bacterial cell viability incubated for 20 to 24 hrs by REMA method2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Design, synthesis, in-silico studies and biological screening of quinazolinone analogues as potential antibacterial agents against MRSA.
AID284998Antimicrobial activity against Enterococcus durans at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1337726Antibacterial activity against Staphylococcus aureus clinical isolate after 18 to 24 hrs by broth microdilution method2016European journal of medicinal chemistry, Nov-29, Volume: 124New isoxazolidinone and 3,4-dehydro-β-proline derivatives as antibacterial agents and MAO-inhibitors: A complex balance between two activities.
AID369445Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID753132Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 2 to 3 weeks by broth microdilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID1770357Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC43300 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID244841Minimum inhibitory concentration against Escherichia coli ATCC 259222004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID528967Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1680058Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 7 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID523808Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 4 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID533751Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID565755Antimicrobial activity against Staphylococcus haemolyticus clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID569339Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by broth micro dilution technique2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID566576Antimicrobial activity against methicillin-resistant Staphylococcus aureus 17 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID583403Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate MI assessed as bacterial count at 4 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1904917Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS 384 (USA300) incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID569344Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID1680039Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 7 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1168002Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 17301 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1451759Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 4.5 days pretreated 24 hrs prior to bacterial infection measured 108 hrs post infection relative 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID292670Antibacterial activity against Streptococcus pneumoniae by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials.
AID285034Antimicrobial activity against Rothia mucilaginosa at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID370038Normalized AUC in Staphylococcus aureus-infected mouse localized thigh infection model at 25 mg/kg2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1241211Binding affinity to 5'-FAM-pre-miR-373 (unknown origin) after 4 hrs by fluorescence assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID1760596Efflux ratio of MIC for Escherichia coli 25922 to MIC for Escherichia coli JW55032021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID53320Inhibitory activity against Escherichia coli DNA gyrase in supercoiling assay; Not tested2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID564813Bactericidal activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID574547Increase in PSMalpha levels in Staphylococcus aureus USA300 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID285157Antimicrobial susceptibility of tetracycline-resistant Streptococcus pneumoniae from respiratory tract disease patient assessed as percent susceptible isolates2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Clonal diversity and resistance mechanisms in tetracycline-nonsusceptible Streptococcus pneumoniae isolates in Poland.
AID1596556Antibacterial activity against vancomycin resistant Enterococcus faecium ATCC 700221 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID390341Antimicrobial activity against Pseudomonas aeruginosa 14732008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID562182Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 36 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID591662Antimicrobial activity against multidrug-resistant Enterococcus faecium after 18 hrs by agar dilution method2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
AID630558Antibacterial activity against Enterococcus faecalis after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID571768Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-I626M mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID373658Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID575102Antimicrobial activity against Streptococcus pneumoniae serotype 19F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID577129Terminal half-life in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1594376Antibacterial activity against Escherichia coli BW25113 after 18 to 24 hrs in presence of colistin by broth microdilution method2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID284981Antimicrobial activity against Enterococcus avium at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1647977Cytotoxicity against human Caco2 cells by CCK8 assay2020Journal of natural products, 02-28, Volume: 83, Issue:2
The Isolation of Pyrroloformamide Congeners and Characterization of Their Biosynthetic Gene Cluster.
AID1271207Solubility of compound at pH 10.2 by HPLC analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID565751Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID319983Antimicrobial activity against Staphylococcus aureus2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID1862428Antibacterial activity against methicillin-resistant Staphylococcus aureus USA 300 (ARLG 1570) assessed as reduction in visible bacterial growth incubated for 18 to 20 hrs by CLSI based broth microdilution analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms.
AID1649291Antibacterial activity against Streptococcus pneumoniae type 1 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID373656Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1877885Antibacterial activity against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus Mu50 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID285347Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20010734 in CCY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID516166Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolates assessed as susceptible isolates by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID548742Antimicrobial activity against Vancomycin-nonsusceptible Enterococcus faecalis assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID571812Antibacterial activity against Clostridium sporosphaeroides by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID717213Antimicrobial activity against methicillin-resistant Staphylococcus aureus CCARM 3090 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID533935Antimicrobial activity against linezolid-resistant Staphylococcus aureus 004-737X harboring plasmid borne cfr gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID244880Minimal inhibitory concentration against Salmonella abony NCTC 60172004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID404950Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus sp. assessed as percent susceptible isolates by CLSI dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
AID206646Antibacterial activity against methicillin resistant Staphylococcus aureus (MRSA)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1076827Antibacterial activity against Escherichia coli ATCC 25922 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID383570Antibacterial activity against multidrug-resistant Streptococcus pneumoniae ATCC 700904 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID542881fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID205743In vitro antibacterial activity against Staphylococcus epidermidis Q004 (S.e.1)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID528691Antibacterial activity against Enterococcus faecalis ATCC 51575 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID429418Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID244921Minimal inhibitory concentration against Serratia marcescens ATCC 129992004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID387462Drug elimination in Swiss albino mouse at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID1514452Antitubercular activity against kanamycin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1680046Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 10 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID292606Antimicrobial activity against Staphylococcus aureus 15187 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID348597Antibacterial activity against Enterococcus faecium C803 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID645043Antibacterial activity against methicillin-resistant Staphylococcus aureus C530 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID1168011Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 31176 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID558735Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 50 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1414196Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 incubated for 24 hrs followed by plating onto tryptic soy agar plates and further incubated for 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID533393Antimicrobial activity against Clostridium innocuum by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID410201Antibacterial activity against Staphylococcus aureus by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID577132Mean residence time in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID583203Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate MU50 after 24 hrs by microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID532795Antibacterial activity against vancomycin-intermediate Staphylococcus aureus IL after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1519036Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID542708fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day administered as 6 divided doses every 4 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1852682Antibacterial activity against efflux pump lacking Escherichia coli assessed as inhibition of bacterial growth
AID260744Antibacterial activity against Escherichia coli J532006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID245011Minimal inhibitory concentration against Staphylococcus epidermidis ATCC 122282004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID285144Antimicrobial activity against viridans group Streptococcus anginosus by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1547714Antibacterial activity against Bacillus licheniformis ATCC 12759 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID562158Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID291410Antibacterial activity against methicillin-resistant Staphylococcus aureus 05-3 after 18 to 24 hrs2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and antibacterial activity of novel fluoroquinolones containing substituted piperidines.
AID577094T>MIC in Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID278917Antibacterial activity against linezolid-susceptible Enterococcus faecium2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID576870Bactericidal activity against 14 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID571821Antibacterial activity against Bifidobacterium longum by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID1126483Antimicrobial activity against penicillin- and erythromycin-resistant Streptococcus pneumoniae in presence of 2.5% horse blood2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID582985Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS06188 harboring MLST sequence type ST78 and pulsotype A expressing vanA gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1501362Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 10 after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID523810Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID429420Antibacterial activity against methicillin-sensitive coagulase-negative Staphylococcus by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID562161Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID558707Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID637968Antibacterial activity against Escherichia coli ATCC 25922 after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID292609Antimicrobial activity against Enterococcus faecalis ATCC 29212 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID1451764Antibacterial activity against Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid for 4.5 days administered 6 hrs post bacterial infection measured 108 hrs post infection relative to co2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID285354Decrease in Panton-Valentine leukocidin level in community acquired methicillin-resistant Staphylococcus aureus HT20020488 in CYY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID558490Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID524717Antibacterial activity against linezolid-resistant Staphylococcus aureus ATCC 29213 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID528845Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1117372Antimicrobial activity against Staphylococcus aureus SG511 assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID533400Antimicrobial activity against Clostridium paraputrificum assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID283397Antimicrobial activity against Nocardia transvalensis after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID1174902Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID1660513Antibacterial activity against Staphylococcus aureus ATCC 25923 after 16 hrs by CLSI-based broth microdilution method2020Journal of natural products, 06-26, Volume: 83, Issue:6
Synthesis of the Cyanobacterial Antibiotics Anaephenes A and B.
AID205740In vitro antibacterial activity against Staphylococcus epidermidis2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and antibacterial activity of oxazolidinone containing sulphonyl group.
AID374009Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 17 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID565753Antimicrobial activity against oxacillin-resistant Staphylococcus haemolyticus clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID477371Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 70069 after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID1308239Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus ATCC 292132016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID285143Antimicrobial activity against beta hemolytic Streptococcus group G by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1151621Toxicity in female rat assessed as effect on WBC count at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 3.66 x 10'9/L)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID370008Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 12.5 mg/kg/day, po administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burd2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID541814Antimicrobial activity against Enterococcus hirae clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1778667Ratio of MBC to MIC against penicillin-susceptible Bacillus subtilis ATCC 93722021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID285075Antimicrobial activity against viridans group Streptococcus anginosus at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID542700fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg /day administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID207720In vitro minimum inhibitory concentration (MIC) against Staphylococcus aureus UC126732003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID285517Antibacterial activity against Enterococcus faecium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID285543Cmax in mouse at 20 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID535776Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID285160Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID267720Antimicrobial activity against Staphylococcus aureus2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings.
AID559794Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at 2 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID68070Antibacterial activity against vancomycin - resistant Enterococcus faecium (OC 3312 VRE)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID1197114Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1852663Antibacterial activity against multidrug resistant Klebsiella pneumoniae ATCC43816 assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID1407934Antibacterial activity against Streptococcus pyogenes ARC838 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID1393959Antibacterial activity against methicillin resistant Staphylococcus epidermidis NR 46386 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID1703732Antibacterial activity against methicillin-resistant Streptococcus pneumoniae ATCC 700677 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID410106Antimicrobial activity against Linezolid-resistant Enterococcus faecalis P5 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID576882Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1852677Antibacterial activity against efflux pump lacking/recombinant OM pore producing Acinetobacter baumannii assessed as inhibition of bacterial growth
AID542704fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID542880fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1252237Antimicrobial activity against Staphylococcus aureus ATCC 292132015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
Rapid synthesis and antimicrobial activity of novel 4-oxazolidinone heterocycles.
AID319161Elimination half life in human2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1174913Antibacterial activity against linezolid-sensitive methicillin-sensitive Staphylococcus aureus by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID1591538Antibacterial activity against Bacillus subtilis ATCC 9372 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1415065Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 1 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID544636Antimicrobial activity against Staphylococcus aureus Xen 30 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID558503Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID387455Antibacterial activity against beta-lactamase deficient Moraxella catarrhalis DRCC 3002008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID583389Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate MU50 assessed as bacterial count at 16 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID576880Bactericidal activity against 24 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID67399In vitro antibacterial activity against Enterococcus faecalis EFS008 (E.f.2)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID581027Inhibition of cell wall synthesis in Staphylococcus epidermidis ATCC 23760 assessed as incorporation of [3H]N-acetylglucosamine at 2 ug/ml after 60 mins by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID1677802Antibacterial activity against Pseudomonas aeruginosa ATCC27853 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID373314Antibacterial activity against vancomycin-sensitive Enterococcus clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID531562Antibacterial activity against coagulase-negative Staphylococcus warneri obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID542897fAUC ( 24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 700 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1680038Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 8 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID562615Antimicrobial activity against methicillin-sensitive Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1474195Antibacterial activity against Escherichia coli 1411 harboring delta-acrAB after 18 to 22 hrs in absence of colistin by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1547720Antibacterial activity against Enterococcus faecium NCTC 7171 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID1596542Antibacterial activity against Staphylococcus aureus NRS107 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID1154472Antibacterial activity against clinical isolate of methicillin-sensitive Staphylococcus aureus infected in iv dosed mouse administered 1 hr after infection for 4 days2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID1680064Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID519998Antimicrobial activity against Streptococcus pyogenes2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID687499Drug excretion in rat urine2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID542904Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial regrowth at 300 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID560799Absorption half life in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID429423Antibacterial activity against vancomycin-sensitive Enterococcus by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID528844Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID534788Antimicrobial activity against community-acquired methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID532796Antibacterial activity against vancomycin-intermediate Staphylococcus aureus PC after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID533631Antimicrobial activity against Propionibacterium acnes by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID24540terminal disposition half-life was evaluated in male Dawley rats at a dose of 25 mg/kg when taken perorally1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID523793Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1574836Antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus aureus by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID525130Antibacterial activity against Staphylococcus aureus KM187 after 18 to 24 hrs by broth microdilution method selected after 16 ug/ml drug exposure for 6 hrs by culture absorbance method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID541088Antibacterial activity against 1 x10'6 to 5 x10'6 CFU/ml methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as log decrease in bacterial count at 4 times MIC after 24 hrs by time kill study2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID390331Antimicrobial activity against quinolone-resistant Streptococcus pneumoniae 3762008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID206469The compound was evaluated for its anti-bacterial activity against methicillin resistant Staphylococcus aureus1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID573157Antibacterial activity against vancomycin-resistant Enterococcus faecium assessed as resistant isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID575078Antimicrobial activity against Streptococcus pneumoniae serotype 35B assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1327115Antibacterial activity against Bacillus subtilis NCIM 2010 at 10 ug/ml measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID520224Antimicrobial activity against Enterococcus faecium A9621 by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID541069Tmax in cage fluid of Albino guiena pig at 75 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID209622In vitro minimum inhibitory concentration against Streptococcus pyogenes penicillin sensitive2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID558483Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1308262Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS70 in ICR mouse neutropenic thigh infection model assessed as reduction in bacterial load at 10 mg/kg, sc tid administered every 8 hrs starting from 1 hr post infection and meas2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID562588Antimicrobial activity against Enterococcus faecium expressing VanA gene clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1873907Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID523804Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1671917Antibacterial activity against Enterococcus faecium ATCC 35667 assessed as minimum inhibitory concentration required for >=90% inhibition of bacterial growth by CLSI protocol based broth microdilution assay2019European journal of medicinal chemistry, Apr-01, Volume: 167An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors.
AID576409AUC in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID563495Antibacterial activity against vancomycin-resistant Enterococcus faecalis EF NJ1 infected in New Zealand White rabbit assessed as log reduction of bacterial count in aortic valve vegetations at 10 mg/kg, administered through ear vein every 12 hrs for 4 da2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID1311363Antibacterial activity against Pseudomonas aeruginosa PA14 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID729177Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in iv dosed systemic infection mouse model administered 1 hr post infection measured after 48 hrs2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID564323Antimicrobial activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 assessed as resistant bacteria on coverslip selected on 4 ug/ml of compound measured on day 11 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID1269335Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
AID284964Antimicrobial activity against Corynebacterium amycolatum at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID558499Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1233139Antibacterial activity against patient-derived methicillin-resistant Staphylococcus aureus K1 after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID370025Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 6.25 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1519035Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID531564Antibacterial activity against methicillin-susceptible, coagulase-negative Staphylococcus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1852681Antibacterial activity against recombinant OM pore producing Escherichia coli assessed as inhibition of bacterial growth
AID390332Antimicrobial activity against ampicillin-resistant Haemophilus influenzae 17422008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID1680010Antibiofilm activity against Escherichia coli ATCC 25922 assessed as inhibition of biofilm formation incubated for 24 hrs by crystal violet staining assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID285345Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20041010 in Mueller-Hinton medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID1117396Antimicrobial activity against Mycobacterium vaccae IMET assessed as inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1395979Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA-1707 planktonic cells after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID291411Antibacterial activity against Streptococcus pneumoniae 05-9 after 18 to 24 hrs2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and antibacterial activity of novel fluoroquinolones containing substituted piperidines.
AID1151776Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0605 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 5 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID552855Antibacterial activity against Staphylococcus aureus infected in po dosed in vivo acute model administered bid for 1 day2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID285130Antimicrobial activity against viridans group Streptococcus sanguinis at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID535023Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-22 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID562625Antimicrobial activity against Group A Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1194834Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID1180582Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC516-2F to MIC for Staphylococcus aureus ARC5162014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID730384Antibacterial activity against macrolides, lincosamides, streptogramin B and methicillin-resistant Staphylococcus aureus 1015-00 assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID1680012Antibiofilm activity against 24 hrs preformed biofilm of Escherichia coli ATCC 25922 assessed as eradication of preformed biofilm incubated for 24 hrs by crystal violet staining assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID519992Antimicrobial activity against vancomycin-susceptible Enterococcus faecium nosocomial isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID590062Antibacterial activity against Haemophilus influenzae by agar dilution method2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1400053Antibacterial activity against Klebsiella pneumoniae ATCC 12019 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID326283Antibacterial activity against methicillin-resistant Staphylococcus aureus 5098 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID1190638Inhibition of biofilm formation of Pseudomonas aeruginosa PAO1 incubated for 18 hrs by crystal violet staining based spectroscopy2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Biofilm inhibition of linezolid-like Schiff bases: synthesis, biological activity, molecular docking and in silico ADME prediction.
AID323786Antibacterial activity against methicillin-resistant Staphylococcus aureus Xen1 infected neutropenic CD1 mouse assessed as mouse survival at 50 mg/kg, sc after 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID561745Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as susceptible isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID564815Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1193400Inhibition of recombinant Bacillus anthracis PurE assessed as inhibition of 4-carboxy-amino-imidazole ribonucleotide to N5-carboxy-amino-imidazole ribonucleotide conversion preincubated for 1.5 mins at 10 uM by mass spectrometry analysis2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID591661Antimicrobial activity against multidrug-resistant Enterococcus faecalis after 18 hrs by agar dilution method2011Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.
AID763981Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID520000Antimicrobial activity against Moraxella catarrhalis2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID292613Antimicrobial activity against Moraxella catarrhalis M2 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID575083Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID576400Residual concentration at the end of the administration interval in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID326282Antibacterial activity against methicillin-resistant Staphylococcus aureus 4930 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID410118Antimicrobial activity against mef (A) Streptococcus pneumoniae 02J1175 in orally dosed mouse peritonitis model2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID548534Antimicrobial activity against viridans group Streptococcus by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID1446753Bactericidal activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID759692Antibacterial activity against methicillin-resistant Staphylococcus aureus 433 assessed as growth inhibition after 18 to 24 hrs by broth microdilution method2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID520230Antimicrobial activity against vancomycin-resistant Enterococcus faecalis 03B10692008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1421223Antibacterial activity against linezolid-resistant Enterococcus faecalis by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID1596566Bactericidal activity against vancomycin resistant Staphylococcus aureus VRS12 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID369673Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 25 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID528971Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1265130Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 259232015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID410203Antibacterial activity against Staphylococcus epidermidis by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID66125Antibacterial activity against Enterococcus species2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1594364Antibacterial activity against methicillin-resistant Staphylococcus epidermidis NRS101 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID559557Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP6 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID576394Cmax in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID528975Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1400038Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1493805Antibacterial activity against Staphylococcus aureus VRS10 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID520012Antimicrobial activity against Staphylococcus aureus A78172008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID511433Antimicrobial activity against Clostridium perfringens LFM1 assessed as resistance breakpoint by DANMAP method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID576892Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID499112Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected immunocompromized SKH1 mouse assessed as lesion volume at 25 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1181 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID549014Antimicrobial activity against Beta-hemolytic Streptococcus assessed as percent resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID576875Bactericidal activity against 2 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1770347Antibacterial activity against clinical isolate Staphylococcus aureus C1 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID270149Antibacterial activity against gram positive methicillin-resistant Staphylococcus aureus OC 28782006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.
AID533752Antimicrobial activity against methicillin-susceptible Staphylococcus aureus SA040 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID552830Antibacterial activity against methicillin-resistant Staphylococcus aureus2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID1472753In vivo anti-virulence activity against methicillin-resistant Staphylococcus aureus NRS271 infected in BALB/c mouse model assessed as reduction in bacterial load in heart at 0.4 mg bid for 4.5 days administered intraperitoneally 6 hrs post infection by se2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID577116ABBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID29427Oral bioavailability in rat (Sprague-Dawley) (male) (dose 10 mg/kg i.v.)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID571804Antibacterial activity against Clostridium hypermegas by CLSI M11-A6 agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
AID565760Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus clinical isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID283614Antimicrobial activity against Enterococcus faecalis 9 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID383555Antibacterial activity against Bacillus pumilus ATCC 14884 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID319160Oral bioavailability in human2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID206787Inhibitory activity against MSSA1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID41285Inhibitory activity against Bacteroides fragilis1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID285141Antimicrobial activity against beta hemolytic Streptococcus group C by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1168010Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 5396 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID577124Residual concentration at the end of the administration interval in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID533946Antimicrobial activity against community acquired methicillin-resistant Staphylococcus aureus NRS192 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1168023Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 5484 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1904915Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS 119 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1434676Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 0204 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1873889Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^6 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID548744Antimicrobial activity against Vancomycin-nonsusceptible Enterococcus faecium assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID564832Bactericidal activity against methicillin-resistant coagulase-negative Staphylococcus sciuri after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID528724Antibacterial activity against Streptococcus oralis clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1151761Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0612 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID573148Antibacterial activity against penicillin-nonsusceptible Streptococcus viridans assessed as resistant isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID297959Antibacterial activity against Streptococcus pneumoniae 548 infected mouse lung infection model assessed as reduction in bacterial count at 40 mg/kg/day, po relative to control2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.
AID523790Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID424758Antibacterial activity against methicillin-sensitive Staphylococcus aureus MB2865 after 20 hrs by twofold serial broth dilution method in presence of 50% human serum2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID565488Ratio of MBC to MIC for methicillin-resistant Staphylococcus aureus2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID1421232Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolates by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID531573Antibacterial activity against Staphylococcus intermedius obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID581033Bacteriostatic activity against Staphylococcus epidermidis ATCC 23760 at 4 X MIC after 24 hrs by time-kill analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID756089Antibacterial activity against Enterococcus faecalis assessed as growth inhibition after 16 hrs by agar dilution method2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
AID576655Bactericidal activity against 24 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID576650Bactericidal activity against 2 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID410228Antibacterial activity against Pseudomonas aeruginosa at 128 ug/mL by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID559364Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP1 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID533010Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR1 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1151731Antibacterial activity against Streptococcus anginosus2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1312942Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID244829Minimum inhibitory concentration against Staphylococcus aureus ATCC 259232004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
AID477374Antibacterial activity against Enterococcus faecalis MTCC 439 after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID1161216Antimicrobial activity against Staphylococcus aureus ATCC 33591 in septicemia mouse model assessed as mortality of host at 20 mg/kg administered intragastrically measured after 14 days relative to control2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID1474259Ratio of MBC50 to MIC50 for vancomycin-resistant Enterococcus faecium ATCC 7002212017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID285108Antimicrobial activity against viridans group Streptococcus mutans at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285153Antimicrobial activity against viridans group Streptococcus sanguinis by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID564808Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus simulans after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID289865Antibacterial activity against Staphylococcus aureus ATCC 292132007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
AID577110ABBC (0 to 24 hrs) in Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID775531Inhibition of CYP2D6 in human liver microsomes assessed as dextromethorphan O-demethylation after 20 mins by LC/MS/MS analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID308920Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID524965Antibacterial activity against methicillin-resistant coagulase-negative unspeciated Staphylococcus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID576887Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID285121Antimicrobial activity against viridans group Streptococcus parasanguis at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1409848Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.1 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 42018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID284967Antimicrobial activity against Corynebacterium jeikeium at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID560503Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 6zjsau7 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID541048Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 25 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID284972Antimicrobial activity against Corynebacterium pseudodiphtheriticum at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285155Antimicrobial activity against viridans group Streptococcus mutans by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID560575Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 51559 expressing vanA gene assessed as change in bacterial count at 16 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1304844Induction of hemolysis in human RBC at 200 uM incubated for 1 hr2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID308925Antibacterial activity against multidrug-resistant Streptococcus pneumoniae ATCC 700904 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID1168014Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 27/16917 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID278859Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID524953Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus xylosus clinical isolate by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Comparative surveillance study of telavancin activity against recently collected gram-positive clinical isolates from across the United States.
AID533664Antimicrobial activity against Staphylococcus aureus RN1024-tms2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID293838Antibacterial activity against methicillin-resistant Staphylococcus aureus MF5352007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
A new class of anti-MRSA and anti-VRE agents: preparation and antibacterial activities of indole-containing compounds.
AID1591552Induction of Bacillus subtilis FtsZ polymerization in presence of GTP at 5 ug/ml measured over 30 mins by microtiter plate-based light-scattering assay2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID531553Antibacterial activity against methicillin susceptible Staphylococcus aureus obtained from complicated skin and skin structure infections by agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro activity of ceftobiprole against pathogens from two phase 3 clinical trials of complicated skin and skin structure infections.
AID1504965Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days under aerobic condition by alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID326287Antibacterial activity against methicillin-resistant Staphylococcus aureus 4342 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID560810Elimination half life in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID520008Antimicrobial activity against Staphylococcus aureus ATCC 292132008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1151769Antibacterial activity against vancomycin-sensitive/high-level gentamycin-resistant Enterococcus faecalis isolate HH22 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID267723Antimicrobial activity against Haemophilus influenzae2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings.
AID573888AUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID710138Antibacterial activity against methicillin-susceptible Staphylococcus aureus2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria.
AID1703708Antibacterial activity against methicillin-sensitive Staphylococcus aureus NRS107 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1432972Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv
AID1151757Antibacterial activity against vancomycin-resistant Enterococcus faecalis isolate EFL 40412014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID206470The compound was evaluated for its anti-bacterial activity against methicillin susceptible Staphylococcus aureus1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID368277Bactericidal activity against vancomycin-intermediate Staphylococcus aureus by microdilution technique2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID1852674Antibacterial activity against multidrug resistant Acinetobacter baumannii AYE assessed as inhibition of bacterial growth incubated for 24 hrs in M9-MOPS medium by twofold serial dilution method
AID383556Antibacterial activity against Bacillus cereus ATCC 11778 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID562635Antimicrobial activity against Corynebacterium spp. assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID573871Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in sc dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID575043Cmin in patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID244836Minimum inhibitory concentration against Staphylococcus pyogenes ATCC 86682004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
AID1778092Antibacterial activity against Bacillus subtilis 168 assessed as inhibition of bacterial growth incubated for 18 hrs by broth microdilution method
AID533931Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS120 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID576419Volume of distribution at steady state in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1553383Inhibition of CYP2D6 (unknown origin)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID571925Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-G616N mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID562388Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID576425Antibacterial activity against Staphylococcus aureus RN4220 by agar dilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID522821Antibacterial activity against vancomycin-intermediate Staphylococcus aureus after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID285128Antimicrobial activity against viridans group Streptococcus salivarius at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1778668Ratio of MBC to MIC against penicillin-susceptible Bacillus pumilus CMCC 632022021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID245129Minimum inhibitory concentration against Staphylococcus aureus (strain A15090) in absence of calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID69617Antibacterial activity against Escherichia coli (EC1008 )2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID112685In vivo antibacterial activity against Staphylococcus aures strain UC 9213 administered perorally in mice1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID522920Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 815 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1430398Antibacterial activity against Staphylococcus aureus 209P after 24 to 48 hrs by macro-broth dilution method2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Methylsulfonyl benzothiazoles (MSBT) derivatives: Search for new potential antimicrobial and anticancer agents.
AID1304832Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID369443Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae after 20 to 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activity of telavancin against gram-positive clinical isolates recently obtained in Europe.
AID1350034Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 5 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1887539Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 16 to 18 hrs by broth microdilution method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID530051Antimicrobial activity against Staphylococcus aureus 286607-R1 harboring wild type gyrB by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID542687fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1519268Antibacterial activity agianst vancomycin-resistant Enterococcus faecium2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID1778644Antibacterial activity against penicillin-susceptible Bacillus pumilus CMCC 63202 assessed as bacterial growth inhibition by broth dilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID1883846Antibacterial activity against Mycobacterium tuberculosis H37Rv in acute Mtb infection BALB/c mouse model assessed as reduction in log10 CFU in lungs at 100 mg/kg, po for 3 weeks2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID564828Bactericidal activity against methicillin-resistant coagulase-negative Staphylococcus simulans after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID567454Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK6 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID1451761Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid for 4.5 days administered 6 hrs post bacterial infection measured 108 hrs post infection relative to 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID68416Minimum inhibitory concentration (MIC) against Enterococcus faecium OC 3312 (VRE)2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID308728Antibacterial activity against Streptococcus pyogenes C203 SP1-1 by micro-broth method2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID1904923Antibacterial activity against Staphylococcus epidermidis NRS 101 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID373847Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 Hershey after 50 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID205691Minimum inhibitory concentration against methicillin resistant Staphylococcus aureus OC 28782003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
AID1609281Antibacterial activity against vancomycin-resistant Staphylococcus aureus 12 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID573889AUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID284965Antimicrobial activity against Corynebacterium amycolatum at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID206594In vitro antibacterial activity against Staphylococcus aureus 29213A (S.a.3)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID609040Antibacterial activity against Bacillus cereus ATCC 11778 after 24 hrs by broth microdilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID695447Cytotoxicity against human CHO cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1303403Antibacterial activity against vancomycin-resistant Enterococcus faecium after 24 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID1873911Antibacterial activity against Streptococcus dysgalactiae incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID285046Antimicrobial activity against Enterococcus durans by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285080Antimicrobial activity against viridans group Streptococcus bovis at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID564817Bactericidal activity against methicillin-resistant coagulase-negative Staphylococcus hominis after 24 hrs by plate counting method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1190639Antibacterial activity against Bacillus subtilis NCIM-2063 incubated for 24 hrs by two fold serial dilution method2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Biofilm inhibition of linezolid-like Schiff bases: synthesis, biological activity, molecular docking and in silico ADME prediction.
AID533957Antimicrobial activity against Listeria monocytogenes infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID576642Bactericidal activity against 12 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID522915Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1838 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID374001Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey after 20 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID297119Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1446759Bactericidal activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1888848Antibacterial activity against Staphylococcus aureus K1758 measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID69193Minimum inhibitory concentration (MIC) against Escherichia coli OC 2530 (HS)2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID541537Antimicrobial activity against vancomycin-resistant Enterococcus faecalis clinical isolate after 18 to 22 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Establishment of in vitro susceptibility testing methodologies and comparative activities of piperacillin in combination with the penem {beta}-lactamase inhibitor BLI-489.
AID1879694Antimycobacterial activity against PAS resistant Mycobacterium tuberculosis H37Rv harboring R49W mutant assessed as inhibition of bacterial growth measured after 2 weeks by microbroth dilution method2022European journal of medicinal chemistry, Mar-15, Volume: 232Synthesis and biological evaluation of orally active prodrugs and analogs of para-aminosalicylic acid (PAS).
AID387451Antibacterial activity against vancomycin-susceptible Enterococcus faecalis DRCC 0342008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID522923Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 1472 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID560581Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 51559 expressing vanA gene assessed as change in bacterial count at 4 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1076834Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID1861535Volume of distribution in Wistar rat at 30 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID775547Antibacterial activity against Enterococcus faecalis SR1004 clinical isolate assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID145139In vitro antibacterial activity against Mycobacterium tuberculosis strain H37Rv1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID11426Cmax in male rat2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1770340Antibacterial activity against penicillin-susceptible Bacillus pumilus CMCC63202 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID533929Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS127 by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID535262Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-10 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID245194In vitro minimum inhibitory concentration against Staphylococcus saprophyticus (ATCC 15305)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID560366Antimicrobial activity against vancomycin-resistant Enterococcus faecium 1119175 by broth dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID458459Antimicrobial activity against Escherichia coli X580 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID284993Antimicrobial activity against Enterococcus casseliflavus at 4 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1514449Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1594359Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1395675Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS119 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1474204Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1395674Antibacterial activity against methicillin-sensitive Staphylococcus aureus NRS107 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID467836Antibacterial activity against Bacillus cereus MTCC 430 after 24 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
AID577130Mean residence time in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID319154Toxicity in dog at 20 mg/kg for 30 days2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1312941Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA200 NRS383 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID1591540Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID533979Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID560376Selectivity ratio of MIC for Enterococcus faecalis ATCC 51299 in presence of 4% HSA to MIC for Enterococcus faecalis 512992009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID576664Bactericidal activity against 24 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1161142Antimicrobial activity against Escherichia coli isolate 2 after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID560582Bactericidal activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 expressing vanB gene assessed as change in bacterial count at 4 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1703722Antibacterial activity against methicillin-resistant Staphylococcus epidermidis NRS101 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID1400052Bactericidal activity against Streptococcus pneumoniae ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID577096T>MIC in Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1361106Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS119 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID571764Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring acrB::rpsLneo mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1058378Antimicrobial activity against vancomycin -resistant Enterococcus faecalis after 24 hrs by microdilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Anti-tubercular agents. Part 8: synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles.
AID1361103Bacteriostatic activity against vancomycin-intermediate Staphylococcus aureus NRS1 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID595021Antibacterial activity against Enterococcus faecalis ATCC 292122011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
AID67398In vitro antibacterial activity against Enterococcus faecalis C6301 (E. f. 1)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID576436Bactericidal activity against 48 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID383565Antibacterial activity against Staphylococcus aureus ATCC 9144 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID374004Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 24 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID558481Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1474216Bacteriostatic activity against vancomycin-resistant Enterococcus faecalis HM-201 assessed as reduction in CFU at 4 times MIC after after 24 hrs2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1596555Antibacterial activity against vancomycin resistant Enterococcus faecalis ATCC 51299 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID207215In vitro minimum inhibitory concentration against Staphylococcus aureus MRQR2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID69130In vitro inhibitory activity against protein synthesis was determined by transcription/translation assay with Escherichia coli S30 Extract System.2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID1174906Antibacterial activity against methicillin-resistant Staphylococcus aureus MRSA F511 by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID410112Antimicrobial activity against methicillin-resistant Staphylococcus aureus 67-0 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID284975Antimicrobial activity against Corynebacterium pseudodiphtheriticum at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID303962Antibacterial activity against vancomycin-resistant Enterococcus faecium by micro-broth technology2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID1233128Antibacterial activity against Enterococcus faecalis after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID562627Antimicrobial activity against Group B Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID520734Antimicrobial activity against methicillin-resistant Staphylococcus aureus CM05 by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Transcriptional and translational control of the mlr operon, which confers resistance to seven classes of protein synthesis inhibitors.
AID205561Minimum inhibitory concentration against Staphylococcus aureus ATCC 292132004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID577095T>MIC in Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1412974Antibacterial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by agar dilution method2018MedChemComm, May-01, Volume: 9, Issue:5
The semi-synthesis, biological evaluation and docking analysis of the oxime, hydrazine and hydrazide derivatives of platensimycin.
AID562169Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 after 50 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID525133Antibacterial activity against Staphylococcus aureus KM52 after 18 to 24 hrs by broth microdilution method selected after 16 ug/ml drug exposure for 6 hrs by culture absorbance method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID604288Antibacterial activity against Staphylococcus aureus ATCC 13709 (Smith) after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID560825fT>MIC in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID318354Antibacterial activity against methicillin and macrolide-resistant Staphylococcus aureus2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID581017Inhibition of protein synthesis in Staphylococcus epidermidis ATCC 23760 assessed as incorporation of [14C]isoleucine at 2 ug/ml by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID1272267Antimicrobial activity against vancomycin-resistant Enterococcus faecalis MMX 486 expressing VanA after 18 to 20 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.
AID202107Inhibitory activity against Streptococcus pneumoniae UC99122000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID563494Antibacterial activity against vancomycin-susceptible Enterococcus faecalis EF 12704 infected in New Zealand White rabbit assessed as log reduction of bacterial count in aortic valve vegetations at 10 mg/kg, administered through ear vein every 12 hrs for 2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID207009Antibacterial activity against ciprofloxacin resistant Staphylococcus aureus (SA1009 CipR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID753126Antibacterial activity against Staphylococcus aureus MTCC 96 assessed as growth inhibition after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID1446751Bactericidal activity against Staphylococcus aureus RN4220 NRS107 clinical isolate after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1649288Antibacterial activity against Vancomycin-resistant Enterococcus faecium SR7940 (VanA) assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID555311Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 345 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID206511In vitro antibacterial activity against Staphylococcus hominis2003Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14
Synthesis and antibacterial activity of oxazolidinone containing sulphonyl group.
AID284961Antimicrobial activity against Corynebacterium spp. at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID391592Antibacterial activity against penicillin-resistant Streptococcus pneumoniae PR44 by agar dilution method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials.
AID574067fCmax in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID285129Antimicrobial activity against viridans group Streptococcus salivarius at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1271231Antibacterial activity against clinical isolate Neisseria meningitidis 184 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID295156Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by microdilution broth method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID561738Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as resistant isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1873906Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID388048Antimicrobial activity against Candida albicans MY1055 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID558712Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID429416Antibacterial activity against Staphylococcus aureus ATCC 25923 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID1168027Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 13246 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID577144Volume of distribution at steady state in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1770356Bactericidal activity against erythromycin-susceptible Staphylococcus aureus ATCC 25923 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID585162Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA G2505A mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID520223Antimicrobial activity against Enterococcus faecium A89482008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID519079Antimicrobial activity wild type Escherichia coli SQ110 by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID210379In vitro antibacterial activity against Streptococcus pneumoniae strain UC 99121996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1117385Antimicrobial activity against Micrococcus luteus ATCC 10240 assessed as unclear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID559563Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP8 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1151747Antibacterial activity against Staphylococcus aureus measured after 9 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1168012Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 31386 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID559288Antimicrobial activity against recombination-deficient Enterococcus faecalis JH2-2 recA harboring nucleotides at position 2576 in rrlA 2576T, rrlB 2576G, rrlC 2576T and rrlD 2576T after 10, 11 passages under Linezolid selective pressure by agar dilution m2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID1710579Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS385 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1760593Antibacterial activity against vancomycin resistant Enterococcus faecium 700221 assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID524725Antibacterial activity against linezolid-resistant Enterococcus faecium 03B1075 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID1778646Antibacterial activity against erythromycin-susceptible Streptococcus pyogenes clinical isolate 1 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID287258Antimicrobial activity against Staphylococcus aureus ATCC 25922 in presence of 50% human plasma by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID373991Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 16 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID542902Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial regrowth at 100 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1451757Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid for 4.5 days treated 24 hrs prior to bacterial infection measured 108 hrs post infection relative to 2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID201410Inhibitory activity against Methicillin-susceptible Staphylococcus aureus UC92132000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID533937Antimicrobial activity against linezolid-resistant Staphylococcus aureus ATCC 29213 by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID559778Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID283159Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2526 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1250831Inhibition of Staphylococcus aureus FabI assessed as reduction in inhibition of reduction of trans-2-octenoyl N-acetylcysteamine substrate by spectrophotometry2015Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20
Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent.
AID1393952Antibacterial activity against methicillin resistant Staphylococcus aureus ATCC 43300 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID523783Antimicrobial activity against linezolid-resistant Staphylococcus aureus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID558529Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID729225Antibacterial activity against methicillin-sensitive Staphylococcus aureus after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID392203Antibacterial activity against Enterococcus faecalis MGH-2 EF1-1 by micro broth method2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents.
AID522926Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 813 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID541040Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 25 mg/kg measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID67394In vitro antibacterial activity against Enterococcus faecalis 29212A (E.f.1)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID1400058Bactericidal activity against Escherichia coli ATCC 10798 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID582986Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0661 harboring MLST sequence type ST78 and pulsotype C expressing vanM gene cluster isolated from exudate of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID519075Antimicrobial activity mutS-expressing Staphylococcus aureus RN4220 by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID541036Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 25 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID439893Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 2 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID558489Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID726198Antibacterial activity against vancomycin-resistant Enterococcus faecalis C474 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID1435921Antibacterial activity against mupirocin/rifampicin-resistant Staphylococcus aureus RN4220 NRS107 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID535029Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-68 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID278858Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID1539448Antibacterial activity against Methicillin-resistant Staphylococcus aureus USA700-NRS386 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID1539441Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS384-USA300 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID285022Antimicrobial activity against Listeria monocytogenes at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1594385Fraction absorbed in human at 625 mg, po2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1437029Antimycobacterial activity against isoniazid/rifampicin/kanamycin/streptomycin-resistant Mycobacterium tuberculosis by microplate Alamar Blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis.
AID383562Antibacterial activity against multidrug-resistant Enterococcus faecalis ATCC 700802 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID560821AUC (0 to 24 hrs) in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1596570Bactericidal activity against Listeria monocytogenes ATCC 19111 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID297126Antibacterial activity against vancomycin-resistant Enterococcus faecalis NCTC-12203 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID565013Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus simulans assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1435934Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRSA10 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID424422Antibacterial activity against vancomycin-resistant Staphylococcus aureus HIP15178 isolated from patients surgical wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID278928Antibacterial activity against Mycoplasma pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID576654Bactericidal activity against 14 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID439891Antibacterial activity against Salmonella Typhimurium ATCC 1639 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID1058366Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 3 weeks by broth dilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Anti-tubercular agents. Part 8: synthesis, antibacterial and antitubercular activity of 5-nitrofuran based 1,2,3-triazoles.
AID1504616Antibacterial activity against Staphylococcus aureus ATCC 6538P by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID284992Antimicrobial activity against Enterococcus casseliflavus at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID542705fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered as 6 divided doses every 4 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID522883Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 509 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1374183Bacteriostatic activity against Staphylococcus aureus ATCC 25923 at 1 times MIC incubated for 24 hrs by time kill curve assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID734685Antibacterial activity against Klebsiella planticola MTCC 530 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID374016Antimicrobial activity against methicillin-resistant Staphylococcus aureus 490 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID326516Cmin in Enterococcus faecalis infected Wistar rat at 600 mg, po four consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID428283Antituberculosis activity against linezolid-resistant Mycobacterium tuberculosis having mutation in 23S rRNA with alteration in domain V2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID1076819Antitubercular activity against extensive drug-resistant Mycobacterium tuberculosis clinical isolate 6 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID710136Antibacterial activity against methicillin-resistant Staphylococcus haemolyticus2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria.
AID131336Dose (administered orally) required to protect the Staphylococcus aureus infected mice was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID206448In vitro antibacterial activity against methicillin susceptible Staphylococcus aureus UC19213 (MSSA); (SA1)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID533662Antimicrobial activity against Staphylococcus aureus RN4220 harboring vgaAv positive plasmid CU12008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID763946Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by NCCLS agar dilution method in presence of human plasma2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID444261Antibacterial activity against methicillin-resistant Staphylococcus aureus 33 by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID533117Antimicrobial activity against Staphylococcus aureus 10*3d1 by Etest method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Serial daptomycin selection generates daptomycin-nonsusceptible Staphylococcus aureus strains with a heterogeneous vancomycin-intermediate phenotype.
AID388042Antibacterial activity against vancomycin-susceptible Enterococcus faecalis CL8516 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID285057Antimicrobial activity against beta hemolytic Streptococcus group C at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1609286Antibacterial activity against methicilline-resistant Staphylococcus aureus NRS123 USA400 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID569343Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID349317Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID303958Inhibition of protein synthesis in Escherichia coli by cell-free transcription-translation assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID285094Antimicrobial activity against viridans group Streptococcus intermedius at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID348860Antibacterial activity against vancomycin-resistant Enterococcus 1 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID372666Antimicrobial activity against Salmonella typhi MTCC 733 after 24 hrs by agar dilution assay2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.
AID560580Bactericidal activity against vancomycin-susceptible Enterococcus faecalis ATCC 29212 assessed as change in bacterial count at 4 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID559284Antimicrobial activity against recombination-deficient Enterococcus faecalis JH2-2 recA harboring nucleotides at position 2576 in rrlA 2576G, rrlB 2576G, rrlC 2576G and rrlD 2576G by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Influence of recombination on development of mutational resistance to linezolid in Enterococcus faecalis JH2-2.
AID1493810Antibacterial activity against Acinetobacter baumannii ATCC 19606 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID558523Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID541061AUC (0 to 24 hrs) in cage fluid of Albino guiena pig at 75 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1304861Dissociation constant, pKa of compound2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1434678Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 3640 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID209293Compound was evaluated for minimum inhibitory concentration against Streptococcus pyogenes 114 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID245153Minimum inhibitory concentration against Enterococcus faecalis UC9217; Range is 2-4 ug/mL2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID562384Antimicrobial activity against Enterococcus faecium clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1151744Antibacterial activity against Staphylococcus aureus measured after 6 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID528713Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus haemolyticus clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID560826Cmax in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID387458AUC (0 to t) in Swiss albino mouse at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID535028Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-51 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1395707Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS384 USA300 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1680049Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 7 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID565081Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus 152 by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
AID1327109Antibacterial activity against Pseudomonas aeruginosa NCIM 2036 at 10 ug/ml measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1680056Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 9 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID567486Antimicrobial activity against vancomycin pretreated vancomycin-intermediate Staphylococcus aureus isolate 1 obtained from wound of patient by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Clinical outcomes by methicillin-resistant Staphylococcus aureus staphylococcal cassette chromosome mec type: isolates recovered from a phase IV clinical trial of linezolid and vancomycin for complicated skin and skin structure infections.
AID559792Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at 0.5 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1539454Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI-based broth microdilution assay
AID262228Antibacterial activity against Enterococcus faecalis ATCC 355502006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID1501360Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID1852679Antibacterial activity against wild type Acinetobacter baumannii assessed as inhibition of bacterial growth
AID348598Antibacterial activity against Streptococcus pneumoniae C402 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID429064Antiplasmodial activity after 72 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum.
AID1770352Antibacterial activity against Vancomycin-resistant Enterococcus faecium ATCC 51559 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID285070Antimicrobial activity against beta hemolytic Streptococci group G at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID549012Antimicrobial activity against Vancomycin-nonsusceptible Enterococcus faecalis assessed as percent resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID1723497Antibacterial activity against Enterococcus faecium NR-32052 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID374007Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID475008Antibacterial activity against Pseudomonas aeruginosa LCB0013 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID562631Antimicrobial activity against Group G Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID544824Antimicrobial activity against Staphylococcus aureus Xen 30 biofilm assessed as log10 CFU/cm'2 in bacterial count2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID558525Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1056358Antibacterial activity against Moraxella catarrhalis SR26840 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1677800Bactericidal activity against Staphylococcus aureus ATCC25923 assessed as reduction in number of colony forming units incubated for 24 hrs followed by re-plating and reincubation on tryptic soy agar plate for 24 hrs2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID535035Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-402 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1446750Antibacterial activity against Staphylococcus aureus RN4220 NRS107 clinical isolate after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1076832Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 6538 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID558502Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID262230Antibacterial activity against Staphylococcus aureus ATCC 91442006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID285023Antimicrobial activity against Listeria monocytogenes at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID323806Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse with peritonitis at 100 mg/kg, po after 3 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID528694Antibacterial activity against methicillin resistant Staphylococcus epidermidis ATCC 35984 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID326526Antibacterial activity against vancomycin-resistant Enterococcus faecalis UCN41 challenged with ID90 bacterial size inoculum in Wistar rat assessed as infection at 600 mg, po four consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID576433Bactericidal activity against 13 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID373988Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID583880Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-2 harboring ribosomal protein L3 Gly155Arg/Met169Leu mutant and cfr-containing p42262 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID1139105Antimicrobial activity against Staphylococcus aureus ATCC 292132014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID511437Antimicrobial activity against flo gene positive Escherichia coli2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID548254Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega after 24 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID1409846Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.1 mg, ip bid for 3.5 days administered 6 hrs post bacterial infection measured 84 hrs post i2018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID574552Decrease in delta toxin levels in Staphylococcus aureus USA300 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID562189Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1677808Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC43300 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID289864Antibacterial activity against Staphylococcus aureus ATCC 499512007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
AID558727Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 50 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID576661Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID542898fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 200 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID730745Antibacterial activity against methicillin-resistant Staphylococcus aureus 1281-07 harboring cfr gene assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID572269Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 49951 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID562247Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 12228 by CLSI broth microdilution assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID1374173Antibacterial activity against Staphylococcus albus AS1.3374 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID645037Antibacterial activity against erythromycin-sensitive Streptococcus pyogenes 9 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID1852693Antibacterial activity against Escherichia coli SQ110 DTC incubated for 24 hrs by twofold serial dilution method
AID533663Antimicrobial activity against Staphylococcus aureus RN10242008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID533960Antimicrobial activity against Staphylococcus epidermidis infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1180572Antimicrobial activity against Staphylococcus aureus ARC1692 by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID545815Antimicrobial activity against 4.6 X 10'6 CFU/peg methicillin-resistant Staphylococcus aureus ATCC 33591 planktonic cells by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID759683Cytotoxicity against porcine PK-15 cells assessed as reduction of cell viability at 5 to 400 ug/ml by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID1400048Antibacterial activity against Enterococcus faecalis ATCC 19433 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1180580Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC2398-2F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1361114Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID205560Minimum inhibitory concentration against Staphylococcus aureus ATCC 259232004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID1770367Bactericidal activity against Vancomycin-resistant Enterococcus faecalis ATCC 51299 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID208626Antibacterial activity was determined against clinically isolated penicillin resistant Streptococcus pneumoniae (PRSP) strains (50 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID374019Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID390323Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 65382008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID1677807Antibacterial activity against Staphylococcus aureus ATCC25923 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1167991Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 22626 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1472752In vivo anti-virulence activity against methicillin-resistant Staphylococcus aureus Mu50 infected in BALB/c mouse model assessed as reduction in bacterial load in heart at 0.4 mg bid for 4.5 days administered intraperitoneally 6 hrs post infection by seri2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID1680047Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 9 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID16465Calculated partition coefficient (clogP)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
3D QSAR studies on new oxazolidinone antibacterial agents by comparative molecular field analysis.
AID424617Antibacterial activity against vancomycin-resistant Staphylococcus aureus AIS2006049 isolated from patients arm wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID1168000Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 27728 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID292607Antimicrobial activity against methicillin-resistant Staphylococcus aureus 562 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID292615Antimicrobial activity against Staphylococcus aureus ATCC 25923 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID559793Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID283624Antimicrobial activity against Enterococcus faecium 34 with homozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID326502Antibacterial activity against vancomycin-susceptible Enterococcus faecalis 1209 after 24 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID1611118Antibacterial activity against Staphylococcus aureus ATCC 29213 CLSI-based double dilution method2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
AID577100T>MIC in Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID285054Antimicrobial activity against beta hemolytic Streptococcus group C at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID576648Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1861538Clearance in Wistar rat at 30 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID528709Antibacterial activity against penicillin resistant Streptococcus pneumoniae clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1151762Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0605 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1446757Bactericidal activity against methicillin-resistant Staphylococcus aureus USA200 NRS383 clinical isolate after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID285107Antimicrobial activity against viridans group Streptococcus mutans at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID745376Inhibition of human CYP2D6 assessed as dextromethorphan O-demethylation after 20 mins by LC/MS/MS analysis2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID326288Antibacterial activity against methicillin-resistant Staphylococcus aureus 293 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID573892fAUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID734688Antibacterial activity against Staphylococcus aureus MTCC 96 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID66901Antibacterial activity against Enterococcus faecalis UC9217 (E. f)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID1852702Selectivity ratio of IC50 for OM pore producing Pseudomonas aeruginosa to IC50 for efflux pump lacking/OM pore producing Pseudomonas aeruginosa
AID1271216AUC (0 to infinity) in BALB/c mouse brain at 10 mg/kg, po by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID555325Antibacterial activity against methicillin-resistant Staphylococcus aureus 145 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1272266Antimicrobial activity against vancomycin-resistant Enterococcus faecalis MMX 202 expressing VanB after 18 to 20 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.
AID609158Antibacterial activity against Bacillus cereus ATCC 11778 at 1 mg/ml after 24 hrs by agar-well diffusion technique2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID576647Bactericidal activity against 48 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1350029Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID566578Antimicrobial activity against Staphylococcus aureus ATCC 6538p by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID575099Antimicrobial activity against Streptococcus pneumoniae serotype 15A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID498883Antimicrobial activity against methicillin-susceptible Staphylococcus aureus OC 4172 assessed as inhibition of growth by broth microdilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1361120Bacteriostatic activity against Acinetobacter baumannii ATCC 19606 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID574072Half life in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1596546Antibacterial activity against methicillin resistant Staphylococcus aureus NRS119 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID206447In vitro antibacterial activity against methicillin susceptible Staphylococcus aureus UC 9213 (MSSA); range is 2-42003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID223270Dose required to cure 50% of Staphylococcus aureus infected mice in the presence of vancomycin when administered orally; value ranges from 2.5-6.42000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID274223Antibacterial activity against Escherichia coli by transcription and translation assay2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID1677806Antibacterial activity against Bacillus pumilus CMCC63202 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID566571Antimicrobial activity against Escherichia coli ATCC 8739 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID576649Bactericidal activity against 1 hr peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID695442Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 1-FQR2M BK2384 expressing GyrA Ser84Leu mutant and GrlA Ser80Phe mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID326521T>MIC in Enterococcus faecalis infected Wistar rat at 600 mg, po four consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID387453Antibacterial activity against vancomycin-resistant Enterococcus faecium DRCC 1542008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID132090Tested for the dose to protect the mice from infection with Staphylococcus aureus OC 4172, by oral administration2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID1873910Antibacterial activity against Enterococcus faecium incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID323812Reduction in bioluminescent methicillin-resistant Staphylococcus aureus Xen1 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, po after 2 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID349315Antibacterial activity against vancomycin-resistant Enterococcus after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID387457Antibacterial activity against Staphylococcus aureus DRCC 035 infected mouse systemic infection model administered orally for 1 day at 1 and 5 hrs post-infection and measured daily for 5 days2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID523835Ratio of vancomycin MIC90 to compound MIC90 for linezolid-susceptible Staphylococcus aureus2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID528841Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID559361Antimicrobial activity against compound-resistant Coxiella burnetii Q212 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1414188Antibacterial activity against Bacillus subtilis ATCC 9372 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1414192Antibacterial activity against clinical isolate of penicillin-resistant Staphylococcus aureus after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID285356Decrease in Panton-Valentine leukocidin level in community acquired methicillin-resistant Staphylococcus aureus HT20040332 in CYY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID522921Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 950 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID390340Antimicrobial activity against Serratia marcescens 16352008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID293552Antibacterial activity against Staphylococcus epidermidis MTCC 2639 after 24 hrs by agar dilution assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Organoiodine(III) mediated synthesis of 3,9-diaryl- and 3,9-difuryl-bis-1,2,4-triazolo[4,3-a][4,3-c]pyrimidines as antibacterial agents.
AID390327Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus 17252008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID542677fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID390329Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae 9752008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID285372Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID352923Antibacterial activity against Enterococcus faecalis C474 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID1446752Antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID206595In vitro antibacterial activity against Staphylococcus aureus 6538p (S.a.1)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID373806Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 Hershey after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID729223Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID285087Antimicrobial activity against viridans group Streptococcus constellatus at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1649281Antibacterial activity against methicillin-resistant Staphylococcus aureus SR3637 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID535030Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-73 expressing SCCmec type 4d element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1699553Induction of cell membrane permeabilization in methicillin resistant Staphylococcus aureus ATCC 700699 measured at 5 mins interval for 2 hrs by propidium iodide staining based fluorescence assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial
AID1647981Antibacterial activity against Klebsiella pneumoniae by resazurin dye based microdilution method2020Journal of natural products, 02-28, Volume: 83, Issue:2
The Isolation of Pyrroloformamide Congeners and Characterization of Their Biosynthetic Gene Cluster.
AID1271209Metabolic stability in human plasma by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID590150Antibacterial activity against methicillin-resistant Staphylococcus aureus Smith infected iv dosed ICR mouse assessed as protection against mouse mortality administered 1 hr after infection measured up to 7 days2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1647979Antibacterial activity against Methicillin resistant Staphylococcus aureus by resazurin dye based microdilution method2020Journal of natural products, 02-28, Volume: 83, Issue:2
The Isolation of Pyrroloformamide Congeners and Characterization of Their Biosynthetic Gene Cluster.
AID542905Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial regrowth at 400 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1898396Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-1707 assessed as bacterial growth inhibition incubated for 16 hrs by broth microdilution susceptibility test2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
A Modular Synthetic Route Involving
AID559801Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at 2 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID562633Antimicrobial activity against Streptococcus pneumoniae assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID753125Antibacterial activity against 16-membered ring macrolide- lincosamide-streptogramin B-resistant Staphylococcus MTCC 2940 assessed as growth inhibition after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID285019Antimicrobial activity against Listeria monocytogenes at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285134Antimicrobial activity against viridans group Streptococcus sanguinis at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID520024Antimicrobial activity against Enterococcus faecalis A59622008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1594374Antibacterial activity against Pseudomonas aeruginosa ATCC 15442 after 18 to 24 hrs in presence of colistin by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID609060Antibacterial activity against Pseudomonas aeruginosa ATCC 25668 at 1 mg/ml after 24 hrs by agar-well diffusion technique2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID1414191Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID560368Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis ATCC 29212 by broth dilution method in presence of 4% HSA2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID245105In vitro minimum inhibitory concentration of compound against Staphylococcus aureus ATCC 49951 (Smith)2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID573151Antibacterial activity against vancomycin-susceptible Enterococcus faecalis assessed as resistant isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1409849Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.4 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 42018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID1553381Inhibition of CYP2C9 (unknown origin)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID565485Bactericidal activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by M26-A method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID541073Tmax in cage fluid of Albino guiena pig at 50 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1596552Antibacterial activity against vancomycin resistant Staphylococcus aureus VRS12 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID428281Antituberculosis activity against linezolid-resistant Mycobacterium tuberculosis without mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
AID581664Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level per mg of protein after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID522919Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 1469 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID582993Antimicrobial activity against Enterococcus faecium BM-0661 transconjugant by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID756091Antibacterial activity against penicillin-resistant Streptococcus pneumoniae assessed as growth inhibition after 16 hrs by agar dilution method2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
AID326514Cmin in Enterococcus faecalis infected Wistar rat at single administration of 600 mg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID581658Cmax in human plasma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID40326Minimum inhibitory concentration against Bacillus cereus MTCC 4302004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID1474260Ratio of MBC50 to MIC50 for Enterococcus faecium clinical isolates2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID477376Antibacterial activity against Streptococcus pyogenes after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID1432971Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 48 hrs by MTT assay
AID1594369Antibacterial activity against Klebsiella pneumoniae ATCC BAA-1705 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID498901fCmax in immunocompetent SKH1 mouse plasma at 50 mg/kg, po2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID429429Antibacterial activity against Haemophilus influenzae isolate 285 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID1888846Antibacterial activity against Staphylococcus aureus 1199B measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID562590Antimicrobial activity against vancomycin-susceptible Enterococcus faecium clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID583706Antibacterial activity against clinical-derived Staphylococcus aureus isolate harboring ribosomal protein L3 deltaSer145/His146Tyr mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID573874Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected in iv dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID585170Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA U2504G mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID10752Clearance (Cl) of compound (10 mg/kg) after iv administration was determined in Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID558720Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1168008Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 15/213 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1493802Antibacterial activity against Staphylococcus aureus NRS119 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID565005Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID572271Antimicrobial activity against methicillin-resistant Staphylococcus aureus NB01021 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID1167734Antimicrobial activity against methicillin-resistant and quinolone-resistant Staphylococcus aureus by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID1434677Anti-bacterial activity against methicillin-susceptible Staphylococcus aureus CCARM 0205 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID311485Antimicrobial activity against Escherichia coli ATCC 25922 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID559550Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP4 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID687495AUC (0 to infinity) in rat at 10 mg/kg, iv2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID1076829Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID410225Antibacterial activity against Moraxella catarrhalis by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID581667Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID424768Antibacterial activity against penicillin-sensitive Streptococcus pneumoniae CL8002 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID68247In vitro antibacterial activity against vancomycin and ciprofloxacin resistant Enterococcus faecium (Efm CIP) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID753116Antibacterial activity against Staphylococcus aureus MTCC 96 assessed as growth inhibition at 20 mg/mL after 24 hrs2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID1904918Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS 385 (USA500) incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID283167Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5254 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID285109Antimicrobial activity against viridans group Streptococcus mutans at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID569341Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 12228 by broth micro dilution technique2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID576396Tmax in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1493812Antibacterial activity against Klebsiella pneumoniae BAA-1706 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1421235Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID560577Bactericidal activity against vancomycin-resistant Enterococcus faecalis 1058946 expressing vanA gene assessed as change in bacterial count at 16 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1271219AUC (0 to infinity) in BALB/c mouse plasma at 10 mg/kg, po by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1474262Ratio of MBC50 to MIC50 for vancomycin-resistant Enterococcus faecalis clinical isolates2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID734689Antibacterial activity against Staphylococcus MLS-16 MTCC 2940 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID1400026Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID572270Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID1400024Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv harboring pFCA-luxAB preincubated for 10 days under anaerobic condition followed by incubation under ambient gaseous condition for 28 hrs by LORA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID560506Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b3k2345 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID519077Antimicrobial activity against wild type Staphylococcus aureus 8325-4 by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID1778659Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 43300 measured after 24 hrs by CLSI protocol based method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID208625Antibacterial activity against Streptococcus pneumoniae (PEN-R)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID533988Bacteriostatic activity against linezolid-resistant Staphylococcus aureus SA040L infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID528699Antibacterial activity against vancomycin resistant Enterococcus faecalis VanB clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1861527Cmax in Beagle dog at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID244920Minimal inhibitory concentration against Salmonella typhi (MDR) ICH 0982004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID559786Antimicrobial activity against heterogeneous vancomycin-susceptible Staphylococcus aureus assessed as resistant isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID370016Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 12.5 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID542901fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID726194Antibacterial activity against Streptococcus pyogenes 308A by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID576404Terminal half-life in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID383741Half life in Sprague-Dawley rat at 10 mg/kg, iv2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID285102Antimicrobial activity against viridans group Streptococcus mitis at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID285026Antimicrobial activity against Micrococcus luteus at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID319981Antimicrobial activity against Staphylococcus aureus ATCC 292132008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID1609301Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS384 USA300 after 18 to 20 hrs by broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID245330Antibacterial activity against Penicillin-resistant Streptococcus pneumoniae (PRSP) J-24 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID323831Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po after 4 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID1852662Antibacterial activity against multidrug resistant Klebsiella pneumoniae ATCC43816 assessed as inhibition of bacterial growth incubated for 24 hrs in M9-MOPS medium by twofold serial dilution method
AID1430400Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 24 to 48 hrs by macro-broth dilution method2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Methylsulfonyl benzothiazoles (MSBT) derivatives: Search for new potential antimicrobial and anticancer agents.
AID1504617Antibacterial activity against Staphylococcus aureus ATCC 33591 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID308926Antibacterial activity against Staphylococcus epidermidis ATCC 155 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID552834Antibacterial activity against multidrug-resistant Enterococcus faecalis2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID1435928Bactericidal activity against mupirocin/rifampicin-resistant Staphylococcus aureus RN4220 NRS107 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID308485Inhibition of transcription and translation activity in Escherichia coli by luciferase reporter assay2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
AID499117Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected immunocompromized SKH1 mouse assessed as lesion volume at 100 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1535 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID523821Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID576667Bactericidal activity against 1 hr peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID246829Efficacy against mice infected with MRSA-33 upon s.c. administration2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1861533Terminal half life in Beagle dog at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID373655Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 Hershey by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1770339Antibacterial activity against penicillin-susceptible Bacillus subtilis ATCC 9372 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID541062AUC (0 to 24 hrs) in cage fluid of Albino guiena pig at 50 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID608939Antibacterial activity against Pseudomonas aeruginosa ATCC 25668 after 24 hrs by broth microdilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID1578411Antimicrobial activity against methicillin-sensitive Staphylococcus aureus NRS 107 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID245964Cytotoxic concentration against Huh7 cells at 48 hours in MTT assay; NT = not tested2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID285076Antimicrobial activity against viridans group Streptococcus anginosus at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID207213In vitro minimum inhibitory concentration against coagulase negative Staphylococcus aureus methicillin resistant (CNSMR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID581659Fraction unbound in human plasma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1539455Antibacterial activity against Listeria monocytogenes ATCC 19111 after 18 to 20 hrs in aerobic condition by CLSI-based broth microdilution assay
AID374000Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey after 50 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID285025Antimicrobial activity against Micrococcus luteus at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID575077Antimicrobial activity against Streptococcus pneumoniae serotype 3 assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID209934Inhibitory activity against Streptococcus pyogenes1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID263967Antibacterial activity against beta lactamase negative Haemophilus influenzae DRCC 4332006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID1873901Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 50% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1853461Bactericidal activity against vancomycin-resistant Enterococcus faecalis ATCC 51575 assessed as reduction in colony forming unit incubated for 20 hrs2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID577137Total clearance in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1167729Fraction unbound in human plasma at 10 uM after 16 hrs by LC-MS/MS analysis2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID206786Inhibitory activity against MRSA1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID125126In vivo antibacterial activity against Staphylococcus aureus after intramuscular administration (10 mg/kg) in mice using (MTT) mouse thigh test2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
AID1395703Bactericidal activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID524719Antibacterial activity against linezolid-resistant Staphylococcus aureus 01A1221 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID630559Antibacterial activity against linezolid-resistant Staphylococcus aureus after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID1056359Antibacterial activity against Enterococcus faecium SR7940 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1677799Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC43300 assessed as reduction in number of colony forming units incubated for 24 hrs followed by re-plating and reincubation on tryptic soy agar plate for 24 hrs2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID585168Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA G2032A mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID1687313Synergistic antibacterial activity against Klebsiella pneumoniae ATCC 1706 in presence of 0.25 times MIC of colistin incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID244870Minimum inhibitory concentration against Pseudomonas aeruginosa ATCC 254162004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID205899Minimum inhibitory concentration measured against Staphylococcus epidermidis2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID1205588Antibacterial activity against Haemophilus influenzae acrB by broth microdilution method2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1649282Antibacterial activity against Vancomycin-resistant Staphylococcus aureus HIP11714 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID558475Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID352922Antibacterial activity against Coagulase negative Staphylococcus after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID206056Inhibitory activity against methicillin-sensitive Staphylococcus epidermidis (MSSE)1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1680011Antibiofilm activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of biofilm formation incubated for 24 hrs by crystal violet staining assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1395705Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS119 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1421222Antibacterial activity against methicillin-sensitive Staphylococcus aureus by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID559771Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 4sy39 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID285317Antimicrobial activity against Rhodococcus spp. by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Daptomycin susceptibility of unusual gram-positive bacteria: comparison of results obtained by the Etest and the broth microdilution method.
AID519080Antimicrobial activity wild type Escherichia coli SQ110 by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID523820Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID245010In vitro minimum inhibitory concentration against Salmonella abony (NCTC 6017)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID319163Total clearance in human2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID559368Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP2 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID562235Antibacterial activity against methicillin-resistant Staphylococcus aureus OC2878 assessed as inhibition of bacterial regrowth at 16 times MIC after 8 hrs by dynamic time kill study2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID533974Antimicrobial activity against linezolid-susceptible Staphylococcus aureus ATCC 25923 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1243933Antimicrobial activity against vancomycin-resistant Staphylococcus aureus VRS2 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID763985Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1056344Tmax in ICR mouse at 67.7 mg/kg, po by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID284980Antimicrobial activity against Enterococcus avium at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID50998In vitro antibacterial activity against Clostridium perfringens strain ATCC 131241996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID245331Antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) 870307 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID522908Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 2003 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID285550Tmax in mouse at 50 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID319164Renal clearance in human2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID534249Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP-1 cells at pH 5.5 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID560369Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 51559 by broth dilution method in presence of 4% HAS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID28208Tmax value in Male Sprague-Dawley Rat at dose 10 (mg/kg iv) [tmax (h)]; ND denotes not reported2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID576413Total clearance in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID574073Half life in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID576403Terminal half-life in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID577114ABBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID751392Inhibition of MAO-A (unknown origin) by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Recent development of potent analogues of oxazolidinone antibacterial agents.
AID1117391Antimicrobial activity against Pseudomonas aeruginosa K799/61 assessed as partially clear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1327107Antibacterial activity against Escherichia coli NCIM 2688 at 3 ug/ml measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1519037Antibacterial activity against methicillin-sensitive Staphylococcus aureus assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID535037Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-404 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID581039Induction of bacterial membrane damage in Staphylococcus epidermidis ATCC 23760 at 4 ug/mL by BacLight assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID244977Antibacterial activity against Klebsiella pneumoniae type II was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID541046Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 75 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1193402Antimicrobial activity against Francisella tularensis BEI/ATCC UTAH 112 measured after overnight incubation2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID449615Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID576646Bactericidal activity against 24 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID561726Antibacterial activity against Enterococcus faecalis assessed as resistant isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1374176Antibacterial activity against Enterococcus faecalis ATCC 35667 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID326292Antibacterial activity against methicillin-resistant Staphylococcus aureus 4930 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID326506Cmax in Enterococcus faecalis infected Wistar rat at 600 mg, po four consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID1194833Antibacterial activity against methicillin-resistant Staphylococcus aureus incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID1539444Antibacterial activity against Methicillin-sensitive Staphylococcus aureus NRS107 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID373666Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 after 22 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID392204Antibacterial activity against Streptococcus pyogenes C-203 by micro broth method2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents.
AID396030Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pAP2 plasmid containing Enterobacter cloacae acrA gene by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID245413Minimum inhibitory concentration against ampicillin-reisitant Haemophilus influenzae UC30063; Range is 8-16 ug/mL2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID1151772Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 10 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID533019Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-2 assessed as inhibition of bacterial growth in Mueller-Hinton broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1514453Antitubercular activity against moxifloxacin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID566583Antimicrobial activity against Staphylococcus xylosus ATCC 2997 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID285049Antimicrobial activity against Enterococcus raffinosus by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID370032Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected in iv dosed DBA/2 mouse localized infection model assessed as reduction of number of CFU per gram of thigh administered 2 hrs postinfection thrice daily for 1 day and 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID295154Antibacterial activity against methicillin-susceptible Staphylococcus aureus by microdilution broth method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID1197116Antibacterial activity against mecA-positive, methicillin/oxacillin/tetracycline-resistant and vancomycin/linezolid susceptible Staphylococcus aureus COL after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1407929Antibacterial activity against Enterobacter cloacae ARC3528 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID523822Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 4 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID383563Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID542882fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered as 4 divided doses every 6 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID523799Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID756094Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as growth inhibition after 16 hrs by agar dilution method2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
AID1312947Bactericidal activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID576874Bactericidal activity against 1 hr peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID207645Antibacterial activity against Staphylococcus aureus UC126731998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID530127Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID1421221Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth liquid microdilution method2018European journal of medicinal chemistry, Oct-05, Volume: 158Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents.
AID319169Plasma concentration in human at 600 mg, po bid2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1126492Antimicrobial activity against LS2 Efflux knock-out Haemophilus influenzae2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID533930Antimicrobial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus NRS119 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID24539terminal disposition half-life was evaluated in male Dawley rats at a dose of 10 mg/kg when taken intravenously1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID285088Antimicrobial activity against viridans group Streptococcus constellatus at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1493804Antibacterial activity against Staphylococcus aureus USA300 NRS384 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1271220Ratio of Cmax in brain to plasma in BALB/c mouse at 10 mg/kg, po2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID542885fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered as 4 divided doses every 6 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1303402Antibacterial activity against methicillin-resistant Staphylococcus aureus after 24 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID745403Antibacterial activity against Enterococcus faecium SR7940 clinical isolate assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID542922Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as bacterial killing at 500 mg administered once every 24 hrs for 15 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID511429Antimicrobial activity against Clostridium perfringens LFM1 assessed as susceptibility breakpoint by DIN-standardized microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID1243926Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA100 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID285097Antimicrobial activity against viridans group Streptococcus intermedius at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID292669Antibacterial activity against Staphylococcus aureus by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
A distal methyl substituent attenuates mitochondrial protein synthesis inhibition in oxazolidinone antibacterials.
AID373993Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID528969Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID499143Ratio of fAUC to MIC in Staphylococcus aureus OC 8525 infected sc dosed SKH1 mouse2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID498884Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 assessed as inhibition of growth by broth microdilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID285009Antimicrobial activity against Enterococcus hirae at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID340860Antimicrobial activity against vancomycin-intermediate resistant Staphylococcus aureus Mu50 vraG mutant microdilution assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus.
AID270151Antibacterial activity against gram positive Staphylococcus aureus Smith OC 4172 in presence of 50% mouse serum2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.
AID519987Antimicrobial activity against methicillin-susceptible Staphylococcus aureus nosocomial isolate2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1609275Bactericidal activity against methicilline-resistant Staphylococcus aureus NRS384 USA300 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID311483Antimicrobial activity against Haemophilus influenzae ATCC 49247 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID532800Antibacterial activity against vancomycin-susceptible Staphylococcus aureus PC after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID582989Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0847 harboring MLST sequence type ST78 and pulsotype E expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID424424Antibacterial activity against vancomycin-resistant Staphylococcus aureus AIS2006032 isolated from patients foot wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID573861Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 after 16 to 20 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1352009Antibacterial activity against wild type Staphylococcus aureus Newman infected in BALB/c mouse assessed as decrease in bacterial load in mouse liver at 0.4 mg, ip bid administered 4.5 days measured after 90 hrs relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.
AID1680043Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 3 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID523814Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at =< 0.25 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1252239Antimicrobial activity against Acinetobacter baumannii ATCC 196062015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
Rapid synthesis and antimicrobial activity of novel 4-oxazolidinone heterocycles.
AID370015Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 25 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1553382Inhibition of CYP2C19 (unknown origin)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID567455Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK7 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID374013Antimicrobial activity against methicillin-resistant vancomycin-intermediate Staphylococcus aureus 555 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1692401Antibacterial activity against methicillin resistant and vancomycin intermediate resistant Staphylococcus aureus MU50 assessed as reduction in bacterial growth incubated for 18 to 24 hrs by broth microdilution method2020European journal of medicinal chemistry, Aug-15, Volume: 200Pharmacomodulations of the benzoyl-thiosemicarbazide scaffold reveal antimicrobial agents targeting d-alanyl-d-alanine ligase in bacterio.
AID1271222Ratio of AUC (0 to infinity) in brain to plasma in BALB/c mouse at 10 mg/kg, po2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID575084Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 6B assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1904914Antibacterial activity against methicillin-sensitive Staphylococcus aureus NRS 107 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID285353Decrease in Panton-Valentine leukocidin level in community acquired methicillin-resistant Staphylococcus aureus HT20010734 in CYY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID308918Antibacterial activity against Staphylococcus aureus ATCC 33592 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID285042Antimicrobial activity against Corynebacterium pseudodiphtheriticum by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID542910Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing at 200 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1414211Toxicity in mouse infected with methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as mouse death at 30 mg/kg, ip administered 0.1, 6 hrs postinfection and measured after 1 week2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID630562Antibacterial activity against linezolid-resistant Enterococcus faecium after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID637977Antibacterial activity against Staphylococcus aureus ATCC 25923 after overnight incubation by twofold broth dilution technique in presence of 50% human serum2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID373832Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 after 23 passages with quinupristin-dalfopristin measured after 10 antibiotic-free subculture by multi-step resistance s2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID370040Bioavailability in Staphylococcus aureus-infected mouse localized thigh infection model at 25 mg/kg2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1472759In vivo anti-virulence activity against methicillin-resistant Staphylococcus aureus LRSA202 infected in BALB/c mouse model assessed as reduction in bacterial load in kidney at 0.4 mg bid for 3.5 days administered intraperitoneally 6 hrs post infection by 2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID525143Antimicrobial activity against linezolid-resistant Staphylococcus aureus isolate 004-737X expressing cfr and ermA gene isolated from paraplegic patient by broth microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID565230Antimicrobial activity against Mycobacterium chelonae 9917 by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID559362Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii Q212 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID583879Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-1 harboring ribosomal protein L3 Gly155Arg mutant and cfr-containing p42262 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID1770386Inhibition of Bacillus subtilis FtsZ assessed as promotion of FtsZ polymerization at 10 ug/ml measured after 10 hrs by fluorescence spectrometer based light scattering assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID363430Antibacterial activity against Staphylococcus aureus ATCC 29213 in absence of human serum2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
AID1778643Antibacterial activity against penicillin-susceptible Bacillus subtilis ATCC 9372 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID424425Antibacterial activity against Enterococcus faecalis AIS2007003 isolated from patients rectum by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID522891Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1008 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1056351Antibacterial activity against methicillin-resistant Staphylococcus aureus SR3637 clinical isolate infected in iv dosed JCL/ICR systemic infection model assessed as mortality administered after 1 hr of infection measured for 7 days2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID368283Half life in rabbit plasma at 58 mg/kg infused every 12 hrs for 4 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID373834Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 504 after 14 passages with CG400549 measured after 10 times antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID763984Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1269334Apparent permeability from basolateral to apical side in human Caco2 cells2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
AID311480Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae ATCC 51915 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID349310Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolate after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID475009Antibacterial activity against Klebsiella pneumoniae LCB0014 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID573144Antibacterial activity against penicillin-susceptible Streptococcus viridans assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID566570Antimicrobial activity against Corynebacterium glutamicum ATCC 13032 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID1243932Antimicrobial activity against vancomycin-intermediate-resistant Staphylococcus aureus NRS1 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID410116Antimicrobial activity against Haemophilus influenzae A1950 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID1197118Antibacterial activity against mecA-positive, ciprofloxacin/gentamicin/oxacillin/penicillin/linezolid-resistant Staphylococcus aureus NRS120 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID558717Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1161141Antimicrobial activity against Escherichia coli isolate 1 after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID560803AUC (0 to 24 hrs) in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID542682fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 300 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID560801Apparent volume of distribution with respect to the bioavailability in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID66113In vitro antibacterial activity against Enterococcus faecalis NCTC 12201 (E. f. 153) vancomycin resistant2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID67894The compound was evaluated for its anti-bacterial activity against Enterococcus faecalis UC 92171998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID1167730Solubility of the compound2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID560831Ratio of AUC (0 to 24 hrs) in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days to MIC for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1151739Antibacterial activity against Staphylococcus aureus measured after 1 serial passage2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1269336Plasma protein binding in human2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
AID244822Minimal inhibitory concentration against Bacillus cereus2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID520026Antimicrobial activity against Enterococcus faecium A59592008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1680042Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 4 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID308915Antibacterial activity against Enterococcus faecalis ATCC 14506 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID79584Inhibitory activity against Haemophilus influenzae UC300632000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID564133Antimicrobial activity against methicillin-resistant Staphylococcus aureus HUSA 304 infected in Wistar rat assessed as decrease in bacterial load in tissue cage fluid at 50 mg/kg, ip administered every 12 hrs for 7 days measured on day 11 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID1168017Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 8/224 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID583705Antibacterial activity against clinical-derived Staphylococcus aureus isolate 42262 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID483191Antibacterial activity against Staphylococcus aureus ATCC 25923 by microbroth dilution technique2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID1194835Antibacterial activity against methicillin-resistant Staphylococcus epidermidis incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID1414193Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID1723532Antibacterial activity against Enterococcus faecium NR-31972 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID205738In vitro antibacterial activity against methicillin resistant Staphylococcus epidermidis UC 12084; range is 1-22003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID244961Minimal inhibitory concentration against Pseudomonas aeruginosa ATCC 278532004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID1710580Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS386 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID575169Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose at 1000 uM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID67384In vitro antibacterial activity against vancomycin resistant Enterococcus faecalis UC 9217 (VREA); range is 1-22003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID695445Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 4-FQR3M BSA643 expressing GyrA Ser84Leu mutant and GrlA Ser80Tyr and Glu84Gly mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1400039Bactericidal activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1437030Antimycobacterial activity against isoniazid/rifampicin/kanamycin/capreomycin-resistant Mycobacterium tuberculosis by microplate Alamar Blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis.
AID1520443Antibacterial activity against methicillin-sensitive Staphylococcus aureus after 18 to 20 hrs by CLSI-protocol based broth microdilution method
AID1723491Antibacterial activity against Enterococcus faecium HM968 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID522890Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 770 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID541068Half life in cage fluid of Albino guiena pig at 50 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID523813Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 4 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID573878Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus Smith ATCC 13709 infected in SKH1 mouse upto 320 mg/kg/day, po administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID583895Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 453 (NRS23) by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID373657Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID560377Selectivity ratio of MIC for Enterococcus faecalis 1058946 in presence of 4% HSA to MIC for Enterococcus faecalis 10589462009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1852687Antibacterial activity against efflux pump lacking/recombinant OM pore producing Pseudomonas aeruginosa assessed as inhibition of bacterial growth
AID608938Antibacterial activity against Escherichia coli ATCC 8739 after 24 hrs by broth microdilution method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID171360Dawley rats at a dose of 10 mg/kg when taken intravenously1998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID304005Effect on hematology in Sprague-Dawley rat assessed as decrease in hemoglobin at 200 mg/kg/day, po after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID444260Antibacterial activity against methicillin-resistant Staphylococcus aureus 562 by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID576666Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID283625Antimicrobial activity against Enterococcus faecium Ho 4136-00422007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID206591In vitro antibacterial activity against Staphylococcus aureus 77 (S.a.2)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID522913Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1806 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1539446Antibacterial activity against Methicillin-resistant Staphylococcus aureus NRS123-USA400 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID274224Antibacterial activity against Staphylococcus aureus UC-76 SA-12006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID520511Cmax in New Zealand rabbit osteomyelitis model at 40 mg/kg, sc administered every 6 hrs for 4 days2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID533944Antimicrobial activity against linezolid-resistant Enterococcus faecalis 1172 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID576675Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID528837Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1367593Antibacterial activity against gram-negative Escherichia coli MG1655 membrane permeabilized mutant in presence of polymyxinnonapeptide by CLSI broth microdilution method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID576673Bactericidal activity against 24 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID85979In vitro antibacterial activity against ampicillin resistant Haemophilus influenzae 30063 (B-lactamase +)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID555509Antibacterial activity against methicillin-resistant, vancomycin-intermediate coagulase-negative Staphylococcus epidermidis 225 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID559562Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP8 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID206227In vitro antibacterial activity against Staphylococcus epidermis C22352003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID283176Increase in biofilm formation of Staphylococcus aureus SA113 at 0.25 times MIC2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID571926Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-N623S-Q624S mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID1407927Antibacterial activity against Klebsiella pneumoniae ARC1865 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID558709Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID319984Antimicrobial activity against vancomycin-sensitive Enterococcus faecalis ATCC 292122008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID533115Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315DeltaIP by Etest method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Serial daptomycin selection generates daptomycin-nonsusceptible Staphylococcus aureus strains with a heterogeneous vancomycin-intermediate phenotype.
AID567567Antimicrobial activity against Bacillus sp. BS-01 expressing multiple resistance gene cfr and phenolic resistance gene fexA obtained from swine feces2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
First report of the multidrug resistance gene cfr and the phenicol resistance gene fexA in a Bacillus strain from swine feces.
AID576899Ratio of AUC (0 to 24 hrs) to MIC for Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1660514Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 16 hrs by CLSI-based broth microdilution method2020Journal of natural products, 06-26, Volume: 83, Issue:6
Synthesis of the Cyanobacterial Antibiotics Anaephenes A and B.
AID268863Antibacterial activity against Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis of novel tricyclic oxazolidinones by a tandem SN2 and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid.
AID532814Antibacterial activity against vancomycin-intermediate Staphylococcus aureus NJ phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID533024Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-4 assessed as inhibition of bacterial growth in brain heart infusion broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID285377Bactericidal activity against vancomycin-intermediate Staphylococcus aureus Mu50 assessed as reduction of CFU using in vitro PK/PD model with human dosage regimen 600 mg every 12 hrs after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID560362Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis ATCC 29212 by broth dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID569345Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID548472Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega after 48 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID370042Antibacterial activity against linezolid-resistant methicillin-resistant Staphylococcus aureus infected in C3H mouse localized infection model assessed as log reduction in CFU per gram of thigh at 100 mg/kg measured after 48 hrs by organ burden assay rela2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID410208Antibacterial activity against Enterococcus faecium by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID753114Antibacterial activity against 16-membered ring macrolide- lincosamide-streptogramin B-resistant Staphylococcus MTCC 2940 assessed as growth inhibition at 20 mg/mL after 24 hrs2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID285547Plasma half life in mouse at 20 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID617586Antibacterial activity against Staphylococcus aureus ATCC 25923 by CLSI method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents. Part II.
AID1721056Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in Balb/c mouse assessed as lung bacterial burden by measuring colony forming unit at 100 mg/kg/day, po administered via gavage 5 times per week for 3 weeks starting from 10 days po2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID319987Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 12202 infected in po dosed mouse2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID392202Antibacterial activity against Streptococcus pneumoniae SV1 SP-3 by micro broth method2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents.
AID245295In vitro minimum inhibitory concentration of compound against Methicillin-resistant Staphylococcus aureus ATCC 292132005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID297960Antibacterial activity against Streptococcus pneumoniae 548 infected mouse lung infection model assessed as reduction in bacterial count at 80 mg/kg/day, po relative to control2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.
AID284970Antimicrobial activity against Corynebacterium jeikeium at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID511432Antimicrobial activity against Clostridium perfringens LFM1 assessed as resistance breakpoint by DIN-standardized microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID541092Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by macrodilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID278918Antibacterial activity against linezolid-resistant Enterococcus faecium2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1723498Antibacterial activity against Enterococcus faecium NR-31971 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID285005Antimicrobial activity against Enterococcus gallinarum at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID519095Antimicrobial activity against Staphylococcus aureus NRS121 clinical isolate harboring G2576U mutation in 23S rRNA by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID564826Antimicrobial activity against methicillin-resistant Staphylococcus aureus assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID1501363Bactericidal activity against Staphylococcus aureus RN4220 NRS107 incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID573153Antibacterial activity against vancomycin-resistant Enterococcus faecalis assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID523837Antimicrobial activity against methicillin-resistant Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1689206Antibacterial activity against Escherichia coli JW55031 harboring tolC mutation assessed as reduction in bacterial growth by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID278875Increase in lactate production in primary human osteoblasts at 6 ug/ml by ELISA2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID1596559Antibacterial activity against Methicillin resistant Streptococcus pneumoniae ATCC 700677 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID1710598Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as reduction in bacterial growth incubated for 18 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID734706Antibacterial activity against Staphylococcus aureus MTCC 96 after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID1680005Induction of cytoplasmic membrane depolarization in Staphylococcus aureus ATCC 29213 at 20 ug/ml measured for 12 mins by DiSC35 dye-based fluorescence assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1770361Ratio of MBC to MIC against erythromycin-susceptible Staphylococcus aureus ATCC 259232021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID1852664Antibacterial activity against multidrug resistant Klebsiella aerogenes ATCC13048 assessed as inhibition of bacterial growth incubated for 24 hrs in M9-MOPS medium by twofold serial dilution method
AID134120Protective dose of subcutaneously administered compound against intraperitoneally-induced septicaemia model (Staphylococcus aureus GO3) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID206452In vitro antibacterial activity against oxazolidinone Linezolid resistant Staphylococcus aureus (Sau3LZD) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID326279Antibacterial activity against methicillin-resistant Staphylococcus aureus at 4 hrs daily exposure for 5 day2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID287257Antimicrobial activity against Staphylococcus aureus ATCC 25922 by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID1390465Antibacterial activity against methicillin-resistant Staphylococcus aureus 12019842018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1677809Antibacterial activity against Bacillus subtilis ATCC9372 incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID560521Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate xa07029 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID572283Antimicrobial activity against methicillin susceptible Staphylococcus aureus ATCC 49951 infected in sc dosed NMRI mouse treated 1 and 5 hrs post infection2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID206817In vitro antibacterial activity against Staphylococcus pyogenes C60032003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1877889Antibacterial activity against Enterococcus faecalis DSM-20478 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID532791Antibacterial activity against vancomycin-intermediate Staphylococcus aureus LIM2 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID133992Protective dose of orally administered compound against intraperitoneally-induced septicaemia model ( vancomycin resistant Enterococci faecium D3HM4 strain) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID1680067Antibacterial activity against Escherichia coli ATCC 25922 assessed as reduction in bacterial growth incubated 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID555302Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID263960Antibacterial activity against methicillin-susceptible Staphylococcus aureus DRCC 0352006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID285112Antimicrobial activity against viridans group Streptococcus oralis at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID383746Bioavailability in Sprague-Dawley rat at 10 mg/kg, iv2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID499162Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 6.2 mg/kg/day, po (Rvb = 1.6 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID304008Increase in bone marrow myeloid/erythroid ratio in Sprague-Dawley rat at 200 mg/kg/day, po after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID1151706Inhibition of human recombinant MAO-A expressed in yeast after 1 hr by luciferin-based luminescence assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1430399Antibacterial activity against methicillin-resistant Staphylococcus aureus 3710 after 24 to 48 hrs by macro-broth dilution method2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Methylsulfonyl benzothiazoles (MSBT) derivatives: Search for new potential antimicrobial and anticancer agents.
AID1887586Synergistic antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 24 hrs in presence of artocarpin by checkerboard method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID582990Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS08257 harboring MLST sequence type ST341 and pulsotype F expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID528704Antibacterial activity against Streptococcus intermedius clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID318368Inhibition of fatty acid synthesis in Staphylococcus aureus in whole cell activity assay2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID409581Antimicrobial activity against sStreptococcus pneumoniae after 16 to 18 hrs by agar dilution method2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID576668Bactericidal activity against 2 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID583887Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus isolate 145 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID370018Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 3.12 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID560519Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate zj07028 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID520226Antimicrobial activity against Streptococcus pneumoniae PU1071099 harboring 65WR66 deletion in ribosomal protein L4 by broth microdilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1252238Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 335912015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
Rapid synthesis and antimicrobial activity of novel 4-oxazolidinone heterocycles.
AID1519265Antibacterial activity agianst vancomycin-resistant Enterococcus faecium clinical isolates2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID523807Antimicrobial activity against oxacillin-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID558472Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID560800Elimination half life in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1904920Antibacterial activity against Vancomycin-resistant Staphylococcus aureus 9 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID528977Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1653081Antibacterial activity against Bacillus pumilus2019European journal of medicinal chemistry, Feb-15, Volume: 164Isatin derivatives and their anti-bacterial activities.
AID1692905Antibacterial activity against hospital acquired methicillin-sensitive Staphylococcus aureus clinical isolates2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID1151778Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 0605 in mouse thigh infection model assessed as reduction of log10 CFU per thigh at 20 mg/kg, po2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID524724Antibacterial activity against linezolid-resistant Enterococcus faecium 03B1074 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID561729Antibacterial activity against Enterococcus faecalis assessed as susceptible isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID283169Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5258 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1680066Antibacterial activity against Salmonella enterica ATCC 8387 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1415067Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 3 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID763951Antibacterial activity against Moraxella catarrhalis clinical isolate 138 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID391589Antibacterial activity against methicillin-sensitive Staphylococcus aureus Smith by agar dilution method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials.
AID1161137Antimicrobial activity against Staphylococcus aureus after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID285074Antimicrobial activity against viridans group Streptococcus anginosus at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285126Antimicrobial activity against viridans group Streptococcus salivarius at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID576406Mean residence time in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1374167Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID617587Antibacterial activity against Staphylococcus epidermidis ATCC 12228 by CLSI method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents. Part II.
AID1308241Bacteriostatic activity against methicillin-resistant Staphylococcus aureus NRS702016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID576432Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID370029Antibacterial activity against 3.6 x 10'8 CFU methicillin-resistant Staphylococcus aureus COL by dilution susceptibility test2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID533009Antibacterial activity against vancomycin-intermediate Staphylococcus aureus 28160 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID368286Half life in rabbit plasma at 58 mg/kg after 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID1374174Antibacterial activity against Staphylococcus epidermidis ATCC 12228 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID260056Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
New potential antibacterials: a synthetic route to N-aryloxazolidinone/3-aryltetrahydroisoquinoline hybrids.
AID390328Antimicrobial activity against vancomycin-resistant Enterococcus faecium 700221 clinical isolate2008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID1852676Antibacterial activity against efflux pump lacking Acinetobacter baumannii assessed as inhibition of bacterial growth
AID410110Antimicrobial activity against vanB+ expressing Enterococcus faecalis 1069 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID1547739Drug level in mouse thigh infected with linezolid-resistant Staphylococcus aureus NRS119 at 40 mg/kg, po administered 1 hrs post infection and measured for 48 hrs2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID1374184Bactericidal activity against Staphylococcus aureus ATCC 25923 at 4 times MIC incubated for 24 hrs by time kill curve assay2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID1547718Antibacterial activity against vancomycin-susceptible Enterococcus faecium 119-39A clinical isolate by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID576871Bactericidal activity against 24 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1197128Antibacterial activity against vancomycin-susceptible Enterococcus faecalis 201 clinical isolate after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID576890Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID308729Antibacterial activity against Enterococcus faecalis MG2 EF1 by micro-broth method2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID573891fAUC (0 to 24 hrs) in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID285348Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20020488 in CCY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID528714Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus capitis clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1781724Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as bacterial growth inhibition incubated for 16 to 18 hrs by broth microdilution method
AID519089Antimicrobial activity against Staphylococcus aureus KM166-167 harboring Ser158Leu mutation in rplC gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID1578430Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 by broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Modifying the lipophilic part of phenylthiazole antibiotics to control their drug-likeness.
AID308916Antibacterial activity against Staphylococcus aureus ATCC 33591 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID560501Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gz06040 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1649283Antibacterial activity against Vancomycin-resistant Staphylococcus aureus HIP11983 assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID323814Reduction in bioluminescent methicillin-resistant Staphylococcus aureus Xen1 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, po after 5 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID374005Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 36 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID572284Antimicrobial activity against methicillin susceptible Staphylococcus aureus ATCC 13709 infected in po dosed NMRI mouse treated 1 and 5 hrs post infection2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID583876Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-2 harboring ribosomal protein L3 Gly155Arg/Met169Leu mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID520013Antimicrobial activity against Staphylococcus aureus A87612008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID303915Antibacterial activity against Enterococcus faecalis ATCC 29212 after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID552861Antibacterial activity against Streptococcus pneumoniae infected in po dosed in vivo lung model administered bid for 3 day2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID1375989Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured after 2 weeks2016MedChemComm, Nov-01, Volume: 7, Issue:11
SAR and identification of 2-(quinolin-4-yloxy)acetamides as
AID352924Antibacterial activity against Enterococcus faecium C803 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID583707Antibacterial activity against clinical-derived Staphylococcus aureus isolate 51312 harboring ribosomal protein L3 deltaMet169-Gly174 mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID1180578Antimicrobial activity against Staphylococcus aureus ARC2398 by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID533938Antimicrobial activity against linezolid-resistant Staphylococcus aureus 425 harboring G2447U in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID319985Antimicrobial activity against vancomycin-resistant Enterococcus faecalis NCTC-122012008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID523795Antimicrobial activity against oxacillin-resistant coagulase-negative Staphylococcus aureus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID542694fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 700 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID206148In vitro antibacterial activity against S. a. 213 (Staphylococcus. aureus ATCC 49951)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Influence of ethylene-oxy spacer group on the activity of linezolid: synthesis of potent antibacterials possessing a thiocarbonyl group.
AID576641Bactericidal activity against 2 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID283626Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4536-0367 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID574082Ratio of fAUC (24 hrs) for community-associated methicillin-resistant Staphylococcus aureus OC8525 infected sc dosed mouse to MIC for community-associated methicillin-resistant Staphylococcus aureus OC85252009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID520774Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 60 mg/kg, po administered every 8 hrs for 4 days measured on week 8 postinfection (Rvb = 2.43 +/- 0.15 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID573120Antibacterial activity against coagulase-negative and oxacillin-susceptible Staphylococcus aureus assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID695446Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 5-FQR4M BSA678 expressing GyrA Ser84Leu and Ser85Pro mutant and GrlA Ser80Phe and Glu84Lys mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID390335Antimicrobial activity against Escherichia coli 25922 QC2008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID532797Antibacterial activity against vancomycin-intermediate Staphylococcus aureus NJ after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID373818Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 after 36 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID373994Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after 21 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1852669Antibacterial activity against multidrug resistant Pseudomonas aeruginosa BAA 2109 assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID1361099Bacteriostatic activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID520488Cmin in New Zealand rabbit at 20 mg/kg, sc administered every 6 hrs for 4 days measured after 1 hr post first dose by RP-HPLC/MS/MS2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID1553375Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 after 16 hrs by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1180576Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC2381-2F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1852680Antibacterial activity against wild type Escherichia coli assessed as inhibition of bacterial growth
AID373836Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 504 after 22 passages with Linezolid measured after 10 times antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID763955Antibacterial activity against Moraxella catarrhalis clinical isolate 1 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID577141Apparent volume of distribution in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID542678fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 700 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID528850Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID458457Antimicrobial activity against Pseudomonas aeruginosa K799/61 mutant at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID289863Antibacterial activity against Staphylococcus aureus ATCC 335912007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
AID345133Antimicrobial activity against Haemophilus influenzae 895 (AcrB-KO) by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
AID542914Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing followed by emergence of resistance between 4 to 8 days at 600 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID576872Bactericidal activity against 48 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1308235Antibacterial activity against methicillin-susceptible Enterococcus faecalis ATCC 29212 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID67387In vitro antibacterial activity against vancomycin-susceptible E. f. 153 (Enterococcus faecalis ATCC 29212)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Influence of ethylene-oxy spacer group on the activity of linezolid: synthesis of potent antibacterials possessing a thiocarbonyl group.
AID1056350Antibacterial activity against methicillin-resistant Staphylococcus aureus SR3637 clinical isolate infected in po dosed JCL/ICR systemic infection model assessed as mortality administered after 1 hr of infection measured for 7 days2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID383569Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS 120 with G 2576T mutation by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID745378Inhibition of human CYP2C9 assessed as tolbutamide hydroxylation after 20 mins by LC/MS/MS analysis2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID729216Antibacterial activity against linezolid-resistant Enterococcus faecalis after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID519081Antimicrobial activity against Escherichia coli KM55-68 harboring G2576U mutation in 23S rRNA by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID562629Antimicrobial activity against Group C Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID285071Antimicrobial activity against viridans group Streptococcus anginosus at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID535020Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-17 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID571765Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID593964Antibacterial activity against Escherichia coli ATCC 259222011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
AID13380Oral bioavailability of compound (25 mg/kg) after po administration was determined in Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID1414197Bactericidal activity against clinical isolate of penicillin-resistant Staphylococcus aureus incubated for 24 hrs followed by plating onto tryptic soy agar plates and further incubated for 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID541076Cmin in cage fluid of Albino guiena pig at 50 mg/kg, ip after 12 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1435924Antibacterial activity against methicillin/ciprofloxacin/clindamycin-resistant Staphylococcus aureus USA100 NRS382 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID373803Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 Michigan after 28 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID285114Antimicrobial activity against viridans group Streptococcus oralis at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID585173Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2055A, A2572U mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID562591Antimicrobial activity against Enterococcus faecium clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID575082Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1873912Antibacterial activity against Staphylococcus chromogenes incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID775545Antibacterial activity against Streptococcus pneumoniae SR26207 clinical isolate assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID1504619Antibacterial activity against methicillin-resistant Staphylococcus aureus 1201984 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID458455Antimicrobial activity against vancomycin-resistant Enterococcus faecalis 1528 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID1151740Antibacterial activity against Staphylococcus aureus measured after 2 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID730383Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID1584843Antibacterial activity against hospital-acquired methicillin/ciprofloxacin/moxifloxacin resistant Staphylococcus aureus SA 481 after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID1350032Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 3 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID207795Compound was evaluated for minimum inhibitory concentration against Staphylococcus aureus 9721 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID541082Cmax in cage fluid of Albino guiena pig at 75 mg/kg, ip after 3 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID522898Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1015 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID410117Antimicrobial activity against Haemophilus influenzae by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID532022Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to CFU count by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID1474205Antibacterial activity against Enterococcus faecalis clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1594372Antibacterial activity against Enterobacter cloacae BAA1134 after 18 to 24 hrs in presence of colistin by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID520016Antimicrobial activity against Staphylococcus epidermidis A89342008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID576861Bactericidal activity against 14 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID246862Efficacy against mice infected with Staphylococcus aureus ATCC 25923 upon s.c. administration2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID532811Antibacterial activity against vancomycin-susceptible Staphylococcus aureus BR5-1 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID565080Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus 56 by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
AID1472757In vivo anti-virulence activity against methicillin-resistant Staphylococcus aureus LRSA202 infected in BALB/c mouse model assessed as reduction in bacterial load in kidney at 0.1 mg bid for 3.5 days administered intraperitoneally 6 hrs post infection by 2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID519482Antibacterial activity against Staphylococcus aureus T2019 with G2576T mutation in 23S rRNA genes by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID533934Antimicrobial activity against linezolid-resistant Staphylococcus aureus CM/05 3067 harboring chromosomal cfr gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID206223In vitro antibacterial activity against Staphylococcus epidermis (S.e.2) C2235.1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID558518Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID206650Antibacterial activity was determined against clinically isolated Levofloxacin-methicillin resistant Staphylococcus aureus (LVFX-r MRSA) strains (74 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID533977Antimicrobial activity against linezolid-susceptible Staphylococcus aureus NRS18 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID573860Antibacterial activity against Methicillin-susceptible Staphylococcus aureus ATCC 13709 after 16 to 20 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID564819Antimicrobial activity against methicillin-resistant coagulase-negative Staphylococcus hominis assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID535254Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-2 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID577101T>MIC in Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID583405Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate MI assessed as bacterial count at 16 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID1563582Inhibition of FabB/FabF in methicillin-resistant Staphylococcus aureus assessed as antibacterial activity at 5 ug/disk after 18 hrs by agar disk diffusion method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID531636Inhibition of 50S ribosomal subunit purified from Staphylococcus aureus ATCC 29213 assessed as inhibition of translation using in vitro transcribed mRNA encoding firefly luciferase2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID69613Antibacterial activity against Escherichia coli (OC 2605)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID285149Antimicrobial activity against viridans group Streptococcus mitis by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID576123Antibacterial activity against 1 x 10'4 CFU Streptococcus pneumoniae ATCC 6305 infected in ICR mouse systemic infection model assessed as mouse protection administered orally twice after 1 and 4 hrs post infection measured after 48 hrs2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1770371Ratio of MBC to MIC against Vancomycin-resistant Enterococcus faecalis ATCC 512992021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID561262Antibacterial activity against Enterococcus faecalis assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID283166Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5204 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID583891Antibacterial activity against vancomycin-heteroresistant Staphylococcus aureus isolate 38 (Mu3) by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID444262Antibacterial activity against Enterococcus faecalis ATCC 29212 by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID1233137Antibacterial activity against patient-derived methicillin-resistant Staphylococcus aureus 7425 after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID245216Minimum inhibitory concentration against Enterococcus faecalis (strain A20688) in presence of 50% calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID1168086Antibacterial activity against Enterococcus infected in Wistar albino rat assessed as reduction in cell count at 25 mg/kg, iv after 1 hr relative to control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1739763Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition incubated for 3 weeks by Microplate Alamar Blue Assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
AID206055Inhibitory activity against methicillin-resistant Staphylococcus epidermidis (MRSE)1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1395677Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS384 USA300 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID637972Antibacterial activity against Enterococcus faecium expressing VanA gene after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID717214Antimicrobial activity against methicillin-resistant Staphylococcus aureus CCARM 3634 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID583708Antibacterial activity against laboratory-derived Staphylococcus aureus ATCC 29213 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID1501365Bactericidal activity against methicillin-resistant Staphylococcus aureus USA100 NRS382 incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID535010Antimicrobial activity against daptomycin-nonsusceptible Staphylococcus aureus assessed as susceptible isolates by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1151748Antibacterial activity against Staphylococcus aureus measured after 10 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID548745Antimicrobial activity against Beta-hemolytic Streptococcus assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID562380Antimicrobial activity against Enterococcus faecium expressing VanB gene clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID268864Antibacterial activity against vancomycin-sensitive Enterococcus faecalis ATCC 292122006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis of novel tricyclic oxazolidinones by a tandem SN2 and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid.
AID495880Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected New Zealand White rabbit aortic valve endocarditis model assessed as decrease in bacterial colony forming unit in kidney at 75 mg/kg, sc dosed every 8 hrs for 4 days (2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ceftobiprole is superior to vancomycin, daptomycin, and linezolid for treatment of experimental endocarditis in rabbits caused by methicillin-resistant Staphylococcus aureus.
AID1361121Bacteriostatic activity against Klebsiella pneumoniae BAA 1706 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID70795In vitro minimum inhibitory concentration (MIC) against Escherichia coli UC66742003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID1539458Antibacterial activity against Clostridium difficile ATCC BAA 1870 incubated for 48 hrs in anaerobic condition by CLSI-based broth microdilution assay
AID1574840Antibacterial activity against clinical isolates of methicillin-sensitive Staphylococcus aureus by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID560809Absorption half life in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID429427Antibacterial activity against Haemophilus influenzae isolate 282 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID1778103Antibacterial activity against linezolid resistant Enterococcus faecium 13549 assessed as bacterial growth inhibition after 18 hrs by broth microdilution method
AID575146Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolate NRS123 by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID285065Antimicrobial activity against beta hemolytic Streptococci group G at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID348596Antibacterial activity against Enterococcus faecalis C474 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID745382Antibacterial activity against methicillin-resistant Staphylococcus aureus SR3637 infected in JCL/ICR mouse systemic infection model assessed as mortality administered as iv measured over 7 days2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID576665Bactericidal activity against 48 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid for every 12 hrs administered as 2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID495883Plasma concentration in Staphylococcus aureus COL infected New Zealand White rabbit aortic valve endocarditis model at 75 mg/kg, sc dosed every 8 hrs for 4 days2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ceftobiprole is superior to vancomycin, daptomycin, and linezolid for treatment of experimental endocarditis in rabbits caused by methicillin-resistant Staphylococcus aureus.
AID590060Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1390476Antibacterial activity against Escherichia coli MG16552018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1174903Antibacterial activity against Staphylococcus aureus Mu50 ATCC 700699 by broth microdilution method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID458454Antimicrobial activity against Enterococcus faecalis ATCC 49532 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID1519270Antibacterial activity agianst linezolid-resistant Enterococcus faecalis2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID516169Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolates assessed as resistant isolates by EUCAST method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID558508Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1390472Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 359842018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1117375Antimicrobial activity against Staphylococcus aureus Efs1 assessed as partially clear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID1168013Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 3864 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1591560Bactericidal activity against Staphylococcus aureus ATCC 25923 assessed as 3 log reduction in number of colony forming units incubated for 24 hrs followed by aliquots transfer to tryptic soy agar and grown for 24 hrs2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID1680040Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 6 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1409850Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in liver at 0.1 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 4.52018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID564320Antimicrobial activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 assessed as resistant bacteria in tissue cage fluid selected on 4 ug/ml of compound measured on day 8 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID575044Drug excretion in healthy human urine assessed as unchanged compound at at 600 mg, po2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID285340Antibacterial activity against Staphylococcus aureus LUG855 in Mueller-Hinton medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID590061Antibacterial activity against vancomycin-resistant Enterococcus by agar dilution method2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID1832942Antibacterial activity against Staphylococcus aureus 1199B assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID1056362Antibacterial activity against methicillin-resistant Staphylococcus aureus SR3637 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID561740Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as susceptible isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1474203Antibacterial activity against Enterococcus faecium clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID576415Apparent volume of distribution in two-compartment pharmacokinetic/pharmacodynamic model at 400 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID206237In vitro antibacterial activity against Staphylococcus aures strain UC 92131996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1395973Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-1707 after 16 to 18 hrs by broth microdilution method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID561727Antibacterial activity against Enterococcus faecium assessed as susceptible isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1400046Antibacterial activity against Enterococcus faecalis ATCC 349 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID287261Antimicrobial activity against methicillin-susceptible coagulase-negative staphylococcus by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID1547716Antibacterial activity against vancomycin-susceptible Enterococcus faecalis 201 clinical isolate by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID54143Inhibitory activity against Corynebacterium1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID576428Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID558524Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID563322Antibacterial activity against vancomycin-resistant Enterococcus faecalis EF NJ1 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID1304835Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-1707 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID528690Antibacterial activity against Streptococcus pyogenes MED 2040 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1699554Induction of cell membrane permeabilization in GFP-expressing Staphylococcus aureus ATCC 700699 assessed as increase in cellular ATP leakage at 5 fold MIC measured after 0.5 hrs by Bactiter-glo assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial
AID1553384Inhibition of CYP3A4 (unknown origin)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1184283Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 infected in Swiss albino CD-1 mouse compound administered orally bid at 1 hr and 4 hrs post infection2014European journal of medicinal chemistry, Sep-12, Volume: 84Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors.
AID520229Antimicrobial activity against methicillin-resistant Staphylococcus aureus BK 115122008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID541053Ratio of AUC (0 to 24 hrs) to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 25 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID532792Antibacterial activity against vancomycin-intermediate Staphylococcus aureus 99/3700-W after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID542890fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 400 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1139117Antimicrobial activity against Streptococcus pneumoniae in presence of 50% human serum2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID574077Apparent oral clearance in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID582810Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS05417 harboring MLST sequence type ST17 and pulsotype A expressing vanA gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1770363Ratio of MBC to MIC against penicillin-resistant Staphylococcus aureus ATCC 310072021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID284951Antimicrobial activity against Bacillus cereus at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID274225Antibacterial activity against Streptococcus pneumoniae SVI SP-32006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID285105Antimicrobial activity against viridans group Streptococcus mitis at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1594389Half life in human at 625 mg, iv2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID374010Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 15 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID645035Antibacterial activity against erythromycin-resistant Streptococcus pyogenes 47 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID319157Plasma concentration in human at 625 mg, po bid after 14 days2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID583888Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus isolate 336 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID318351Antibacterial activity against methicillin-sensitive Staphylococcus aureus2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID1361049Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 after 16 to 18 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Halogenated quinolines bearing polar functionality at the 2-position: Identification of new antibacterial agents with enhanced activity against Staphylococcus epidermidis.
AID373844Antimicrobial activity against methicillin and vancomycin-resistant Staphylococcus aureus 509 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID542920Antimicrobial activity against wild-type Bacillus anthracis2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID544825Antimicrobial activity against Staphylococcus aureus Xen 30 biofilm assessed as log10 CFU/cm'2 in bacterial count in presence of 2000 microamperes of electric current by bioelectric effect assay2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID561234Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID374012Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID528966Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID576652Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID532785Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR5-1 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID373822Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after 15 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1395676Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123 USA400 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID561734Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as resistant isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1611122Antibacterial activity against vancomycin-resistant Enterococcus faecium CLSI-based double dilution method2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
AID285001Antimicrobial activity against Enterococcus gallinarum at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID429424Antibacterial activity against vancomycin-resistant Enterococcus by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID533952Antimicrobial activity against Staphylococcus epidermidis SA362 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1167731Antimicrobial activity against Streptococcus pneumoniae by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID283633Antimicrobial activity against Staphylococcus aureus RN4220 with 23S rRNA G2447T mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID560357Cmax in healthy human male at 600 mg, po every 12 hrs by LC/MS/MS analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID555303Antibacterial activity against methicillin-resistant Staphylococcus aureus 145 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1435929Bactericidal activity against methicillin/ciprofloxacin/gentamicin/clindamycin-resistant Staphylococcus aureus USA200 NRS383 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID1721017Stability in CD-1 mouse liver microsome assessed as parent compound remaining at 1 uM measured after 30 mins in presence of NADPH by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1474261Ratio of MBC50 to MIC50 for Enterococcus faecalis clinical isolates2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID558703Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID208733Compound was evaluated for minimum inhibitory concentration against Streptococcus A 44 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID523777Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as percent susceptible strain by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID559564Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP8 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1609270Antibacterial activity against methicillin-resistant Staphylococcus epidermidis NRS101 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID297132Antibacterial activity against Pseudomonas aeruginosa 46001 by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1367596Efflux index, ratio of MIC for wild type Escherichia coli MG1655 to MIC for Escherichia coli MG1655 expressing AcrAB-TolC efflux pump deletion mutant2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Compound design guidelines for evading the efflux and permeation barriers of Escherichia coli with the oxazolidinone class of antibacterials: Test case for a general approach to improving whole cell Gram-negative activity.
AID534248Antimicrobial activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells at pH 7.4 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID409580Antimicrobial activity against methicillin-resistant Staphylococcus aureus after 16 to 18 hrs by agar dilution method2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID410219Antibacterial activity against Escherichia coli LCB0010 at 128 ug/mL by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID533754Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus ATCC 33591 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1760592Antibacterial activity against Enterococcus faecium 35667 assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID1395988Induction of biofilm eradication of vancomycin-resistant Enterococcus faecium ATCC 700221 after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID1151760Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID424763Antibacterial activity against Staphylococcus epidermidis CL8040 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID555499Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 051 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID387449Antibacterial activity against methicillin-resistant Staphylococcus aureus DRCC 0192008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID1304834Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-44 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID522904Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1005 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1361122Bacteriostatic activity against Pseudomonas aeruginosa ATCC 15442 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID753124Antibacterial activity against Micrococcus luteus MTCC 2470 assessed as growth inhibition after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID373846Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 Hershey after 18 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID575080Antimicrobial activity against Streptococcus pneumoniae serotype 11A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID576126Antibacterial activity against 1 x 10'7 CFU methicillin-susceptible Staphylococcus aureus Giorgio infected in ICR mouse systemic infection model assessed as mouse protection administered orally twice after 1 and 4 hrs post infection measured after 48 hrs2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID576399Residual concentration at the end of the administration interval in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID561339Antimicrobial activity against Staphylococcus aureus isolate UAMS-929 harboring sarA gene mutant by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of sarA on antibiotic susceptibility of Staphylococcus aureus in a catheter-associated in vitro model of biofilm formation.
AID1653082Antibacterial activity against Bacillus megaterium2019European journal of medicinal chemistry, Feb-15, Volume: 164Isatin derivatives and their anti-bacterial activities.
AID562637Antimicrobial activity against Listeria monocytogenes assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID532023Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to CFU count by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID285137Antimicrobial activity against viridans group Streptococcus vestibularis at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1271223Antibacterial activity against Streptococcus pneumoniae ATCC 49619 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1424066Antibiotic activity against methicillin-resistant Staphylococcus aureus isolate CAIRD116 by broth microdilution assay or Alamar blue dye based colorimetric assay2017Journal of natural products, 04-28, Volume: 80, Issue:4
The Berkeleylactones, Antibiotic Macrolides from Fungal Coculture.
AID1609288Antibacterial activity against methicilline-sensitive Staphylococcus aureus ATCC 6538 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID40483Minimum inhibitory concentration against Bacillus pumilus MTCC 16072004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID726187Inhibition of human MAO-A assessed as residual activity at 10 uM2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID558507Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID474997Antibacterial activity against methicillin-resistant Staphylococcus aureus LCB0002 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID1692901Antibacterial activity against methicillin-resistant Staphylococcus aureus2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID576410AUC in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID498906fAUC (0-infinity) in immunocompetent SKH1 mouse plasma at 50 mg/kg, po2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID734690Antibacterial activity against Micrococcus luteus MTCC 2470 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID528712Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus hominis subsp. novobiosepticus clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID560513Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b6k7974 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1547705Antibacterial activity against Staphylococcus aureus N315 (NRS70) by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID292611Antimicrobial activity against Streptococcus pyogenes ATCC 19615 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID1395982Induction of biofilm eradication of methicillin-resistant Staphylococcus aureus 2 after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID759678Cytotoxicity against porcine PK-15 cells assessed as stimulation of cell replication at 400 ug/mL2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID1193406Antimicrobial activity against TolC-deficient Escherichia coli BW25113 measured after overnight incubation2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Identification of Bacillus anthracis PurE inhibitors with antimicrobial activity.
AID284962Antimicrobial activity against Corynebacterium spp. at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID391593Antibacterial activity against vancomycin-resistant Enterococcus faecium A2280 by agar dilution method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials.
AID576894Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID283385Decrease in mitochondrial Cytochrome C oxidase protein expression in PBMCs from patient on a long-term schedule of the drug with hyperlactatemia relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reversible inhibition of mitochondrial protein synthesis during linezolid-related hyperlactatemia.
AID542693fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID373306Lipophilicity, log P of the compound2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID1553370Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 measured after 18 hrs by broth microdilution method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1271218AUC (0 to t) in BALB/c mouse plasma at 10 mg/kg, po by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID283389Effect on mitochondrial mass in PBMCs from patient during hyperlactemic phase by V-DAC method relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reversible inhibition of mitochondrial protein synthesis during linezolid-related hyperlactatemia.
AID561724Antibacterial activity against Enterococcus faecium assessed as resistant isolates by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1311366Antibacterial activity against methicillin-sensitive Mycobacterium tuberculosis H37Rv measured after 14 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID533951Antimicrobial activity against hospital acquired methicillin-resistant, vancomycin resistant Staphylococcus aureus VRS2 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID534507Drug level in human THP1 cells at 250 mg/L after 2 hrs in presence of 50 uM proton inophore monesin relative to control2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
AID205681Minimum inhibitory concentration against Staphylococcus aureus OC 4172 in precense of 50% mouse serum2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
AID1151623Toxicity in female rat assessed as effect on hemoglobin level at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 141.8 g/L)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID374002Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1873890Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^5 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID263965Antibacterial activity against vancomycin-resistant Enterococcus faecalis DRCC 1542006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID560827AUC (0 to 12 hrs) in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID522893Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1010 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID545816Antimicrobial activity against 4.6 X 10'6 CFU/peg methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as inhibition of biofilm formation after 24 hrs by serial dilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID576429Bactericidal activity against 1 hr peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID206647Antibacterial activity against methicillin susceptible Staphylococcus aureus (MSSA)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID285014Antimicrobial activity against Enterococcus raffinosus at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID572486Antimicrobial activity against Streptococcus pneumoniae ATCC 6303 infected in po dosed NMRI mouse administered thrice daily for 4 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID1271230Antibacterial activity against clinical isolate Neisseria meningitidis E-95 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID396028Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID284959Antimicrobial activity against Corynebacterium spp. at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1703714Antibacterial activity against methicillin-resistant Staphylococcus aureus USA500 NRS385 assessed as inhibition of bacterial growth measured after 18 to 20 hrs by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID10894Tmax in male rat2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID67094Compound was evaluated for minimum inhibitory concentration against Enterococcus faecalis 68 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID283161Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2588 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1704213Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 incubated for 18 hrs2020European journal of medicinal chemistry, Nov-15, Volume: 2061,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
AID576395Cmax in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID763982Antibacterial activity against vancomycin-resistant Enterococcus after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1501364Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS123 (USA400) incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID533987Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus SA238 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID207646Antibacterial activity against Staphylococcus aureus UC92131998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID542895fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID285350Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20040332 in CCY media2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID1350037Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 8 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID558716Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID577104AUBC (0 to 24 hrs) in Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1197126Antibacterial activity against Bacillus licheniformis ATCC 12759 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1414190Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID576884Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID577126Residual concentration at the end of the administration interval in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1596563Bactericidal activity against methicillin-resistant Staphylococcus aureus USA300 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID560509Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b4k6307 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID285341Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus HT20010734 in in Mueller-Hinton medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID564321Antimicrobial activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 assessed as resistant bacteria in tissue cage fluid selected on 4 ug/ml of compound measured on day 11 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID85980In vitro antibacterial activity against ampicillin resistant Haemophilus influenzae 30063 (AMPR b-lactamase+)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID1653047Antibacterial activity against Staphylococcus aureus2019European journal of medicinal chemistry, Feb-15, Volume: 164Isatin derivatives and their anti-bacterial activities.
AID373830Antimicrobial activity against panton-valentine leukocidin-positive community-acquired methicillin-resistant Staphylococcus aureus 490 after 14 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection techni2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1374168Antibacterial activity against Staphylococcus aureus ATCC 6538 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID363436Antibacterial activity against Streptococcus pneumoniae ATCC 6303-infeceted Sprague-Dawley rat assessed as reduction in lung bacterial density at 50 mg/kg, po administered twice at 18 and 26 hrs after bacterial challenge measured at 72 hrs postinfection2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
AID525132Antibacterial activity against Staphylococcus aureus KM53 after 18 to 24 hrs by broth microdilution method selected after 16 ug/ml drug exposure for 6 hrs by culture absorbance method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID562233Antibacterial activity against methicillin-resistant Staphylococcus aureus OC2878 by broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID284958Antimicrobial activity against Corynebacterium spp. at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1603255Antibacterial activity against Mycobacterium tuberculosis H37Rv harboring LuxAB incubated for 10 days under anaerobic conditions followed by incubation under aerobic conditions for 28 hrs by LORA method
AID1677795Bacteriostatic activity against methicillin-resistant Staphylococcus aureus ATCC43300 assessed as ratio of MBC to MIC2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID531645Displacement of [3H]puromycin from 70S ribosomal complex in Staphylococcus aureus ATCC 29213 by competitive binding assay2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID671568Antibacterial activity against methicillin-resistant Staphylococcus aureus VL-137 infected in neutropenic Balb/c mouse assessed as reduction in lung CFU at 10 mg/kg, iv administered 2 and 12 hrs post infection measured 24 hrs post treatment2012Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
Fluorocyclines. 2. Optimization of the C-9 side-chain for antibacterial activity and oral efficacy.
AID68391In vitro antibacterial activity against vancomycin-resistant Enterococcus faecium 2164 (VRE.3)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID244998Antibacterial activity against Enterococcus faecalis ATCC 19433 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID410204Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID552859Antibacterial activity against Enterococcus faecalis infected in po dosed in vivo acute model administered bid for 1 day2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID734709Antibacterial activity against Bacillus subtilis MTCC 121 after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID576897Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1407933Antibacterial activity against methicillin-resistant Staphylococcus aureus USA100 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID558531Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID645032Antibacterial activity against Streptococcus pyogenes ATCC 19615 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID525126Suppression of drug resistance development in LZD intermediate-resistant Staphylococcus aureus KM183 assessed as prolonged length of subculture to develop Linezolid resistance at 4 times MIC and 0.25 times IC50 after 8 days2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID542908Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as prevention of bacterial regrowth at 700 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1877891Antibacterial activity against Escherichia coli K12 harbouring TolC-deficient mutant assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID1168025Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 6/22 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1312946Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS119 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID388043Antibacterial activity against methicillin-susceptible Staphylococcus aureus MB2865 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID483194Antibacterial activity against Staphylococcus epidermidis ATCC 12228 by microbroth dilution technique2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID1390460Antibacterial activity against Enterococcus faecium 5752018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1151737Antibacterial activity against linezolid-resistant Staphylococcus aureus isolate 41842014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID206727In vitro antibacterial activity against the methicillin-resistant Staphylococcus aureus 881999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
3D QSAR studies on new oxazolidinone antibacterial agents by comparative molecular field analysis.
AID297120Antibacterial activity against vancomycin-resistant Staphylococcus aureus 70 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1312948Bactericidal activity against methicillin-resistant Staphylococcus aureus USA100 NRS382 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID390336Antimicrobial activity against extended spectrum beta-lactamase producing Escherichia coli 22692008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID1361123Bacteriostatic activity against Escherichia coli BW25113 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID535260Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-8 expressing SCCmec element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1563584Inhibition of FabB/FabF in Staphylococcus aureus ATCC 29213 assessed as antibacterial activity after 16 hrs by agar dilution method2019Journal of medicinal chemistry, 07-25, Volume: 62, Issue:14
Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
AID1609284Antibacterial activity against methicilline-resistant Staphylococcus aureus NRS386 USA700 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID206450In vitro antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) C6068.1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID319162Protein binding in human plasma2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1852685Antibacterial activity against recombinant OM pore producing Pseudomonas aeruginosa assessed as inhibition of bacterial growth
AID1770351Antibacterial activity against Vancomycin-susceptible Enterococcus faecium ATCC 19434 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID520765Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as improvement in rate of bone reconstruction at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 6 po2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID370014Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 3.12 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1393953Antibacterial activity against methicillin resistant Staphylococcus aureus BAA-44 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID1770368Ratio of MBC to MIC against Vancomycin-susceptible Enterococcus faecalis ATCC 292122021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID285031Antimicrobial activity against Rothia mucilaginosa at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID517668Antimicrobial activity against methicillin-resistant Staphylococcus aureus 92-1191 by standard serial-dilution technique2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
AID534509Drug level in human THP1 cells at 50 mg/L after 30 mins at pH 62010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
AID1609277Bactericidal activity against methicilline-resistant Staphylococcus aureus NRS-119 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1704212Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 incubated for 18 hrs2020European journal of medicinal chemistry, Nov-15, Volume: 2061,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
AID283617Antimicrobial activity against Enterococcus faecium 44 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID1692902Antibacterial activity against methicillin-sensitive Staphylococcus aureus2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID285161Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID577091Ratio of AUC (0 to 24 hrs) to MIC for Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID583391Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate NJ992 assessed as bacterial count at 4 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID287262Antimicrobial activity against Streptococcus pneumoniae by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID283384Decrease in mitochondrial Cytochrome C oxidase 2 protein expression in PBMCs from patient on a long-term schedule of the drug with hyperlactatemia relative to control2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Reversible inhibition of mitochondrial protein synthesis during linezolid-related hyperlactatemia.
AID583893Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 435 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID532799Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID285066Antimicrobial activity against beta hemolytic Streptococci group G at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID303968Bactericidal activity against Streptococcus pneumoniae after 48 hrs by time kill study2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID1680041Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 5 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID278923Antibacterial activity against macrolide-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
In vitro antibacterial activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID567452Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK4 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID285131Antimicrobial activity against viridans group Streptococcus sanguinis at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID477375Antibacterial activity against Klebsiella pneumoniae ATCC 27736 after 24 hrs2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial.
AID576653Bactericidal activity against 13 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID560363Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 51559 by broth dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1504625Antibacterial activity against Staphylococcus epidermidis ATCC 14990 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID523817Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID285016Antimicrobial activity against Enterococcus raffinosus at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID522922Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 1471 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1151741Antibacterial activity against Staphylococcus aureus measured after 3 serial passages2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1327110Antibacterial activity against Pseudomonas aeruginosa NCIM 2036 at 3 ug/ml measured after 8 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID575160Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose upto 2 mM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID565502Plasma protein binding in human2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID734686Antibacterial activity against Pseudomonas aeruginosa MTCC 2453 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID576883Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID375354Antibacterial activity against Staphylococcus aureus infected iv bid dosed mouse model assessed as reduction of colony forming unit in kidney2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
AID548475Antibacterial activity against vancomycin-susceptible Staphylococcus aureus Mu50omega expressing vraSm, graRm mutant gene after 48 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID1271228Antibacterial activity against clinical isolate Neisseria meningitidis M-1 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1603256Antibacterial activity against RMP-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay
AID1723515Bacteriostatic activity against Enterococcus faecium ATCC 700221 assessed as reduction in bacterial burden at 5 times MIC preincubated for 24 hrs followed by replating on soya agar plates and measured after 16 hrs by time-kill assay
AID533420Antimicrobial activity against Micromonas micros assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID66896Antibacterial activity against Enterococcus faecalis (ATCC 29212)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID405632Drug level at steady state in human serum at 600 mg administered every 12 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID533753Antimicrobial activity against linezolid resistant methicillin-susceptible Staphylococcus aureus SA040L after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID541065Half life in cage fluid of Albino guiena pig at 75 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID548523Antimicrobial activity against Vancomycin-susceptible Enterococcus faecium assessed as percent resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID68563Minimum inhibitory concentration measured against Enterococcus faecium2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID1680068Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as reduction in bacterial growth incubated 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID1519041Antibacterial activity against clinical isolates of methicillin-sensitive Staphylococcus aureus assessed as reduction in bacterial cell growth by CLSI protocol based broth microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID1395678Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS385 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1770344Antibacterial activity against penicillin-susceptible Pseudomonas aeruginosa ATCC 27853 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID1888847Antibacterial activity against Staphylococcus aureus 1199 measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1390461Antibacterial activity against PVL positive Staphylococcus aureus2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID573154Antibacterial activity against vancomycin-resistant Enterococcus faecalis assessed as resistant isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID293554Antibacterial activity against Bacillus subtilis MTCC 121 after 24 hrs by agar dilution assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Organoiodine(III) mediated synthesis of 3,9-diaryl- and 3,9-difuryl-bis-1,2,4-triazolo[4,3-a][4,3-c]pyrimidines as antibacterial agents.
AID523292Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as 2 log reduction in bacterial burden in lungs orally treated in water-1% methylcellulose upto 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID1687309Synergistic antibacterial activity against Escherichia coli ATCC 25922 in presence of 0.25 times MIC of colistin incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID67400In vitro antibacterial activity against Enterococcus faecalis strain ATCC 292121996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1704255Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 measured after 18 hrs by CLSI-based broth microdilution method2020European journal of medicinal chemistry, Nov-15, Volume: 2061,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
AID530050Antimicrobial activity against Staphylococcus aureus 286607-R1 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID284956Antimicrobial activity against Bacillus cereus at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID303912Antibacterial activity against methicillin-resistant Staphylococcus aureus 562 after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID535022Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-19 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1710587Antibacterial activity against cephalosporin-resistant Streptococcus pneumoniae ATCC 51916 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID352926Antibacterial activity against Streptococcus pyogenes ATCC 8736 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID283631Antimicrobial activity against methicillin-resistant Staphylococcus aureus B2 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID475010Antibacterial activity against Haemophilus influenzae LCB0015 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID531640Antimicrobial activity against linezolid-,erythromycin-resistant Staphylococcus aureus A7820 with G2576U mutation at 23s rRNA2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID390326Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 20122008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID409578Antimicrobial activity against Staphylococcus aureus ATCC 29213 after 16 to 18 hrs by agar dilution method2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID284940Antimicrobial activity against Aerococcus spp. at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID573135Antibacterial activity against erythromycin-nonsusceptible Streptococcus pyogenes assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID560518Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 15b52 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID285346Antibacterial activity against Staphylococcus aureus LUG855 in CCY media2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID542900fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID405630Toxicity in rabbit heart mitochondria assessed as inhibition of mitochondrial protein synthesis2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID576867Bactericidal activity against 12 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1721020Antitubercular activity against linezolid-resistant Mycobacterium tuberculosis incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID209463In vitro antibacterial activity against Streptococcus pyogenes ATCC 8668 (S.p.1).1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1393957Antibacterial activity against methicillin resistant Staphylococcus aureus NR 45898 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID206228In vitro antibacterial activity against Staphylococcus epidermis strain UC 300311996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID576663Bactericidal activity against 14 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID532804Antibacterial activity against vancomycin-susceptible Staphylococcus aureus 99/3700-W after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1352003Antibacterial activity against methicillin/linezolid-resistant Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as decrease in bacterial survival in mouse liver at 0.4 mg, ip bid administered 4.5 days measured after 90 hrs2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.
AID283391Antimicrobial activity against Nocardia farcinica after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID520028Antimicrobial activity against Enterococcus faecium A63452008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID542883fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID559363Antimicrobial activity against compound-susceptible Coxiella burnetii Q212 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1861525Cmax in Wistar rat at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID1514448Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID323813Reduction in bioluminescent methicillin-resistant Staphylococcus aureus Xen1 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, po after 3 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID560365Antimicrobial activity against vancomycin-resistant Enterococcus faecalis 1058946 by broth dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID564092Antimicrobial activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 by M7-A6 method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID576888Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1680055Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 10 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID285045Antimicrobial activity against Enterococcus casseliflavus by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1190641Antibacterial activity against Pseudomonas aeruginosa NCIM-2036 incubated for 24 hrs by two fold serial dilution method2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Biofilm inhibition of linezolid-like Schiff bases: synthesis, biological activity, molecular docking and in silico ADME prediction.
AID577098T>MIC in Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1395708Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS385 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID763983Antibacterial activity against vancomycin-susceptible Enterococcus after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1327112Antibacterial activity against Staphylococcus aureus NCIM 2079 at 10 ug/ml measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID531639Antimicrobial activity against Staphylococcus aureus ATCC 292132008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID207025Antibacterial activity against methicillin susceptible Staphylococcus aureus (OC 4172) in broth (without serum)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID1303407Antibacterial activity against Pseudomonas aeruginosa after 24 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID262234Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS 1192006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID1151750Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate 06122014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1770350Antibacterial activity against Vancomycin-susceptible Enterococcus faecalis ATCC 29212 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID562592Antimicrobial activity against Enterococcus faecalis expressing VanB gene clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID532787Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR3 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID574554Decrease in PSMbeta1 levels in Staphylococcus aureus USA300 at subinhibitory concentration after 24 hrs by RP-HPLC/ESI-MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID283640Antimicrobial activity against Staphylococcus aureus ST/02/2121 with 23S rRNA G2447T mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID348865Antibacterial activity against vancomycin-resistant Enterococcus 6 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID530128Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID1139120Dose normalized AUC in rat at 2.8 to 9.5 mg/kg, iv2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID520027Antimicrobial activity against Enterococcus faecium A59602008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1547712Antibacterial activity against Staphylococcus haemolyticus ATCC 29970 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID244877Antibacterial activity against Escherichia coli NIHJ was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID562173Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 after 50 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID574069Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus OC8525 infected in SKH1 mouse assessed as log reduction in CFU/g skin at 5 mg/kg/day, sc administered post infection measured after 48 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID409584Antimicrobial activity against methicillin-resistant Staphylococcus aureus 05-2 infected in iv dosed KunMing SPF mouse2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID285093Antimicrobial activity against viridans group Streptococcus gordonii at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID499160Protein binding in mouse plasma2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID572274Antimicrobial activity against multiple drug-resistant Streptococcus pneumoniae ATCC 700677 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID283638Antimicrobial activity against Staphylococcus aureus ST/02/21212007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID533011Antibacterial activity against vancomycin-intermediate Staphylococcus aureus BR2 phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID559359Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii Nine-Mile obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID274228Antibacterial activity against Haemophilus influenzae HI35422006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
AID295159Antibacterial activity against penicillin-resistant Streptococcus pneumoniae by microdilution broth method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID285357Decrease in Panton-Valentine leukocidin level in community acquired methicillin-resistant Staphylococcus aureus HT20041010 in CYY medium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Effect of antibiotics on Staphylococcus aureus producing Panton-Valentine leukocidin.
AID207797Compound was evaluated for minimum inhibitory concentration against Staphylococcus aureus 9776 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID583885Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus isolate 56 (494) by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID523830Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 64 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID559552Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP4 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID575046Cmin in human surgical patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID1407935Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID267724Antimicrobial activity against Moraxella catarrhalis2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and structure-activity studies of antibacterial oxazolidinones containing dihydrothiopyran or dihydrothiazine C-rings.
AID726186Inhibition of human MAO-B assessed as residual activity at 10 uM2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID1594370Antibacterial activity against Pseudomonas aeruginosa ATCC 15442 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1167987Antibacterial activity against vancomycin-resistant Enterococcus ATCC 51299 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID245334In vitro minimum inhibitory concentration against Enterococcus faecalis [(VRE) ATCC 346-VRE and 5B-VRE]2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID576644Bactericidal activity against 13 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID583390Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus isolate MU50 assessed as bacterial count at 32 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID763947Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID287264Antimicrobial activity against vancomycin-resistant Enterococcus by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID283636Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS revertant with 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID558710Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 measured on day 40 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID318362Antibacterial activity against Staphylococcus aureus expressing antisense fabF assessed as drug level causing >5 mm zone of inhibition after 18 hrs by agar diffusion two plate differential sensitivity antisense assay2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID352930Antibacterial activity against vancomycin-resistant Enterococcus faecalis after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID535001Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus assessed as susceptible isolates by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1390474Antibacterial activity against linezolid-resistant Staphylococcus epidermidis 10891912018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID368284Cmax in rabbit plasma at 58 mg/kg after 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID583875Antibacterial activity against laboratory-derived Staphylococcus aureus isolate 29213-1 harboring ribosomal protein L3 Gly155Arg mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID383743Half life in Sprague-Dawley rat at 25 mg/kg, po2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID1574834Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID1308234Antibacterial activity against Bacillus licheniformis ATCC 12759 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID1501367Bactericidal activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID444264Antibacterial activity against Streptococcus pyogenes ATCC 19615 by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID561242Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID285096Antimicrobial activity against viridans group Streptococcus intermedius at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID566580Antimicrobial activity against Staphylococcus lentus ATCC 29070 by conventional agar-dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation.
AID1710578Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1139119Volume of distribution at steady state in rat at 2.8 to 9.5 mg/kg, iv2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID575149Antimicrobial activity against vancomycin-resistant Staphylococcus aureus VRS3 by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID545802Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 planktonic cells by broth microdilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID285371Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID561240Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as resistant isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID245647Minimum inhibitory concentration against methicillin, ciprofloxacin, rifampin, imipenem-resistant Staphylococcus aureus UC12673; Range is 2-4 ug/mL2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Conformational constraint in oxazolidinone antibacterials. Synthesis and structure-activity studies of (azabicyclo[3.1.0]hexylphenyl)oxazolidinones.
AID499142Ratio of fAUC to MIC in Staphylococcus aureus OC 4172 infected sc dosed SKH1 mouse2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID577092Ratio of AUC (0 to 24 hrs) to MIC for Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID745405Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID1832939Antibacterial activity against Staphylococcus aureus NCTC 13616 assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID576886Ratio of Cmax to MIC for 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1609274Bactericidal activity against methicilline-resistant Staphylococcus aureus NRS385 USA500 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID745401Antibacterial activity against Streptococcus pneumoniae SR26207 clinical isolate assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID590059Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Discovery of torezolid as a novel 5-hydroxymethyl-oxazolidinone antibacterial agent.
AID595023Antibacterial activity against Staphylococcus aureus ATCC 259232011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
AID520766Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as improvement in extent of bone remodeling at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 6 post2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID467840Antibacterial activity against Streptococcus pyogenes after 24 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
AID475007Antibacterial activity against Escherichia coli LCB0012 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID1434682Anti-bacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3635 by 2-fold microtiter broth dilution method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Cadiolides J-M, antibacterial polyphenyl butenolides from the Korean tunicate Pseudodistoma antinboja.
AID475004Antibacterial activity against Enterococcus faecium LCB0009 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID115955Minimum inhibitory concentration in mice against antimicrobial activity in methicillin-resistant Staphylococcus pneumoniae (PISP 49619).2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids.
AID520767Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as improvement in rate of bone reconstruction at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 8 po2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID1609278Bactericidal activity against methicilline-sensitive Staphylococcus aureus NRS-107 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID206822Antibacterial activity against Staphylococcus pyogenes2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID520018Antimicrobial activity against Staphylococcus aureus pL1502008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID576674Bactericidal activity against 48 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID645042Antibacterial activity against methicillin-resistant glycopeptide-intermediate Staphylococcus aureus Mu50 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID429065Antiplasmodial activity after 96 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum.
AID710151Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria.
AID558478Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 509 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID560370Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 by broth dilution method in presence of 4% HSA2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID581040Inhibition of ribosomal activity in Escherichia coli S30 by coupled transcription/translation assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID410340Antimicrobial activity against Haemophilus influenzae 895 (AcrB-KO) by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID283632Antimicrobial activity against Staphylococcus aureus RN42202007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID1609271Bactericidal activity against vancomycin-resistant Staphylococcus aureus 12 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1400756Hemolytic activity in human RBC at 200 uM after 1 hr relative to control2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID208149Minimum inhibitory concentration Streptococcus pneumoniae UC99121998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID552835Antibacterial activity against multidrug-resistant Enterococcus faecium2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID283627Antimicrobial activity against methicillin-resistant Staphylococcus aureus Ho 4280-0256 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID542899fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 400 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1744564Antibacterial activity against methicillin resistant Staphylococcus aureus assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID348604Antibacterial activity against vancomycin-resistant Enterococcus faecium 2 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID1167732Antimicrobial activity against Streptococcus pyogenes by broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
AID205577Antibacterial activity against Staphylococcus epidermidis UC30031UC1998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID326293Antibacterial activity against methicillin-resistant Staphylococcus aureus 5098 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID565229Antimicrobial activity against Mycobacterium chelonae ATCC 35752 harboring pZS01 carrying mspA gene by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID573150Antibacterial activity against vancomycin-susceptible Enterococcus faecalis assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID542697fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID574063Cmax in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID206436In vitro antibacterial activity against ciprofloxacin and oxazolidinone Linezolid resistant Staphylococcus aureus ATCC 29213 (Saul)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID12298Half life of compound (10 mg/kg) after iv administration was determined in Sprague-Dawley rat2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID352931Antibacterial activity against vancomycin-resistant Enterococcus faecium after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID560367Antimicrobial activity against vancomycin-resistant Enterococcus faecium 1059060 by broth dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1375990Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring cyd deletion mutant measured after 2 weeks by microplate alamar blue assay2016MedChemComm, Nov-01, Volume: 7, Issue:11
SAR and identification of 2-(quinolin-4-yloxy)acetamides as
AID260741Antibacterial activity against Enterococcus faecalis 292122006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID1493803Antibacterial activity against Staphylococcus aureus USA400 NRS123 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID285386Area under population analysis profile for heteroresistant vancomycin-intermediate Staphylococcus aureus Mu3 using in vitro PK/PD model relative to growth control with 120 mg/24 hrs continuous infusion regimen after 72 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID533953Antimicrobial activity against Listeria monocytogenes EGD after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID284941Antimicrobial activity against Aerococcus spp. at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID574553Decrease in PSMbeta1 levels in Staphylococcus aureus Sanger 252 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID630561Antibacterial activity against linezolid-resistant Enterococcus faecalis after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID1271210Metabolic stability in mouse liver microsomes after 30 mins by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID528846Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID245136Minimum inhibitory concentration against Staphylococcus aureus ATCC 13709; value ranges from 3-6 uM2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID1553368Antibacterial activity against Staphylococcus aureus JC9213 by CLSI based broth dilution assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1594068Antibacterial activity against Escherichia coli assessed as reduction in bacterial cell viability incubated for 20 to 24 hrs by REMA method2019Bioorganic & medicinal chemistry, 06-15, Volume: 27, Issue:12
Design, synthesis, in-silico studies and biological screening of quinazolinone analogues as potential antibacterial agents against MRSA.
AID522911Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus isolate 1766 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID528693Antibacterial activity against multidrug resistant Streptococcus pneumoniae MED 1090 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1778660Bactericidal activity against penicillin-resistant Staphylococcus aureus measured after 24 hrs by CLSI protocol based method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID560830Ratio of AUC (0 to 12 hrs) in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 5 days to MIC for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID525147Antimicrobial activity against linezolid-resistant Staphylococcus aureus isolate 004-737X expressing cfr and ermA gene isolated from paraplegic patient by disk diffusion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID1308237Antibacterial activity against Enterococcus faecium NCTC 7171 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID283165Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2664 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID542698fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered as 6 divided doses every 4 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID85780In vitro antibacterial activity against Haemophilia influenzae strains 30063 and ATCC 31517 (HI); range is 8-162003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID284976Antimicrobial activity against Corynebacterium striatum at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1609273Bactericidal activity against methicilline-resistant Staphylococcus aureus NRS386 USA700 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID555309Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 197 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1407932Antibacterial activity against methicillin-resistant Staphylococcus aureus FQ-R after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID1539449Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 10 after 18 to 20 hrs in aerobic condition by CLSI-based broth microdilution assay
AID523792Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID558084Antimicrobial activity against Mycoplasma genitalium isolated from human by two fold serial dilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
AID1481713Potentiation of imipenem-induced antibacterial activity against methicillin-resistant Staphylococcus aureus COL MB 5393 infected in neutropenic balb/c mouse assessed as reduction in bacterial burden in kidney at 10 mg/kg, sc administered three times per d2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
AID577143Volume of distribution at steady state in two-compartment pharmacokinetic/pharmacodynamic model at 400 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1395980Induction of biofilm eradication of methicillin-resistant Staphylococcus aureus BAA-1707 after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID483193Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by microbroth dilution technique2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID1852695Antibacterial activity against Escherichia coli SQ110 DTC C2610A incubated for 24 hrs by twofold serial dilution method
AID208944In vitro minimum inhibitory concentration (MIC) against Streptococcus pneumoniae UC99122003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID1596557Antibacterial activity against Listeria monocytogenes ATCC 19111 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID544828Antimicrobial activity against Staphylococcus epidermidis Xen 43 biofilm assessed as log10 CFU/cm'2 in bacterial count2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID565017Antimicrobial activity against methicillin-susceptible coagulase-negative Staphylococcus sciuri assessed as susceptible isolates after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro activities of panduratin A against clinical Staphylococcus strains.
AID567451Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK3 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID1861519Antibacterial activity against methicillin-resistant Staphylococcus aureus Sta-032 incubated for 18 hrs by CLSI protocol based two-fold serial agar dilution method2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID1591541Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 incubated for 24 hrs by CLSI protocol based broth microdilution method2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID261062Antibacterial activity against Streptococcus pneumoniae SVI SP-32006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Conformational constraint in oxazolidinone antibacterials. Part 2: Synthesis and structure-activity studies of oxa-, aza-, and thiabicyclo[3.1.0]hexylphenyl oxazolidinones.
AID323808Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse with peritonitis at 100 mg/kg, po after 5 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID1409853Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid administered at 12 hrs prior to bacterial infection dosed at 12 intervals for 4.52018ACS medicinal chemistry letters, Mar-08, Volume: 9, Issue:3
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant
AID287266Antimicrobial activity against Moraxella catarrhalis2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID562187Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 after 50 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1446762Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRSA10 after 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID522899Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 1016 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID1400751Antibiofilm activity against methicillin-resistant Staphylococcus aureus isolate 2 after 24 hrs by calgary biofilm device-based assay2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID523832Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 256 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID559559Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP7 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID558514Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1435923Antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 18 to 20 hrs by broth microdilution method2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID287265Antimicrobial activity against Haemophilus influenzae2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID1609272Bactericidal activity against vancomycin-resistant Staphylococcus aureus 10 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID424762Antibacterial activity against ampicillin-sensitive Staphylococcus haemolyticus CL8544 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID637973Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID1197122Antibacterial activity against Staphylococcus haemolyticus ATCC 29970 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID283619Antimicrobial activity against Enterococcus faecium 18 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID297122Antibacterial activity against methicillin-resistant Staphylococcus aureus Mu50 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID375939Antibacterial activity against methicillin-resistant Staphylococcus aureus 78-13607A after 24 hrs by broth microdilution method2006Journal of natural products, Apr, Volume: 69, Issue:4
Antibacterial, partially acetylated oligorhamnosides from Cleistopholis patens.
AID1205587Inhibition of Escherichia coli switch region of RNA polymerase after 1 hr by transcription-coupled translation assay2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID576671Bactericidal activity against 13 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1205589Partition coefficient, log D of the compound at pH 7.4 by shake flask method2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID244932Minimal inhibitory concentration against Klebsiella pneumoniae ATCC 153802004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID127519In vitro antibacterial activity against Moraxella catarrhalis strains 30607 and 30603 (MC); range is 4-82003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID210055Compound was evaluated for minimum inhibitory concentration against Streptococcus pneumoniae 9757 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID1873887Induction of drug resistance in Escherichia coli ATCC 25922 assessed as increase in MIC measured after 30 passages by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID559802Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at 4 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID68056In vitro minimum inhibitory concentration (MIC) against Enterococcus faecalis UC92172003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID370039Fraction unbound in Staphylococcus aureus-infected mouse localized thigh infection model plasma at 25 mg/kg2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1907629Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC2858 incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID206210In vitro minimum inhibitory concentration (MIC) against Staphylococcus epidermidis UC120842003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID533392Antimicrobial activity against Clostridium perfringens assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID285125Antimicrobial activity against viridans group Streptococcus salivarius at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID567449Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK1 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID576416Apparent volume of distribution in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID523831Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 128 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID520520AUC in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model at 60 mg/kg, po after 24 hrs2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID369674Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as mortality at 12.5 mg/kg/day, po administered within 15 mins of infection measured after 48 hrs by organ burden assay relative to control2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID560502Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gz06051 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1553386Inhibition of SDH-A (unknown origin) by ELISA2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID93890Minimum inhibitory concentration against Klebsiella pneumoniae ATCC 100312004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID499115Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected immunocompromized SKH1 mouse assessed as lesion volume at 6.2 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1535 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1676979Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 assessed as reduction in microbial growth after 48 hrs by CLSI based broth microdilution method
AID533986Bacteriostatic activity against linezolid-susceptible Staphylococcus aureus SA040 infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID283634Antimicrobial activity against Staphylococcus aureus RN4220 with 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID523797Antimicrobial activity against linezolid-resistant coagulase-negative Staphylococcus by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID759694Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 assessed as growth inhibition after 18 to 24 hrs by broth microdilution method2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID285078Antimicrobial activity against viridans group Streptococcus bovis at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID292608Antimicrobial activity against methicillin-resistant Staphylococcus aureus 33 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID533939Antimicrobial activity against linezolid-resistant Staphylococcus aureus 480 harboring G2447U in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID541083Cmax in cage fluid of Albino guiena pig at 25 mg/kg, ip after 3 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID574064Cmax in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID528702Antibacterial activity against Streptococcus constellatus clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID1704211Antibacterial activity against Methicillin-resistant Staphylococcus aureus KU602020European journal of medicinal chemistry, Nov-15, Volume: 2061,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
AID1710572Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID308730Antibacterial activity against Heamophilus influenzae HI3542 by microbroth method2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID211460Inhibitory activity against Escherichia coli Topoisomerase IV in relaxation assay; Not tested2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID318363Cytotoxicity against human HeLa cells by MTT assay2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID1519267Antibacterial activity agianst methicillin-sensitive Staphylococcus aureus clinical isolates2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID1350033Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 4 incubated overnight by agar dilution method2018Journal of natural products, 02-23, Volume: 81, Issue:2
Biomimetic Stereoselective Sulfa-Michael Addition Leads to Platensimycin and Platencin Sulfur Analogues against Methicillin-Resistant Staphylococcus aureus.
AID1451756Antibacterial activity against Staphylococcus aureus Newman infected in BALB/c mouse assessed as reduction of bacterial burden in heart 0.4 mg, ip bid for 4.5 days administered 6 hrs post bacterial infection measured 108 hrs post infection relative to con2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID535034Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-126 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID67729Minimum inhibitory concentration (MIC) against Enterococcus faecalis ATCC 292122004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID1407928Antibacterial activity against Haemophilus influenzae ATCC 49247 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID729215Antibacterial activity against linezolid-resistant Enterococcus faecium after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID520236Antimicrobial activity against Enterococcus faecium A63492008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1180573Antimicrobial activity against 2 times drug resistance selected Staphylococcus aureus ARC1692-1F by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1311367Antibacterial activity against Mycobacterium tuberculosis 115R measured after 14 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID396033Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pBGS18 plasmid by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID533660Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid VGA2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID326520T>MIC in Enterococcus faecalis infected Wistar rat at 600 mg, po two consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID775544Antibacterial activity against Haemophilus influenzae SR27914 clinical isolate assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID1574842Antibacterial activity against clinical isolates of vancomycin-resistant Enterococcus faecium by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID576893Ratio of Cmax to MIC for 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID576656Bactericidal activity against 48 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID577128Terminal half-life in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID475005Antibacterial activity against Escherichia coli LCB0010 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID1853631Inhibition of protein synthesis in Staphylococcus aureus ATCC 29213 at 8 times MIC preincubated for 30 mins followed by [3H]-leucine and measured after 40 mins by [3H]-leucine incorporation based beta scintillation counter analysis2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
Design, synthesis, and antibacterial activity of
AID577113ABBC (0 to 24 hrs) in Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID125103Antibacterial activity against Moraxella catarrhalis2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1596894Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 18 hrs by broth microdilution assay
AID544830Antimicrobial activity against Staphylococcus epidermidis Xen 43 biofilm assessed as log10 CFU/cm'2 in bacterial count in presence of 200 microamperes of electric current by bioelectric effect assay2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID572485Antimicrobial activity against methicillin-resistant Staphylococcus aureus NB01021 infected in po dosed BALB/c mouse administered 0, 4, 23 hrs post infection2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID1778662Bactericidal activity against penicillin-susceptible Bacillus pumilus CMCC 63202 measured after 24 hrs by CLSI protocol based method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID763987Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID555743Antibacterial activity against methicillin-resistant, vancomycin-intermediate coagulase-negative Staphylococcus epidermidis 225 by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID134115Protective dose of orally administered compound against intraperitoneally-induced septicaemia model (Enterococci faecium D3HT7 strain) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID1400025Selectivity ratio of MIC for antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv harboring pFCA-luxAB to MIC100 for antibacterial activity against replicating Mycobacterium tuberculosis H37Rv2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1168022Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 16115 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID562246Antibacterial activity against Staphylococcus epidermidis 1653059 harboring rplC G469A/C470G, L3 Ala157Arg and 23S rRNA G2447T mutant by CLSI broth microdilution assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutations in ribosomal protein L3 are associated with oxazolidinone resistance in staphylococci of clinical origin.
AID1059061Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate OM584 by liquid microdilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-anti-MRSA activity relationship of macrocyclic bis(bibenzyl) derivatives.
AID373809Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID552863Antibacterial activity against Streptococcus pyogenes infected in po dosed in vivo acute model administered bid for 1 day2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
AID609058Antibacterial activity against Escherichia coli ATCC 8739 at 1 mg/ml after 24 hrs by agar-well diffusion technique2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A regioselective synthesis of some new pyrazol-1'-ylpyrazolo[1,5-a]pyrimidines in aqueous medium and their evaluation as antimicrobial agents.
AID205897Minimum inhibitory concentration against Staphylococcus epidermidis MTCC 1552004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID576669Bactericidal activity against 12 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1778100Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as bacterial growth inhibition after 18 hrs by broth microdilution method
AID533017Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-1 assessed as inhibition of bacterial growth in Mueller-Hinton broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID555316Antibacterial activity against methicillin-susceptible, vancomycin-intermediate Staphylococcus aureus 505 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID528706Antibacterial activity against Streptococcus agalactiae group B clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID323790Antibacterial activity against methicillin-resistant Staphylococcus aureus Xen1 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po within 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID285086Antimicrobial activity against viridans group Streptococcus constellatus at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1446755Bactericidal activity against methicillin-resistant Staphylococcus aureus USA100 NRS382 clinical isolate after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1680061Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 5 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID66574Antibacterial activity was determined against clinically isolated vancomycin-B resistant enterococci (VRE) strains (10 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID284947Antimicrobial activity against Bacillus spp. at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1126491Antimicrobial activity against Haemophilus influenzae ATCC 31517 MMSA2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID1271226Antibacterial activity against pencillin-resistant erm+ve Streptococcus pneumoniae ATCC 700904 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID520019Antimicrobial activity against Staphylococcus aureus pLXM1 harboring cfr gene2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID303918Antibacterial activity against methicillin-resistant Staphylococcus aureus 562 infected orally dosed Swiss albino mouse after 7 days2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID576407Mean residence time in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID370030Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as renal sterilization at 25 mg/kg/day, po administered 15 mins postinfection2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID373318Antibacterial activity against Enterococcus faecalis ATCC 29212 after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID1653062Antibacterial activity against Staphylococcus epidermidis2019European journal of medicinal chemistry, Feb-15, Volume: 164Isatin derivatives and their anti-bacterial activities.
AID763978Antibacterial activity against Moraxella catarrhalis ATCC 8176 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID1596571Bactericidal activity against Cephalosporin resistant Streptococcus pneumoniae ATCC 51916 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilut2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID370019Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 25 mg/kg/day, iv administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burden2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID66576Antibacterial activity was determined against clinically isolated vancomycin-A resistant enterococci (VRE) strains (33 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1197131Antibacterial activity against vancomycin-resistant Enterococcus faecium 119-39A clinical isolate after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID268862Antibacterial activity against Staphylococcus aureus ATCC 499512006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis of novel tricyclic oxazolidinones by a tandem SN2 and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid.
AID577105AUBC (0 to 24 hrs) in Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID287260Antimicrobial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID745374Inhibition of MAO-A in rat forebrain using [14C]5-HT as substrate at 30 uM incubated for 20 mins prior to substrate addition measured after 5 mins by liquid scintillation counting analysis relative to control2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID1647980Antibacterial activity against Escherichia coli by resazurin dye based microdilution method2020Journal of natural products, 02-28, Volume: 83, Issue:2
The Isolation of Pyrroloformamide Congeners and Characterization of Their Biosynthetic Gene Cluster.
AID304006Effect on hematology in Sprague-Dawley rat assessed as increase in hematocrit at 200 mg/kg/day, po after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID373989Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 after 20 passages with daptomycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID573137Antibacterial activity against erythromycin-susceptible Streptococcus agalactiae assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID134124Protective dose of subcutaneously administered compound against intraperitoneally-induced septicaemia model (Staphylococcus pneumoniae PW3 strain) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID577109AUBC (0 to 24 hrs) in Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID763948Antibacterial activity against Moraxella catarrhalis clinical isolate 3447 after 18 hrs by NCCLS agar dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and antibacterial activities of N-substituted-glycinyl 1H-1,2,3-triazolyl oxazolidinones.
AID349314Antibacterial activity against Haemophilus influenzae clinical isolate after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID285139Antimicrobial activity against viridans group Streptococcus vestibularis at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID541052Ratio of AUC (0 to 24 hrs) to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 50 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1180586Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC2381-3F to MIC for Staphylococcus aureus ARC23812014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID533006Antibacterial activity against vancomycin-intermediate Staphylococcus aureus 99/3759-V phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID345138Antimicrobial activity against Haemophilus influenzae RD1 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
AID292902Antimicrobial activity against streptococcus pneumoniae by broth dilution method2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.
AID1190640Antibacterial activity against Escherichia coli NCIM-2256 incubated for 24 hrs by two fold serial dilution method2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Biofilm inhibition of linezolid-like Schiff bases: synthesis, biological activity, molecular docking and in silico ADME prediction.
AID630563Antibacterial activity against Staphylococcus aureus ATCC 19636 infected in mouse systemic infection model administered orally 1 hour after infection measured 48 hrs of post-treatment2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID687493Oral bioavailability in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID1126488Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis ATCC 292122014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID1594386Cmax in human at 625 mg, iv2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID567450Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK2 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID29429Oral bioavailability in rat (Sprague-Dawley) (male) (dose 25 mg/kg p.o.)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID370026Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as reduction in log number of CFU at 3.12 mg/kg/day, iv administered within 15 mins of infection measured after 48 hrs by organ burden assay 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID1472763In vivo anti-virulence activity against Staphylococcus aureus Mu50 infected in BALB/c mouse model assessed as reduction in bacterial load in kidney at 0.4 mg bid for 4.5 days administered orally 6 hrs post infection by serial dilution method relative to c2018Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
AID319986Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 122022008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID1076820Antitubercular activity against extensive drug-resistant Mycobacterium tuberculosis clinical isolate 5 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID285089Antimicrobial activity against viridans group Streptococcus gordonii at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID392200Antibacterial activity against Escherichia coli by transcription-translation assay2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents.
AID67086Antibacterial activity against Enterococcus faecalis UC92171998Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
AID458453Antimicrobial activity against methicillin-resistant Staphylococcus aureus 143/93 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID245424Minimum inhibitory concentration against methicillin resistant Staphylococcus aureus (strain A27223) in presence of 50% calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID575143Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolate NRS70 by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID1501369Bactericidal activity against vancomycin-resistant Staphylococcus aureus isolate 10 incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID535027Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-27 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID576437Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 MutS2 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusio2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1877887Antibacterial activity against penicillin-resistant Streptococcus pneumoniae DSM-11865 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID710137Antibacterial activity against methicillin-resistant Staphylococcus epidermidis2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
From triclosan toward the clinic: discovery of nonbiocidal, potent FabI inhibitors for the treatment of resistant bacteria.
AID520222Antimicrobial activity against Enterococcus faecium A96502008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1474208Bactericidal activity against Enterococcus faecium after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1539445Antibacterial activity against linezolid-resistant/Methicillin-resistant Staphylococcus aureus NRS119 clinical isolates after 18 to 20 hrs in aerobic condition by CLSI protocol based broth microdilution assay
AID260740Antibacterial activity against methicillin resistant Staphylococcus aureus MRSA 10942006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID283168Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5256 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID370036Antibacterial activity against methicillin-resistant Staphylococcus aureus COL infected in po dosed DBA/2 mouse localized infection model assessed as log reduction in CFU per gram of thigh at 10 mg/kg, iv administered 2 hrs postinfection thrice daily for 2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID285058Antimicrobial activity against beta hemolytic Streptococcus group C at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285098Antimicrobial activity against viridans group Streptococcus intermedius at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID374018Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID284999Antimicrobial activity against Enterococcus durans at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID532805Antibacterial activity against vancomycin-susceptible Staphylococcus aureus LIM2 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID576397Tmax in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1400054Bactericidal activity against Klebsiella pneumoniae ATCC 12019 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID560375Selectivity ratio of MIC for Enterococcus faecium ATCC 51559 in presence of 4% HSA to MIC for Enterococcus faecium ATCC 515592009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1687310Antibacterial activity against Klebsiella pneumoniae ATCC 1706 incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID1584838Antibacterial activity against vancomycin-resistant Enterococcus faecalis JH2-2::C1 after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID574546Antimicrobial activity against community-associated methicillin-resistant Staphylococcus aureus Sanger 2522010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID283641Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID1904080Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 433002022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID439895Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID542712fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered as 6 divided doses every 4 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID729222Antibacterial activity against methicillin-resistant Staphylococcus epidermidis after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID1770360Ratio of MBC to MIC against penicillin-susceptible Bacillus pumilus CMCC632022021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID576679Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID542690fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 300 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1168026Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 18906 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1395679Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS386 after 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1778091Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth incubated for 18 hrs by broth microdilution method
AID1435933Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRSA4 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID285084Antimicrobial activity against viridans group Streptococcus constellatus at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1519272Antibacterial activity agianst methicillin-sensitive Staphylococcus aureus2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID308726Antibacterial activity against Staphylococcus aureus UC76 SA1 by micro-broth method2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID1710584Antibacterial activity against vancomycin-resistant Staphylococcus aureus 10 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID575100Antimicrobial activity against Streptococcus pneumoniae serotype 22F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1361050Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-1707 after 16 to 18 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Halogenated quinolines bearing polar functionality at the 2-position: Identification of new antibacterial agents with enhanced activity against Staphylococcus epidermidis.
AID560806AUC (0 to 24 hrs) at steady state in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1596551Antibacterial activity against methicillin resistant Staphylococcus epidermidis NRS101 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID207682Minimum inhibitory concentration (MIC) against methicillin-resistant Staphylococcus aureus (MRSA) OC28782004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
AID520483Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 30 mg/kg, sc administered every 12 hrs for 4 days measured on week 4 postinfection (Rvb = 2.84 +/- 0.30 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID424767Antibacterial activity against vancomycin, linezolid-resistant Enterococcus faecium CL5791 after 20 hrs by twofold serial broth dilution method in presence of 50% human serum2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID1649279Antibacterial activity against Staphylococcus aureus SMITH assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID1649289Antibacterial activity against Vancomycin-resistant Enterococcus faecium SR23598 (VanB) assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID560576Bactericidal activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 expressing vanB gene assessed as change in bacterial count at 16 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID569347Antibacterial activity against penicillin-resistant Streptococcus pneumoniae by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID575076Antimicrobial activity against Streptococcus pneumoniae serotype 19A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1446763Bactericidal activity against vancomycin-resistant Staphylococcus aureus VRSA10 after 18 hrs by broth microdilution method2017European journal of medicinal chemistry, Apr-21, Volume: 130Diphenylurea derivatives for combating methicillin- and vancomycin-resistant Staphylococcus aureus.
AID541044Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 25 mg/kg after measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID558493Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID368291Bactericidal activity against vancomycin-intermediate Staphylococcus aureus in rabbit endocarditis model assessed as growth inhibition at 58 mg/kg infused every 12 hrs for 4 days measured after 48 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID542911Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing at 300 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID576862Bactericidal activity against 24 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 800 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID604292Antibacterial activity against vancomycin-resistant Enterococcus faecium after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID523788Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 4 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID283395Antimicrobial activity against Nocardia nova after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID125104Inhibitory activity against Moraxella catarrhalis1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1877886Antibacterial activity against Streptococcus pneumoniae DSM-20566 assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID577133AUC in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID645047Antibacterial activity against Serratia marcescens Mel 522 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID726199Antibacterial activity against methicillin-resistant coagulase negative Staphylococcus by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID285385Area under population analysis profile for methicillin-resistant Staphylococcus aureus using in vitro PK/PD model relative to growth control with 120 mg/24 hrs continuous infusion regimen after 72 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID285010Antimicrobial activity against Enterococcus hirae at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID41262In vitro antibacterial activity against Bacteroides fragilis strain ATCC 252851996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1197121Antibacterial activity against Staphylococcus epidermidis ATCC 35547 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID349318Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID373998Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 Hershey after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID255571In vitro minimum inhibitory concentration against Enterococcus faecium ATCC 29212 after incubation in air at 35 degree C for 24 hr using agar dilution method2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID558479Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 10 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID582984Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0649 harboring MLST sequence type ST17 and pulsotype B expressing vanA gene cluster isolated from exudate of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID562621Antimicrobial activity against vancomycin-resistant Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1414198Selectivity ratio of MBC for Staphylococcus aureus ATCC 25923 to MIC for Staphylococcus aureus ATCC 259232018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID633448Bacteriostatic activity against Staphylococcus aureus ATCC 01001 infected in thigh of CD1 mouse assessed as prevention of colony formation at 80 mg/kg, po administered 2 hrs post infection measured after 24 hrs2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.
AID511430Antimicrobial activity against Clostridium perfringens LFM1 assessed as susceptibility breakpoint by DANMAP method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Resistance to linezolid in a porcine Clostridium perfringens strain carrying a mutation in the rplD gene encoding the ribosomal protein L4.
AID475003Antibacterial activity against vancomycin-resistant Enterococcus faecium LCB0008 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID576672Bactericidal activity against 14 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID499110Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected immunocompromized SKH1 mouse assessed as lesion volume at 1.6 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1181 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID535258Antimicrobial activity against vancomycin resistant Staphylococcus aureus VRS-6 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID563323Antibacterial activity against vancomycin-susceptible Enterococcus faecalis EF 12704 assessed as log reduction in bacterial count at 12 mg/l after 24 hrs by time kill assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID1861524Antibacterial activity against Linezolid-resistant Staphylococcus aureus Sta-5060 incubated for 18 hrs by CLSI protocol based two-fold serial agar dilution method2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID585164Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA G2576U mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID565487Bactericidal activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by M26-A method in presence of 50% human plasma2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID285018Antimicrobial activity against Enterococcus raffinosus at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID458452Antimicrobial activity against wild type Staphylococcus aureus SG 511 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID542689fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 200 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID753131Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis assessed as growth inhibition after 2 to 3 weeks by broth microdilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID1770353Antibacterial activity against Vancomycin-resistant Enterococcus faecalis ATCC 51299 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID560813AUC (0 to 24 hrs) in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID569342Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID1689207Antibacterial activity against Escherichia coli BW25113 assessed as reduction in bacterial growth by CLSI based broth microdilution method2020European journal of medicinal chemistry, Mar-01, Volume: 189Oxadiazolylthiazoles as novel and selective antifungal agents.
AID1873909Antibacterial activity against Klebsiella pneumoniae ATCC 13883 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID532790Antibacterial activity against vancomycin-intermediate Staphylococcus aureus 28160 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID759693Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 assessed as growth inhibition after 18 to 24 hrs by broth microdilution method2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID311475Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID499114Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected immunocompromized SKH1 mouse assessed as lesion volume at 1.6 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1535 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID726195Antibacterial activity against Streptococcus agalactiae ATCC 2901 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID285104Antimicrobial activity against viridans group Streptococcus mitis at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID244828Minimum inhibitory concentration against Enterococcus faecalis ATCC 292122004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
AID308490Antibacterial activity against Moraxella catarrhalis BC-35312007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
AID558474Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID581671Antibacterial activity against normal phenotype Staphylococcus aureus in cation-adjusted MH 2 broth at pH 5.5 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1519042Antibacterial activity against clinical isolates of linezolid-resistant Enterococcus faecalis assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID348861Antibacterial activity against vancomycin-resistant Enterococcus 2 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID522918Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-positive Staphylococcus aureus isolate 1468 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID284948Antimicrobial activity against Bacillus spp. at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID285068Antimicrobial activity against beta hemolytic Streptococci group G at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1594390Volume of distribution in human at 625 mg, iv2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1312951Bactericidal activity against vancomycin-resistant Staphylococcus aureus 10 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID374020Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID734708Antibacterial activity against Staphylococcus MLS-16 MTCC 2940 after 24 hrs by agar dilution method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID519084Antimicrobial activity against Escherichia coli KM75-84 harboring Gly153Arg mutation in rplC gene by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID559782Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at 0.25 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID285008Antimicrobial activity against Enterococcus hirae at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID561236Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as resistant isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID559370Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP3 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1574837Antibacterial activity against methicillin-sensitive Staphylococcus aureus by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID1609263Bactericidal activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID283158Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2492 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID542710fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID562164Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID574079Ratio of fAUC (24 hrs) for Methicillin-susceptible Staphylococcus aureus ATCC 13709 infected sc dosed mouse to MIC for Methicillin-susceptible Staphylococcus aureus ATCC 13702009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID574081Ratio of fAUC (24 hrs) for community-associated methicillin-resistant Staphylococcus aureus OC8525 infected po dosed mouse to MIC for community-associated methicillin-resistant Staphylococcus aureus OC85252009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID577120Cmax in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1059062Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate OM481 by liquid microdilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-anti-MRSA activity relationship of macrocyclic bis(bibenzyl) derivatives.
AID1609259Bactericidal activity against methicillin-resistant Streptococcus pneumoniae ATCC 700677 incubated for 18 to 20 hrs followed by replating on tryptic soy agar plate and further incubated for 18 to 24 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID574070Tmax in CF-1 mouse serum at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID125078In vitro antibacterial activity against Moraxella catarrhalis 30607 (b-lactamase+).2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID1853478Bactericidal activity against persister methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as reduction in colony forming unit at 1 x MIC incubated for 18 to 24 hrs by Time-kill analysis2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
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AID1493813Antibacterial activity against Pseudomonas aeruginosa ATCC 15442 after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID567569Antimicrobial activity against Staphylococcus aureus RN42202010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
First report of the multidrug resistance gene cfr and the phenicol resistance gene fexA in a Bacillus strain from swine feces.
AID1197130Antibacterial activity against vancomycin-susceptible Enterococcus faecium 119-39A clinical isolate after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID555502Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 057 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID604291Antibacterial activity against Enterococcus faecium ATCC 19434 after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID575148Antimicrobial activity against vancomycin-resistant Staphylococcus aureus VRS2 by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID1680051Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 5 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID533016Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1 assessed as inhibition of bacterial growth in brain heart infusion broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID717208Antimicrobial activity against methicillin-sensitive Staphylococcus aureus CCARM 0027 incubated for 24 hrs by microtiter broth dilution method2012Journal of natural products, Dec-28, Volume: 75, Issue:12
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
AID1269332Half life in mouse liver microsomes2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
AID573862Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 6301 after 16 to 20 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID523811Antimicrobial activity against linezolid-susceptible coagulase-negative Staphylococcus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID584971Antibacterial activity against Mycobacterium smegmatis SZ558 after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID577125Residual concentration at the end of the administration interval in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID209464In vitro antibacterial activity against Streptococcus pyogenes C6003 (S.p.2).1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles.
AID1832940Antibacterial activity against Staphylococcus aureus ATCC 9144 assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID560578Bactericidal activity against vancomycin-resistant Enterococcus faecium 1119175 expressing vanB gene assessed as change in bacterial count at 16 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1501356Antibacterial activity against Staphylococcus aureus RN4220 NRS107 after 20 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID1692903Antibacterial activity against linezolid-resistant Enterococcus faecalis2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID387454Antibacterial activity against linezolid-resistant Enterococcus faecalis DRCC 6322008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID1861523Antibacterial activity against Linezolid-resistant Staphylococcus aureus Sta-5059 incubated for 18 hrs by CLSI protocol based two-fold serial agar dilution method2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID560373Antimicrobial activity against vancomycin-resistant Enterococcus faecium 1059060 by broth dilution method in presence of 4% HSA2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1390462Antibacterial activity against Staphylococcus aureus ATCC 292132018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID577118Cmax in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID528840Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1594388Clearance in human at 625 mg, iv2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID523800Antimicrobial activity against linezolid-susceptible Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1311358Antibacterial activity against Acinetobacter baumannii 6M-1b measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID375938Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 24 hrs by broth microdilution method2006Journal of natural products, Apr, Volume: 69, Issue:4
Antibacterial, partially acetylated oligorhamnosides from Cleistopholis patens.
AID410220Antibacterial activity against Escherichia coli LCB0011 by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID524720Antibacterial activity against linezolid-resistant Enterococcus faecalis ATCC 29212 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro antibacterial activity of CE-156811, a novel analog derived from hygromycin A.
AID1594368Antibacterial activity against Enterobacter cloacae BAA1134 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1271213Plasma protein binding in human2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID581012Antimicrobial activity against Staphylococcus aureus ATCC 25923 by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID1168004Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 23/240 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID210056Compound was evaluated for minimum inhibitory concentration against Streptococcus pneumoniae 9798 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID498896Tmax in immunocompetent SKH1 mouse plasma at 50 mg/kg, po2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID132799compound was tested against Staphylococcus aureus UC9213 the vancomycin administered (sc) in mouse positive control expressed as ED50 values.1998Journal of medicinal chemistry, Sep-10, Volume: 41, Issue:19
Piperazinyl oxazolidinone antibacterial agents containing a pyridine, diazene, or triazene heteroaromatic ring.
AID1451765Antibacterial activity against Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as reduction of bacterial burden in heart at 0.4 mg, ip bid for 4.5 days treated 24 hrs prior to bacterial infection measured 108 hrs post infection relative to co2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.
AID405629Toxicity in rat liver mitochondria assessed as inhibition of mitochondrial protein synthesis2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID559770Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 4sy32 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1181167Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_1 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID560361Cmin in healthy human male at 600 mg, po every 12 hrs by LC/MS/MS analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1596567Bactericidal activity against methicillin resistant Staphylococcus epidermidis NRS101 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution 2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID542676fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 5000 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID574066fCmax in CF-1 mouse at 2 mg/kg, iv2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID541059Ratio of Cmax to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 25 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID573129Antibacterial activity against penicillin-resistant Streptococcus pneumoniae assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID734691Antibacterial activity against Bacillus subtilis MTCC 121 at 20 ug/ml after 24 hrs by disk diffusion method2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis, biological evaluation of new oxazolidino-sulfonamides as potential antimicrobial agents.
AID522820Antibacterial activity against vancomycin-susceptible Staphylococcus aureus after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID558725Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 510 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID574085Ratio of fAUC (24 hrs) for penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected sc dosed mouse to MIC for penicillin-susceptible Streptococcus pneumoniae ATCC 63012009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID245240In vitro minimum inhibitory concentration against Staphylococcus aureus (ATCC 25923 and 29213)2005Bioorganic & medicinal chemistry letters, Jun-15, Volume: 15, Issue:12
Synthesis and antibacterial activity of novel (un)substituted benzotriazolyl oxazolidinone derivatives.
AID562190Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID542387Antimicrobial activity against Staphylococcus aureus RN42202009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr.
AID1197115Antibacterial activity against mecA-positive, methicillin/oxacillin/tetracycline-resistant and vancomycin/linezolid susceptible Staphylococcus aureus ATCC 27660 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID1649293Antibacterial activity against Streptococcus pneumoniae tupelo (VTSP) assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID285545AUC (0-24 hrs) in mouse at 20 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID759690Antibacterial activity against methicillin-susceptible Staphylococcus aureus M923 assessed as growth inhibition after 18 to 24 hrs by broth microdilution method2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID517665Antimicrobial activity against Staphylococcus aureus FDA209P by standard serial-dilution technique2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID67397In vitro antibacterial activity against Enterococcus faecalis C6291 (E. f. 1)2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1744563Antibacterial activity against methicillin sensitive Staphylococcus aureus assessed as inhibition of bacterial growth measured after 16 hrs by agar plate dilution method2021ACS medicinal chemistry letters, Mar-11, Volume: 12, Issue:3
Semisynthesis and Biological Evaluation of Platencin Thioether Derivatives: Dual FabF and FabH Inhibitors against MRSA.
AID268861Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 335912006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis of novel tricyclic oxazolidinones by a tandem SN2 and SNAr reaction: SAR studies on conformationally constrained analogues of Linezolid.
AID523816Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 1 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID533981Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA238L infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID542386Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ST9 expressing cfr, fexA and erm(C) genes2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr.
AID1574841Antibacterial activity against clinical isolates of linezolid-resistant Enterococcus faecalis by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID1770362Ratio of MBC to MIC against methicilline-resistant Staphylococcus aureus ATCC433002021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID326510Tmax in Enterococcus faecalis infected Wistar rat at 600 mg, po two consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID284997Antimicrobial activity against Enterococcus durans at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID558731Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 50 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID604293Antibacterial activity against Escherichia coli J-53 after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID1329446Antibacterial activity against linezolid-resistant Mycobacterium tuberculosis H37Rv in hollow-fiber infection model assessed as reduction in bacterial burden at 858 mg, po at 24 hrs dose regimen measured after 3 weeks2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
From lead optimization to NDA approval for a new antimicrobial: Use of pre-clinical effect models and pharmacokinetic/pharmacodynamic mathematical modeling.
AID293840Antibacterial activity against vancomycin-resistant Enterococcus faecium VRA2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
A new class of anti-MRSA and anti-VRE agents: preparation and antibacterial activities of indole-containing compounds.
AID1474225Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC HM-968 assessed as ratio of MIC after and before 3 serial passages measured after 18 hrs by broth microdillution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1611119Antibacterial activity against methicillin-resistant Staphylococcus aureus CLSI-based double dilution method2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
AID729176Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 infected in po dosed systemic infection mouse model administered 1 hr post infection measured after 24 hrs2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID1887588Antibacterial activity against Staphylococcus aureus ATCC 29213 at 1 time MIC after 24 hrs by time kill assay2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID562593Antimicrobial activity against Enterococcus faecalis expressing VanA gene clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID326515Cmin in Enterococcus faecalis infected Wistar rat at 600 mg, po dosed consecutive administration every 12 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID207794Compound was evaluated for minimum inhibitory concentration against Staphylococcus aureus 966 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID745402Antibacterial activity against Moraxella catarrhalis SR26840 clinical isolate assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID287263Antimicrobial activity against vancomycin-sensitive Enterococcus by agar dilution method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Structure-antibacterial activity of arylcarbonyl- and arylsulfonyl-piperazine 5-triazolylmethyl oxazolidinones.
AID1197117Antibacterial activity against mecA-positive, ciprofloxacin/gentamicin/oxacillin/penicillin/linezolid-resistant Staphylococcus aureus NRS119 after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID368288Bactericidal activity against methicillin-resistant Staphylococcus aureus SA2 in rabbit endocarditis model assessed per gram of aortic vegetation at 58 mg/kg infused every 12 hrs for 4 days measured after 48 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID577122Tmax in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID285027Antimicrobial activity against Micrococcus luteus at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1474194Antibacterial activity against Escherichia coli 1411 after 18 to 22 hrs in absence of colistin by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID1609268Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID348862Antibacterial activity against vancomycin-resistant Enterococcus 3 after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID449617Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by agar dilution method2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID207026Antibacterial activity against methicillin susceptible Staphylococcus aureus (OC 4172) in presence of 50% mouse serum2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Novel piperidinyloxy oxazolidinone antimicrobial agents.
AID348601Antibacterial activity against Haemophilus influenzae after 18 to 20 hrs by agar dilution method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Synthesis and antibacterial activities of novel oxazolidinones having cyclic sulfonamide moieties.
AID1395706Bactericidal activity against methicillin-resistant Staphylococcus aureus NRS123 USA400 incubated fo 18 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID532802Antibacterial activity against vancomycin-susceptible Staphylococcus aureus AMC11094 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID528716Antibacterial activity against methicillin resistant Staphylococcus epidermidis clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID533385Antimicrobial activity against Clostridium difficile by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1594384Tmax in human at 625 mg, po2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID396032Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pAP3 plasmid containing Enterobacter aerogenes acrR gene by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID509630Antimicrobial activity against Staphylococcus aureus RN4220 by broth microdilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Identification of a plasmid-borne resistance gene cluster comprising the resistance genes erm(T), dfrK, and tet(L) in a porcine methicillin-resistant Staphylococcus aureus ST398 strain.
AID558476Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 measured on day 5 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1076831Antibacterial activity against methicillin-susceptible Staphylococcus aureus CMCC 26003 assessed as growth inhibition after 18 hrs by broth microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID542681fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 200 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID583894Antibacterial activity against vancomycin-intermediate Staphylococcus aureus isolate 440 (A6298) by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID1311362Antibacterial activity against Klebsiella pneumoniae ATCC 35657 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID285111Antimicrobial activity against viridans group Streptococcus mutans at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID326519T>MIC in Enterococcus faecalis infected Wistar rat at single administration of 600 mg, po2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Single-dose oral amoxicillin or linezolid for prophylaxis of experimental endocarditis due to vancomycin-susceptible and vancomycin-resistant Enterococcus faecalis.
AID295158Antibacterial activity against Enterococcus faecalis by microdilution broth method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID285548Plasma half life in mouse at 50 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID304002AUC (0 to 24 hrs) in Sprague-Dawley rat plasma at 200 mg/kg/day, po after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID1676980Antimicrobial activity against vancomycin-resistant Enterococcus faecium ATCC 51299 assessed as reduction in microbial growth after 48 hrs by CLSI based broth microdilution method
AID559553Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP5 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID206442In vitro antibacterial activity against methicillin resistant Staphylococcus aureus UC 12673 (MRSA); range is 2-42003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
AID1180575Antimicrobial activity against Staphylococcus aureus ARC2381 by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID255577In vitro minimum inhibitory concentration against vancomycin-resistant Enterococcus faecium 6A after incubation in air at 35 degree C for 24 hr using agar dilution method2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID1352005Antibacterial activity against vancomycin-intermediate methicillin-resistant Staphylococcus aureus Mu50 infected in BALB/c mouse assessed as decrease in bacterial survival in mouse liver at 0.4 mg, ip bid administered 4.5 days measured after 90 hrs2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.
AID542918Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as cell killing at 800 mg administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID245169Minimum inhibitory concentration against Enterococcus faecalis ATCC 29212; value ranges from 3-6 uM2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID318359Antibacterial activity against Streptococcus pneumoniae2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID534506Drug level in human THP1 cells at 50 mg/L after 2 hrs in presence of 50 uM proton inophore monesin relative to control2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
AID549013Antimicrobial activity against Vancomycin-nonsusceptible Enterococcus faecium assessed as percent resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID1271205Solubility of compound at pH 4.5 by HPLC analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID1304852Ratio of MIC for methicillin-resistant Staphylococcus aureus clinical isolate 2 in absence and presence of Fe2+2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID576430Bactericidal activity against 2 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID291412Antibacterial activity against Enterococcus faecalis 03-4 after 18 to 24 hrs2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and antibacterial activity of novel fluoroquinolones containing substituted piperidines.
AID532798Antibacterial activity against vancomycin-intermediate Staphylococcus aureus MI after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1852694Antibacterial activity against Escherichia coli SQ110 incubated for 24 hrs by twofold serial dilution method
AID373826Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 after 37 passages with Linezolid measured after 10 antibiotic-free subculture by multi-step resistance selection techniq2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID30969Harmonic mean apparent terminal disposition half-life [t1/2beta (h)] in Male Sprague-Dawley Rat at dose 25 (mg/kg po)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID561247Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as intermediate isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID1596572Bactericidal activity against Methicillin resistant Streptococcus pneumoniae ATCC 700677 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdiluti2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID520232Antimicrobial activity against Streptococcus pneumoniae 02J11752008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID541051Ratio of AUC (0 to 24 hrs) to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 75 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID133296Minimum inhibitory concentration of the subcutaneously administered compound evaluated against Staphylococcus aureus GO3 strain in mice (SC)2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID475011Antibacterial activity against Moraxella catarrhalis LCB0016 by two fold serial dilution method2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis, crystal and antibacterial studies of diversely functionalized tetrahydropyridin-4-ol.
AID499166Antimicrobial activity against methicillin-resistant Staphylococcus aureus OC 8525 infected in SKH1 mouse assessed as log change in bacterial colony forming unit per gram of skin tissue at 6.2 mg/kg/day, po (Rvb = 0.8 deltalog CFU)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID1778090Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by MABA
AID695444Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 3-FQR3M ATCC 700699 expressing GyrA Ser84Leu mutant and Glu409Lys mutant and GrlA Ser80Phe mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID112681In vivo antibacterial activity against Enterococcus faecalis strain UC 12379 administered perorally in mice1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID1861534Volume of distribution in Wistar rat at 15 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID1056357Antibacterial activity against Streptococcus pneumoniae SR26207 clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1710581Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS387 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID530125Antimicrobial activity against community acquired methicillin-resistant Staphylococcus aureus 146 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID1680060Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 6 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID284983Antimicrobial activity against Enterococcus avium at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID559800Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1520486Antibacterial activity against methicillin-sensitive Staphylococcus aureus infected in Kunming mouse dosed subcutaneously at 0.5 and 4.0 hrs postinfection and measured at 7 to 14 days post treatment by Bliss method
AID308488Antibacterial activity against Enterococcus faecalis MGH2 EF1-12007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
AID530126Antimicrobial activity against community acquired methicillin-resistant Staphylococcus aureus 144 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID1653059Antibacterial activity against Pseudomonas aeruginosa2019European journal of medicinal chemistry, Feb-15, Volume: 164Isatin derivatives and their anti-bacterial activities.
AID1770372Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as decrease of bacterial growth at 32 ug/ml measured up to 24 hrs by Time kill assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID283635Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS with 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID285373Half life for simulated intermittent-dosage regimen at 600 mg every 12 hrs using in vitro PK/PD model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
AID373662Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 after 37 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID637976Antibacterial activity against methicillin-resistant Staphylococcus aureus after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID560816AUC (0 to 24 hrs) at steady state in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID562594Antimicrobial activity against vancomycin-nonsusceptible Enterococcus faecalis clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1361105Bacteriostatic activity against vancomycin-resistant Enterococcus faecium ATCC 700221 clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID548738Antimicrobial activity against Oxacillin-resistant Staphylococcus aureus assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID244849Minimum inhibitory concentration against Staphylococcus agalactiae ATCC 138132004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
AID577099T>MIC in Enterococcus faecalis Ef1497 in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hr infusion for 2 days2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1770354Bactericidal activity against penicillin-susceptible Bacillus subtilis ATCC 9372 assessed as inhibition of bacterial growth measured after 20 hrs by two-fold microdilution assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID1596558Antibacterial activity against Cephalosporin resistant Streptococcus pneumoniae ATCC 51916 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID374589Antimicrobial activity against Staphylococcus epidermidis MTCC 2639 after 24 hrs by agar dilution assay2009European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.
AID1710575Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS382 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID775551Antibacterial activity against Enterococcus faecium SR7940 clinical isolate assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID285003Antimicrobial activity against Enterococcus gallinarum at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID530052Antimicrobial activity against Staphylococcus aureus RN4220 expressing gyrB D437N mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID1400051Antibacterial activity against Streptococcus pneumoniae ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1126489Antimicrobial activity against vancomycin-resistant Enterococcus faecium2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID1414194Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by broth microdilution based CLSI method2018European journal of medicinal chemistry, Nov-05, Volume: 159Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators.
AID559798Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at 0.25 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID292903Inhibition human liver MAOA activity2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID283170Increase in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1308227Antibacterial activity against vancomycin/methicillin-resistant Staphylococcus aureus VRS1 clinical isolate incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID575049Cmin in liver transplant patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID285002Antimicrobial activity against Enterococcus gallinarum at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID522887Antibacterial activity against vancomycin-hetero-intermediate Staphylococcus aureus isolate 873 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID562595Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID560807Absorption rate constant in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID577121Tmax in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID383557Antibacterial activity against Streptococcus pyogenes ATCC 14289 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID1710583Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS484 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID1547700Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID449618Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by agar dilution method2009Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18
Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID1603309Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 measured after 16 hrs by broth microdilution method2019ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3
Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics.
AID534510Drug level in human THP1 cells at 250 mg/L after 30 mins at pH 62010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacokinetics of the novel biaryloxazolidinone radezolid in phagocytic cells: studies with macrophages and polymorphonuclear neutrophils.
AID1680053Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae clinical isolate 3 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID522882Antibacterial activity against vancomycin-resistant Staphylococcus aureus isolate 557 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID285012Antimicrobial activity against Enterococcus hirae at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1139116Antimicrobial activity against Streptococcus pneumoniae2014Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
AID130381In vivo efficacy of compound to protect the Staphylococcus aureus UC9213 infected mouse from death after sc administration2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID533661Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid CU12008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID390334Antimicrobial activity against Escherichia coli 14112008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID373307Antibacterial activity against methicillin-susceptible Staphylococcus aureus clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID574068fCmax in CF-1 mouse at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID391847Antibacterial activity against Haemophilus influenzae IID983 by agar dilution method2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Synthesis and structure-activity relationship studies of highly potent novel oxazolidinone antibacterials.
AID730749Antibacterial activity against macrolides, lincosamides, and streptogramin B-resistant Streptococcus pyogenes 1304-00 assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID1596544Antibacterial activity against methicillin resistant Staphylococcus aureus USA400 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs by broth microdilution method2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID284949Antimicrobial activity against Bacillus spp. at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID373824Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 after 14 passages with CG400549 measured after 10 antibiotic-free subculture by multi-step resistance selection techniqu2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID558509Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 168 measured on day 25 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1180569Antimicrobial activity against Staphylococcus aureus ARC516 by broth microdilution/CLSI method2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID565231Antimicrobial activity against Mycobacterium chelonae 9917 harboring pZS01 carrying mspA gene by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID574083Ratio of fAUC (24 hrs) for community-associated methicillin-resistant Staphylococcus aureus OC8525 infected iv dosed mouse to MIC for community-associated methicillin-resistant Staphylococcus aureus OC85252009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID373309Antibacterial activity against methicillin-sensitive coagulase-negative Staphylococcus clinical isolate after 18 hrs by NCCLS M7-A4 method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
AID559799Antimicrobial activity against vancomycin-susceptible Staphylococcus aureus assessed as growth inhibition at 0.5 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID283390Antimicrobial activity against Nocardia cyriacigeorgica after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID292612Antimicrobial activity against Streptococcus pneumoniae ATCC 6303 by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID565079Antibacterial activity against community-acquired methicillin-resistant Staphylococcus aureus 147 by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
AID303969Antibacterial activity against methicillin-resistant Staphylococcus aureus SA1417 by micro-broth technology2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID569346Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae by agar dilution method2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID730744Antibacterial activity against methicillin-resistant Staphylococcus aureus 1279-07 harboring cfr gene assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID563321Antibacterial activity against vancomycin-susceptible Enterococcus faecalis EF 12704 infected in New Zealand White rabbit assessed as reduction of bacterial count in aortic valve vegetations at 10 mg/kg, administered through ear vein every 12 hrs for 4 da2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and van
AID1162168Antitubercular activity against Mycobacterium tuberculosis assessed as growth inhibition2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID523789Antimicrobial activity against oxacillin-resistant Staphylococcus aureus assessed as inhibition of microbial growth at 2 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1207747Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID1400755Antibiofilm activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 24 hrs by calgary biofilm device-based assay2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID292610Antimicrobial activity against vancomycin-resistant Enterococcus faecium 6A by agar dilution method2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
AID1904081Antibacterial activity against Enterococcus faecium NCTC 71712022European journal of medicinal chemistry, Apr-05, Volume: 233Alternative approaches utilizing click chemistry to develop next-generation analogs of solithromycin.
AID1519259Intrinsic clearance in human liver microsomes2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID207725Minimum inhibitory concentration against Staphylococcus aureus broth2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
AID775550Antibacterial activity against Moraxella catarrhalis SR26840 clinical isolate assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID1400037Bactericidal activity against Staphylococcus aureus incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID560815Tmax in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID196897Inhibition of mitochondrial protein synthesis (MPS) in rat heart mitochondria2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID560823Ratio of AUC (0 to 12 hrs) in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days to MIC for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID67092Compound was evaluated for minimum inhibitory concentration against Enterococcus faecalis 50 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID388041Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae CL2883 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID112683In vivo antibacterial activity against Enterococcus faecium strain UC 15090 administered perorally in mice1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Synthesis and antibacterial activity of U-100592 and U-100766, two oxazolidinone antibacterial agents for the potential treatment of multidrug-resistant gram-positive bacterial infections.
AID520225Antimicrobial activity against Enterococcus faecium A87672008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1594356Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123 USA400 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID561338Antimicrobial activity against Staphylococcus aureus isolate UAMS-1 by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of sarA on antibiotic susceptibility of Staphylococcus aureus in a catheter-associated in vitro model of biofilm formation.
AID583406Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate MI assessed as bacterial count at 32 times MIC after 24 hrs by colony counting method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates.
AID575079Antimicrobial activity against Streptococcus pneumoniae serotype 7F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID695236Cytotoxicity against human Hep2 cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID542696fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg /day administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID559776Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as resistant isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID429421Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID1609267Antibacterial activity against cephalosporin-resistant Streptococcus pneumoniae ATCC 51916 after 18 to 20 hrs by CLSI-based broth microdilution assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Phenylthiazoles with nitrogenous side chain: An approach to overcome molecular obesity.
AID1692900Antibacterial activity against Staphylococcus aureus ATCC 292132021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID541093Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as inhibition of bacterial growth in cage fluid at 75 mg/kg measured on day 10 postinfection compared to the bacterial growth on d2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID206226In vitro antibacterial activity against Staphylococcus epidermis ATCC 12282003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID560805Tmax in human adults with pulmonary tuberculosis at 600 mg administered daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1574838Antibacterial activity against linezolid-resistant Enterococcus faecalis by broth liquid microdilution method2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID1861529AUC in Wistar rat at 30 mg/kg, iv2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID520764Antimicrobial activity against methicillin-resistant Staphylococcus aureus infected in New Zealand rabbit osteomyelitis model assessed as improvement in extent of bone remodeling at 60 mg/kg, po administered every 8 hrs for 4 weeks measured on week 2 post2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID323822Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, po after 4 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID410206Antibacterial activity against vancomycin-resistant Enterococcus faecalis by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID1194836Antibacterial activity against penicillin-resistant Streptococcus pneumoniae incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID559796Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at 16 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID572282Antimicrobial activity against methicillin susceptible Staphylococcus aureus ATCC 49951 infected in po dosed NMRI mouse treated 1 and 5 hrs post infection2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID295162Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 03427 infected po dosed KunMing mouse2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID555498Antibacterial activity against methicillin-resistant and vancomycin-resistant Staphylococcus aureus VRS1 after 50 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID205744In vitro antibacterial activity against Staphylococcus epidermidisMR 887E (S. e. MR)2003Bioorganic & medicinal chemistry letters, Nov-17, Volume: 13, Issue:22
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
AID522927Antibacterial activity against community-acquired methicillin-resistant panton-valentine leukocidin-negative Staphylococcus aureus isolate 1470 after 24 hrs by modified broth macrodilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Antistaphylococcal activity of ACHN-490 tested alone and in combination with other agents by time-kill assay.
AID370010Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 3.12 mg/kg/day, po administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burd2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID12181Area under curve was determined in male rat2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
AID1415064Antibacterial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID1861520Antibacterial activity against Streptococcus pneumoniae ATCC 49619 incubated for 18 hrs by CLSI protocol based two-fold serial agar dilution method2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID535775Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID574084Ratio of fAUC (24 hrs) for penicillin-susceptible Streptococcus pneumoniae ATCC 6301 infected po dosed mouse to MIC for penicillin-susceptible Streptococcus pneumoniae ATCC 63012009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1374175Antibacterial activity against Enterococcus faecalis ATCC 33186 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID573866Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 infected in po dosed Swiss Webster mouse administered at 1 to 3 hrs post infection measured after 3 days2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1327118Antitubercular activity against dormant stage Mycobacterium tuberculosis H37Ra at 10 ug/ml measured after 12 days by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1778649Antibacterial activity against penicillin-susceptible Pseudomonas aeruginosa ATCC27853 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID562589Antimicrobial activity against vancomycin-nonsusceptible Enterococcus faecium clinical isolates assessed as resistant isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID373749Antimicrobial activity against mupirocin-susceptible methicillin-resistant Staphylococcus aureus assessed as resistant rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID542388Antimicrobial activity against Staphylococcus aureus RN4220 transformed with Staphylococcus aureus ST398 plasmid pSCFS3 carrying cfr and fexA genes2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr.
AID1060729Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ.
AID1265127Reversible inhibition of human MAO-B2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.
AID319150Oral bioavailability in dog at 25 mg/kg2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID1611121Antibacterial activity against linezolid-resistant Enterococcus faecalis CLSI-based double dilution method2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
AID548737Antimicrobial activity against Oxacillin-susceptible Staphylococcus aureus assessed as percent susceptible isolate by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Activities of dalbavancin against a worldwide collection of 81,673 gram-positive bacterial isolates.
AID349311Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by agar dilution method in presence of 50% human plasma2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID581023Inhibition of RNA synthesis in Staphylococcus aureus ATCC 25923 assessed as incorporation of [3H]uridine at 2 ug/ml by liquid scintillation counter2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID1723495Antibacterial activity against Enterococcus faecium NR-31914 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID283616Antimicrobial activity against Enterococcus faecium 28 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID520020Antimicrobial activity against Enterococcus faecalis ATCC 292122008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID1520444Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 to 20 hrs by CLSI-protocol based broth microdilution method
AID528974Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1710577Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS384 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID205729In vitro antibacterial activity against Staphylococcus epidermidis strains UC12084, 30031, and CDC-CNS90 (SE); range is 1-22003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID1649286Antibacterial activity against Vancomycin-resistant Enterococcus faecalis SR23630 (VanB) assessed as inhibition of bacterial growth incubated for 20 hrs by microdilution broth method
AID1167997Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 6093 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID1596569Bactericidal activity against vancomycin resistant Enterococcus faecium ATCC 700221 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution as2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID308913Antibacterial activity against Staphylococcus epidermidis ATCC 12228 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID759684Cytotoxicity against human HepG2 cells assessed as reduction of cell viability at 5 to 400 ug/ml by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens.
AID523296Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as assessed as lowest concentration to reduce bacterial burden in lungs to level of reduction achieved with higher doses orally treated in water-1% methylcel2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID1407926Antibacterial activity against Acinetobacter baumannii ARC3495 after 24 hrs by broth microdilution method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria.
AID319982Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 335912008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Synthesis, SAR, and antibacterial activity of novel oxazolidinone analogues possessing urea functionality.
AID525138Antibacterial activity against Staphylococcus aureus RN4220 after 18 to 24 hrs by broth microdilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID573126Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID558530Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 35 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID535025Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-24 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1308225Antibacterial activity against mecA-positive multidrug resistant Staphylococcus aureus NRS119 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID396026Antibacterial activity against drug-resistant Enterobacter cloacae EcDC64 isolate expressing AcrAB-TolC efflux pump by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID645033Antibacterial activity against erythromycin-resistant Streptococcus pyogenes 6 after 16 to 20 hrs by microbroth dilution method2012European journal of medicinal chemistry, Apr, Volume: 50Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
AID1723496Antibacterial activity against Enterococcus faecium NR-31916 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID245388Minimum inhibitory concentration against methicillin resistant Staphylococcus aureus (strain A27223) in absence of calf serum2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.
AID535031Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-74 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID560585Bactericidal activity against vancomycin-resistant Enterococcus faecium 1059060 expressing vanA gene assessed as change in bacterial count at 4 ug/ml by time-kill assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
AID1504618Antibacterial activity against Staphylococcus aureus ATCC 29213 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID516162Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolates assessed as susceptible isolates by EUCAST method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
AID1877883Antibacterial activity against methicillin-sensitive Staphylococcus aureus Newman assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 03-01, Volume: 59Novel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part.
AID533388Antimicrobial activity against Clostridium difficile assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID255578In vitro minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus 562 after incubation in air at 35 degree C for 24 hr using agar dilution method2005Bioorganic & medicinal chemistry letters, Oct-01, Volume: 15, Issue:19
Synthesis and SAR of novel oxazolidinones: discovery of ranbezolid.
AID1547709Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS1 clinical isolate by broth microdilution method2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.
AID1501366Bactericidal activity against methicillin-resistant Staphylococcus aureus USA200 NRS383 incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID318355Antibacterial activity against methicillin and linezolid-resistant Staphylococcus aureus2007Proceedings of the National Academy of Sciences of the United States of America, May-01, Volume: 104, Issue:18
Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties.
AID308731Antibacterial activity against Moraxella catarrhalis BC-3531 by micro-broth method2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID1435930Bactericidal activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID262226Antibacterial activity against Bacillus pumilus ATCC 143482006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID1594358Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS119 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1760594Antibacterial activity against Staphylococcus aureus 29213 assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID562194Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 540 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1308229Antibacterial activity against Staphylococcus epidermidis ATCC 35547 incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID319171Protection against vancomycin-resistant Enterococcus infection in pneumonia patient2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID558718Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1594366Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 18 to 24 hrs by broth microdilution assay2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID1852673Antibacterial activity against multidrug resistant Acinetobacter baumannii Ab5075 assessed as inhibition of bacterial growth incubated for 24 hrs in MHI medium by twofold serial dilution method
AID1154477Antibacterial activity against of methicillin-resistant Staphylococcus aureus ATCC 33591 infected in iv dosed neutropenic mouse assessed as host survival administered 1 hr after infection measured after 24 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID558521Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID303914Antibacterial activity against vancomycin-resistant Enterococcus faecium 6A after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID284995Antimicrobial activity against Enterococcus durans at 0.12 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1493823Antibacterial activity against Staphylococcus aureus NRS119 clinical isolate after 18 to 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1519266Antibacterial activity agianst linezolid-resistant Enterococcus faecalis clinical isolates2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID576659Bactericidal activity against 2 hrs peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID115950Minimum inhibitory concentration in mice against antimicrobial activity in methicillin-resistant Staphylococcus aureus(MRSA 27660).2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids.
AID390330Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae 9402008Journal of natural products, Dec, Volume: 71, Issue:12
Citreamicins with potent gram-positive activity.
AID559358Antimicrobial activity against compound-resistant Coxiella burnetii Nine-Mile obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID564132Antimicrobial activity against methicillin-resistant Staphylococcus aureus HUSA 304 infected in Wistar rat assessed as decrease in bacterial load in tissue cage fluid at 50 mg/kg, ip administered every 12 hrs for 7 days measured on day 8 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID576864Bactericidal activity against 0.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusio2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID70920In vitro antibacterial activity against Escherichia coli ATCC 25922 (Ecol) was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID1778665Ratio of MBC to MIC against methicillin-resistant Staphylococcus aureus ATCC 433002021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID260737Antibacterial activity against Bacillus subtilis BD542006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID1271215AUC (0 to t) in BALB/c mouse brain at 10 mg/kg, po by LC-MS/MS analysis2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID262236Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 7008022006Bioorganic & medicinal chemistry letters, Mar-15, Volume: 16, Issue:6
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
AID388047Antibacterial activity against Escherichia coli MB2884 after 18 to 20 hrs by serial dilution method2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
AID560814Cmax in human adults with pulmonary tuberculosis at 600 mg administered twice daily for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID1117370Antimicrobial activity against Bacillus subtilis ATCC 6633 assessed as partially clear inhibition zone at 37 degC for 24 hrs by agar diffusion method2010MedChemComm, Aug-01, Volume: 1, Issue:2
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
AID583882Antibacterial activity against cfr positive Staphylococcus aureus clinical isolate by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Elevated linezolid resistance in clinical cfr-positive Staphylococcus aureus isolates is associated with co-occurring mutations in ribosomal protein L3.
AID245125In vitro minimum inhibitory concentration against vancomycin-resistant Enterococcus faecalis NCTC 122012005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID283611Antimicrobial activity against Enterococcus faecalis 25 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID729221Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID520234Antimicrobial activity against Haemophilus influenzae A19502008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID576435Bactericidal activity against 24 hrs peripheral compartment culture samples of Staphylococcus aureus RN4220 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID560517Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 07b63 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID68251In vitro antibacterial activity against vancomycin-resistant Enterococcus faecium UC12712 (VRE); range is 0.5-12003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID1400043Bactericidal activity against Staphylococcus aureus BAA 1683 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID353060Antibacterial activity against vancomycin-resistant Enterococcus 3 after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID641049Antibacterial activity against Streptococcus pneumoniae by agar microdilution method2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID542674fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 300 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1312940Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA100 NRS382 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID373828Antimicrobial activity against panton-valentine leukocidin-negative community-acquired methicillin-resistant Staphylococcus aureus 481 after 50 passages with vancomycin measured after 10 antibiotic-free subculture by multi-step resistance selection techni2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1374169Antibacterial activity against Staphylococcus aureus CMCC 26003 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID349313Antibacterial activity against Moraxella catarrhalis clinical isolate after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID1151629Toxicity in female rat assessed as effect on lymphocyte count at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 74.8%)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID533948Antimicrobial activity against methicillin-resistant, vancomycin intermediate Staphylococcus aureus NRS52 after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID1243928Antimicrobial activity against methicillin-resistant Staphylococcus aureus USA300 assessed as reduction in bacterial growth incubated for 18 to 20 hrs at 37 degC by broth microdilution method2015European journal of medicinal chemistry, Aug-28, Volume: 101Discovery and characterization of aryl isonitriles as a new class of compounds versus methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1861522Antibacterial activity against Staphylococcus aureus Sta-5027 infected in Swiss mouse model of septicemia administered by oral route 1 h and 5 h post-infection2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID206613In vitro antibacterial activity against the methicillin-resistant Staphylococcus aureus 881999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
3D QSAR studies on new oxazolidinone antibacterial agents by comparative molecular field analysis.
AID531643Antimicrobial activity against linezolid-resistant Enterococcus faecium A6349 expressing VanA gene2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID756092Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as growth inhibition after 16 hrs by agar dilution method2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
AID1883847Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 14 to 21 days2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Tuberculosis Drug Discovery: Challenges and New Horizons.
AID297121Antibacterial activity against methicillin-resistant Staphylococcus aureus 92-1191 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1778652Antibacterial activity against penicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth measured by broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID533021Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-3 assessed as inhibition of bacterial growth in Mueller-Hinton broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID534154Antimicrobial activity against linezolid-resistant Enterococcus faecalis 3124 harboring G2576U mutation in peptidyl transferase centre by broth microdilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
AID561250Antibacterial activity against Streptococcus pneumoniae assessed as susceptible isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID576658Bactericidal activity against 1 hr peripheral compartment culture samples of Enterococcus faecalis ATCC 29212 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1059060Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate N315 by liquid microdilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-anti-MRSA activity relationship of macrocyclic bis(bibenzyl) derivatives.
AID1435932Bactericidal activity against methicillin/erythromycin/tetracycline-resistant Staphylococcus aureus USA300 NRS384 clinical isolate after 24 hrs2017European journal of medicinal chemistry, Jan-27, Volume: 126Phenylthiazole antibiotics: A metabolism-guided approach to overcome short duration of action.
AID285083Antimicrobial activity against viridans group Streptococcus constellatus at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID429428Antibacterial activity against Haemophilus influenzae isolate 283 by agar dilution method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antibacterial activity of novel 5-(4-methyl-1H-1,2,3-triazole) methyl oxazolidinones.
AID383561Antibacterial activity against Enterococcus faecalis ATCC 14506 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID68066Antibacterial activity against ciprofloxacin resistant and linezolid-resistant Enterococcus faecium (EF4008 LinR;CipR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID559372Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP3 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID573140Antibacterial activity against erythromycin-nonsusceptible Streptococcus agalactiae assessed as susceptible isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID1594387Tmax in human at 625 mg, iv2019Bioorganic & medicinal chemistry, 05-01, Volume: 27, Issue:9
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.
AID278860Antiproliferative effect against HeLa cells after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID1677794Bacteriostatic activity against penicillin-resistant Staphylococcus aureus assessed as ratio of MBC to MIC2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID1327114Antibacterial activity against Bacillus subtilis NCIM 2010 at 30 ug/ml measured after 12 hrs by spectrophotometric method2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1852666Antibacterial activity against multidrug resistant Klebsiella pneumoniae ATCC13883 assessed as inhibition of bacterial growth incubated for 24 hrs in M9-MOPS medium by twofold serial dilution method
AID283162Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2622 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1180588Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC2398-2F to MIC for Staphylococcus aureus ARC23982014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID528848Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1056363Antibacterial activity against Staphylococcus aureus Smith clinical isolate assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID1710585Antibacterial activity against vancomycin-resistant Staphylococcus aureus 12 assessed as inhibition of visible bacterial growth incubated for 18 to 20 hrs by CLSI method2020RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1
Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria.
AID293553Antibacterial activity against Escherichia coli MTCC 51 after 24 hrs by agar dilution assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Organoiodine(III) mediated synthesis of 3,9-diaryl- and 3,9-difuryl-bis-1,2,4-triazolo[4,3-a][4,3-c]pyrimidines as antibacterial agents.
AID1272265Antimicrobial activity against vancomycin-susceptible Enterococcus faecalis MMX 101 after 18 to 20 hrs by microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.
AID1059059Antibacterial activity against 2-phenoxyphenol and trichlosan-resistant Staphylococcus aureus clinical isolate N315 by liquid microdilution method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Structure-anti-MRSA activity relationship of macrocyclic bis(bibenzyl) derivatives.
AID444263Antibacterial activity against vancomycin-resistant Enterococcus faecium 6A by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID207721In vitro minimum inhibitory concentration (MIC) against Staphylococcus aureus UC92132003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID373660Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1474206Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolates after 18 to 22 hrs by broth microdilution method2017Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
AID349312Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by agar dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and structure-antibacterial activity of triazolyl oxazolidinones containing long chain acyl moiety.
AID577134AUC in two-compartment pharmacokinetic/pharmacodynamic model at 600 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID284966Antimicrobial activity against Corynebacterium jeikeium at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID410109Antimicrobial activity against Linezolid-resistant Enterococcus faecalis ATCC 29212-P5 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID520029Antimicrobial activity against Enterococcus faecium A6348 harboring G2576U mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID499111Antimicrobial activity against methicillin-susceptible Staphylococcus aureus Smith OC 4172 infected immunocompromized SKH1 mouse assessed as lesion volume at 6.2 mg/kg/day, sc measured after 48 hrs postinfection (Rvb = 1181 mm3)2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vivo activity of ceftobiprole in murine skin infections due to Staphylococcus aureus and Pseudomonas aeruginosa.
AID520235Antimicrobial activity against Staphylococcus aureus A78202008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID533003Antibacterial activity against vancomycin-intermediate Staphylococcus aureus PC phenotypic revertant after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID1151753Antibacterial activity against penicillin intermediate-sensitive Streptococcus pneumoniae ATCC 49619 clinical isolate2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1721016Inhibition of mitochondrial protein synthesis in rat H9c2 cells measured after 5 days by ELISA2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID542887fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered as 2 divided doses every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID542692fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID311477Antimicrobial activity against Staphylococcus epidermidis ATCC 700578 after 14 to 16 hrs by serial micro-broth dilution method2007Journal of natural products, Sep, Volume: 70, Issue:9
Lipoxazolidinones A, B, and C: antibacterial 4-oxazolidinones from a marine actinomycete isolated from a Guam marine sediment.
AID576398Tmax in two-compartment pharmacokinetic/pharmacodynamic model at 800 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID575145Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolate NRS71 by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID285011Antimicrobial activity against Enterococcus hirae at 1 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID558721Antimicrobial activity against methicillin-resistant Staphylococcus aureus 525 measured on day 45 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1721019Antitubercular activity against Mycobacterium tuberculosis isolate 12525 incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID284942Antimicrobial activity against Aerococcus spp. at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID405627Toxicity in rat heart mitochondria assessed as inhibition of mitochondrial protein synthesis2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID68064Antibacterial activity against ciprofloxacin resistant Enterococcus faecium (EF4010 CipR)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Novel oxazolidinone-quinolone hybrid antimicrobials.
AID531637Inhibition of 50S ribosomal subunit purified from linezolid-,erythromycin-resistant Staphylococcus aureus A7820 with G2576U mutation in 23s rRNA assessed as inhibition of translation using in vitro transcribed mRNA encoding firefly luciferase2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
R chi-01, a new family of oxazolidinones that overcome ribosome-based linezolid resistance.
AID584996Antibacterial activity against methicillin-resistant Staphylococcus aureus M05/0060 harboring cfr-encoding conjugative pSCFS7 and fexA by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Identification and characterization of the multidrug resistance gene cfr in a Panton-Valentine leukocidin-positive sequence type 8 methicillin-resistant Staphylococcus aureus IVa (USA300) isolate.
AID1308228Antibacterial activity against vancomycin/methicillin-resistant Staphylococcus aureus VRS2 clinical isolate incubated for 16 to 20 hrs by microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
AID134114Protective dose of orally administered compound against intraperitoneally-induced septicaemia model (Enterococci faecalis D2HT6 strain) in murine2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115.
AID442575Antibacterial activity against Bacillus cereus MTCC 430 after 24 hrs by spectrophotometry2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Synthesis of nitroimidazole derived oxazolidinones as antibacterial agents.
AID1126490Antimicrobial activity against erythromycin-susceptible Streptococcus pneumoniae ATCC 496192014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID245299Minimal inhibitory concentration against methicillin resistant Staphylococcus epidermidis ATCC 237602004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
AID630557Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID1723500Antibacterial activity against Enterococcus faecalis HM-334 incubated for 18 to 20 hrs under aerobic condition by CLSI protocol based broth microdilution assay
AID244924Antibacterial activity against Streptococcus mitis IID685 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID541079Cmin in cage fluid of Albino guiena pig at 25 mg/kg, ip after 12 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID560510Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b5k3529 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID396029Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate in presence of 20 ug/ml efflux pump inhibitor Phe-Arg-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID1584841Antibacterial activity against methicillin and linezolid resistant Staphylococcus aureus NRS 119 clinical isolate after 18 to 24 hrs by microdilution assay2018European journal of medicinal chemistry, Nov-05, Volume: 1591-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.
AID576408AUC in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1861521Antibacterial activity against Haemophilus influenzae pneumoniae ATCC 35054 incubated for 18 hrs by CLSI protocol based two-fold serial agar dilution method2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71WCK 4034: A promising oxazolidinone for treating gram positive infections.
AID533634Antimicrobial activity against Propionibacterium acnes assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID201408Inhibitory activity against Methicillin-resistant Staphylococcus aureus UC66852000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Substituent effects on the antibacterial activity of nitrogen-carbon-linked (azolylphenyl)oxazolidinones with expanded activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID533023Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1-4 assessed as inhibition of bacterial growth in Mueller-Hinton broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID562195Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 measured after 10 antibiotic-free subculturing by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID575147Antimicrobial activity against vancomycin-resistant Staphylococcus aureus VRS1 by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID520771Toxicity in methicillin-resistant Staphylococcus aureus-infected New Zealand rabbit osteomyelitis model assessed as body weight at 60 mg/kg, po administered every 8 hrs for 4 days measured on week 2 postinfection (Rvb = 2.43 +/- 0.15 kg)2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Efficacies of ceftobiprole medocaril and comparators in a rabbit model of osteomyelitis due to methicillin-resistant Staphylococcus aureus.
AID1519260Metabolic stability in human liver microsomes assessed as parent compound remaining after 45 mins in presence of NADPH relative to control2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID345134Inhibition of protein synthesis in Escherichia coli S30 extract by translation assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
AID1304833Antibacterial activity against Staphylococcus epidermidis ATCC 12228 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID520010Antimicrobial activity against Staphylococcus aureus A8833 harboring U2500A mutation in 23S rRNA2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID585163Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2571G mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID409583Antimicrobial activity against methicillin-resistant Staphylococcus aureus 05-2 infected in po dosed KunMing SPF mouse2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
AID562175Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 1287 after 50 passages by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1501368Bactericidal activity against vancomycin-resistant Staphylococcus aureus isolate 4 incubated for 20 hrs followed by replating on tryptic soy agar plates and further incubated for 18 hrs by broth microdilution assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.
AID517670Antimicrobial activity against Enterococcus faecium NCTC 12203 by standard serial-dilution technique2010Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
AID1400019Antibacterial activity against Staphylococcus aureus incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID205585Compound was evaluated for minimum inhibitory concentration against Staphylococcus epidermidis 9753 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID424423Antibacterial activity against Enterococcus faecalis HIP15179 coisolated with vancomycin-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID1312943Antimicrobial activity against vancomycin-resistant Staphylococcus aureus 10 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID1519043Antibacterial activity against clinical isolates of vancomycin-resistant Enterococcus faecium assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID565076Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacodynamic profile of tigecycline against methicillin-resistant Staphylococcus aureus in an experimental pneumonia model.
AID410103Inhibition of Escherichia coli translation2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
AID542915Antimicrobial activity against Bacillus anthracis infected in in vitro hollow fiber PK/PD model assessed as reduction in bacterial burden at 700 mg administered once every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID530123Antimicrobial activity against hospital acquired methicillin-resistant Staphylococcus aureus 56 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Pharmacodynamic characterization of ceftobiprole in experimental pneumonia caused by phenotypically diverse Staphylococcus aureus strains.
AID528978Antimicrobial activity against methicillin-susceptible Staphylococcus aureus assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID484701Antimicrobial activity against methicillin-resistant Staphylococcus aureus2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Potent antimicrobial activity of 3-(4,5-diaryl-1H-imidazol-2-yl)-1H-indole derivatives against methicillin-resistant Staphylococcus aureus.
AID458456Antimicrobial activity against wild type Pseudomonas aeruginosa K799 at 2 mM after overnight incubation by agar diffusion method2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Syntheses and antibacterial activity studies of new oxazolidinones from nitroso Diels-Alder chemistry.
AID523815Antimicrobial activity against oxacillin-susceptible coagulase-negative Staphylococcus aureus assessed as inhibition of microbial growth at 0.5 ug/ml by CLSI method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Comparative activities of TR-700 (torezolid) against staphylococcal blood isolates collected in Spain.
AID1076823Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate 2 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID352928Antibacterial activity against Haemophilus influenzae after 18 to 20 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9
Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties.
AID528710Antibacterial activity against penicillin intermediate Streptococcus pneumoniae clinical isolate assessed as susceptibility level by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro activity of telavancin against resistant gram-positive bacteria.
AID558500Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1898414Bactericidal activity against methicillin-resistant vancomycin-resistant Enterococcus faecium ATCC 700221 planktonic cells assessed as planktonic eradication incubated for 24 hrs followed by incubation for overnight in fresh medium by Calgary biofilm devi2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
A Modular Synthetic Route Involving
AID293839Antibacterial activity against Enterococcus faecium ATCC 194342007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
A new class of anti-MRSA and anti-VRE agents: preparation and antibacterial activities of indole-containing compounds.
AID548253Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 after 24 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID567456Antimicrobial activity against methicillin-resistant Staphylococcus aureus CGK8 by Etest method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
AID368290Bactericidal activity against methicillin-resistant Staphylococcus aureus SA2 in rabbit endocarditis model assessed as growth inhibition at 58 mg/kg infused every 12 hrs for 4 days measured after 48 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID410221Antibacterial activity against Escherichia coli LCB0012 by broth micro dilution method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID1151707Antibacterial activity against Staphylococcus aureus in po dosed mouse septicemia model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1493806Antibacterial activity against Staphylococcus aureus VRS11a clinical isolate after 20 hrs by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1778658Bactericidal activity against erythromycin-susceptible Staphylococcus aureus ATCC 25923 measured after 24 hrs by CLSI protocol based method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID308725Inhibition of transcription and translation activity in Escherichia coli by luciferase reporter assay2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
AID1400760Bactericidal activity against vancomycin-resistant Enterococcus faecium ATCC 700221 after 24 hrs by calgary biofilm device-based assay2017MedChemComm, Apr-01, Volume: 8, Issue:4
Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria.
AID207882Antibacterial activity against Methicillin-resistant Staphylococcus epidermidis UC12084 (S. e)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials.
AID68249In vitro antibacterial activity against vancomycin-resistant Enterococcus faecium 154 (Enterococcus faecium ATCC 12202)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Influence of ethylene-oxy spacer group on the activity of linezolid: synthesis of potent antibacterials possessing a thiocarbonyl group.
AID575051Cmin in patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs co-treated with rifampin by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID559795Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as growth inhibition at 4 times MIC2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1770370Ratio of MBC to MIC against Vancomycin-resistant Enterococcus faecium ATCC 515592021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID1778645Antibacterial activity against erythromycin-susceptible Staphylococcus aureus ATCC 25923 assessed as bacterial growth inhibition incubated for 24 hrs by CLSI protocol based broth microdilution method2021European journal of medicinal chemistry, Oct-05, Volume: 221Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.
AID297124Antibacterial activity against Staphylococcus aureus macrolide-resistance after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1197119Antibacterial activity against vancomycin/methicillin-resistant Staphylococcus aureus VRS1 clinical isolate after 16 to 20 hrs by broth microdilution method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID284950Antimicrobial activity against Bacillus spp. at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1400061Antibacterial activity against Bacillus subtilis ATCC 6051 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID368289Bactericidal activity against vancomycin-intermediate Staphylococcus aureus in rabbit endocarditis model assessed per gram of aortic vegetation at 58 mg/kg infused every 12 hrs for 4 days measured after 48 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
AID1151625Toxicity in female rat assessed as effect on mean corpuscular volume at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 53.72 fL)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1519039Antibacterial activity against vancomycin-resistant Enterococcus faecium assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID1400023Antibacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 15 days under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1504623Antibacterial activity against Streptococcus pneumoniae 55143 by microbroth dilution method2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Design, Synthesis, and Antibacterial Evaluation of Oxazolidinones with Fused Heterocyclic C-Ring Substructure.
AID284985Antimicrobial activity against Enterococcus avium at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID70918In vitro antibacterial activity against Escherichia coli AS19 (Eco2), permeable mutant was determined2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
AID1304847Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 incubated for 16 hrs by broth microdilution method in presence of tiron2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1154473Antibacterial activity against clinical isolate of methicillin-sensitive Staphylococcus aureus infected in iv dosed mouse assessed as host survival administered 1 hr after infection for 4 days2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID533980Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA040L infected in THP1 cells after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID345137Antimicrobial activity against linezolid-resistant Enterococcus faecalis P5 by NCCLS method2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Design at the atomic level: generation of novel hybrid biaryloxazolidinones as promising new antibiotics.
AID542673fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 200 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1329448Antibacterial activity against linezolid-resistant Mycobacterium tuberculosis H37Rv in hollow-fiber infection model assessed as reduction in bacterial burden at 342 mg, po at 24 hrs dose regimen measured after 3 weeks2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
From lead optimization to NDA approval for a new antimicrobial: Use of pre-clinical effect models and pharmacokinetic/pharmacodynamic mathematical modeling.
AID374015Antimicrobial activity against methicillin-resistant Staphylococcus aureus 481 after single-step resistance selection by agar dilution CLSI method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID285024Antimicrobial activity against Listeria monocytogenes at 2 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1432970Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay
AID1680044Antibacterial activity against NDM1 producing carbapenem-resistant Enterobacteriaceae clinical isolate 2 assessed as reduction in bacterial growth incubated for 16 to 20 hrs by CLSI-based broth microdilution method2018European journal of medicinal chemistry, Jul-15, Volume: 155Synthesis and antibacterial bioactivities of cationic deacetyl linezolid amphiphiles.
AID637974Antibacterial activity against Enterococcus faecalis ATCC 29212 expressing VanS gene after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID533973Antimicrobial activity against linezolid-resistant Staphylococcus aureus SA040L infected in THP1 cells assessed as log reduction in bacterial count after 24 hrs2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Cellular pharmacodynamics of the novel biaryloxazolidinone radezolid: studies with infected phagocytic and nonphagocytic cells, using Staphylococcus aureus, Staphylococcus epidermidis, Listeria monocytogenes, and Legionella pneumophila.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID383737Tmax in Sprague-Dawley rat at 25 mg/kg, po2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID1167989Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 5814 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID533015Antibacterial activity against vancomycin-susceptible Staphylococcus aureus N315-LR5-P1 assessed as inhibition of bacterial growth in Mueller-Hinton broth medium2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID574076Apparent oral clearance in CF-1 mouse at 10 mg/kg, sc2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
In vivo activity of the pyrrolopyrazolyl-substituted oxazolidinone RWJ-416457.
AID1873905Antibacterial activity against Staphylococcus aureus incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1390467Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 BAA-15562018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID292908Antibacterial activity against Streptococcus pneumoniae ARC548 infected C57BL/6 mouse lung at 25 mg/kg, po after 2 days relative to Linezolid2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New carbon-linked azole oxazolidinones with improved potency and pharmacokinetics.
AID1393956Antibacterial activity against methicillin resistant Staphylococcus aureus NR 45913 after 16 to 20 hrs by CLSI method2018Bioorganic & medicinal chemistry letters, 09-01, Volume: 28, Issue:16
3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
AID1415066Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 2 after 16 hrs by agar dilution method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Semisynthesis of Platensimycin Derivatives with Antibiotic Activities in Mice via Suzuki-Miyaura Cross-Coupling Reactions.
AID1233136Antibacterial activity against patient-derived methicillin-resistant Staphylococcus aureus B19506 after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID285062Antimicrobial activity against beta hemolytic Streptococci group F at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID576423Antibacterial activity against Enterococcus faecalis Ef1497 by agar dilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1056349Inhibition of rat forebrain MAO-B using [14C]PEA as substrate at 30 uM preincubated for 20 mins followed by substrate addition measured after 10 mins by liquid scintillation counting analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID132588In vivo Efficacy of compound after peroral administration to protect the Staphylococcus aureus mouse septicemia model2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
AID1603310Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 measured after 16 hrs by broth microdilution method2019ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3
Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics.
AID565489Ratio of MBC to MIC for methicillin-susceptible Staphylococcus aureus2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID576868Bactericidal activity against 12.5 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 200 mg, bid administered as 0.5 hr infusi2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID1400049Bactericidal activity against Enterococcus faecalis ATCC 19433 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID208011The compound was evaluated for its anti-bacterial activity against Streptococcus pneumoniae UC 99121998Journal of medicinal chemistry, Dec-17, Volume: 41, Issue:26
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
AID289868Antibacterial activity against Enterococcus faecium ATCC 122022007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
AID67754Minimum inhibitory concentration against Enterococcus faecalis MTCC 4392004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Oxazolidinone: search for highly potent antibacterial.
AID1692906Antibacterial activity against hospital acquired vancomycin-resistant Enterococcus faecium clinical isolates2021Bioorganic & medicinal chemistry letters, 01-15, Volume: 32Design, synthesis and antibacterial evaluation of novel oxazolidinone derivatives nitrogen-containing fused heterocyclic moiety.
AID1760589Antibacterial activity against wild type Escherichia coli JW5503 delta tolC assessed as inhibition of bacterial growth measured after 24 hrs2021European journal of medicinal chemistry, Feb-05, Volume: 211Installation of an aryl boronic acid function into the external section of N-aryl-oxazolidinones: Synthesis and antimicrobial evaluation.
AID1574849Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Design and synthesis of biaryloxazolidinone derivatives containing a rhodanine or thiohydantoin moiety as novel antibacterial agents against Gram-positive bacteria.
AID1591547Ratio of MBC for methicillin-resistant Staphylococcus aureus ATCC 43300 to MIC for methicillin-resistant Staphylococcus aureus ATCC 433002019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Discovery of 1,3,4-oxadiazol-2-one-containing benzamide derivatives targeting FtsZ as highly potent agents of killing a variety of MDR bacteria strains.
AID285549Tmax in mouse at 20 mg/kg, sc2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID1519261Cytotoxicity against human HepG2 cells assessed as reduction in cell viability2019Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety.
AID285092Antimicrobial activity against viridans group Streptococcus gordonii at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID439892Antibacterial activity against Pseudomonas aeruginosa ATCC 90277 after 18 hrs by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones.
AID66111In vitro antibacterial activity against Enterococcus faecalis ATCC 29212 (E. f. 034) vancomycin sensitive2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID308923Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 by broth microdilution method2007Bioorganic & medicinal chemistry letters, Sep-15, Volume: 17, Issue:18
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
AID775533Inhibition of CYP1A2 in human liver microsomes assessed as ethoxyresorufin O-deethylation after 20 mins by fluorescence plate reader analysis2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID525145Antimicrobial activity against linezolid-resistant Staphylococcus aureus isolate 004-737X expressing cfr and ermA gene isolated from paraplegic patient by Etest method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID1151647Inhibition of MAO-A (unknown origin) using tyramine as substrate after 30 to 60 mins by fluorescence plate reader analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID577136Total clearance in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hr infusion over 24 hrs2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID558494Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID585166Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2499A2 mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID67385In vitro antibacterial activity against vancomycin susceptible Enterococcus faecalis UC19217 (VSEF)2003Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23
The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones.
AID205839Minimum inhibitory concentration measured against Staphylococcus aureus2002Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16
The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.
AID585172Antibacterial activity against Mycobacterium smegmatis harboring 23S rRNA C2055A mutant after 24 generation times2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Mutations in 23S rRNA at the peptidyl transferase center and their relationship to linezolid binding and cross-resistance.
AID775546Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 assessed as growth inhibition by broth microdilution method2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis and in vitro/in vivo antibacterial activity of oxazolidinones having thiocarbamate at C-5 on the A-ring and an amide- or urea-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane as the C-ring.
AID1154475Antibacterial activity against of methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in iv dosed mouse assessed as host survival administered 1 hr after infection measured after 48 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID383560Antibacterial activity against Staphylococcus aureus ATCC 25923 by broth microdilution technique2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
AID1375987Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 2 weeks by microplate alamar blue assay2016MedChemComm, Nov-01, Volume: 7, Issue:11
SAR and identification of 2-(quinolin-4-yloxy)acetamides as
AID630555Antibacterial activity against methicillin-resistant Staphylococcus aureus after 16 hrs by agar dilution method2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
AID245185Minimum inhibitory concentration against Proteus vulgaris ATCC 8427; value ranges from 12-25 uM2004Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
Aryl urea analogs with broad-spectrum antibacterial activity.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID528972Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID573145Antibacterial activity against penicillin-susceptible Streptococcus viridans assessed as resistant isolates by CLSI M7-A7 broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
In vitro profiling of ceftaroline against a collection of recent bacterial clinical isolates from across the United States.
AID549536Apparent permeability from apical to basolateral side of MDCK cells2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
MDCK cell permeability characteristics of a sulfenamide prodrug: strategic implications in considering sulfenamide prodrugs for oral delivery of NH-acids.
AID1677804Antibacterial activity against Staphylococcus aureus clinical isolate incubated for 24 hrs by CLSI-based broth microdilution method2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID295161Antibacterial activity against methicillin-susceptible Staphylococcus aureus 04-5 infected po dosed KunMing mouse2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID560818Antimicrobial activity against Mycobacterium tuberculosis in human adults with pulmonary tuberculosis at 600 mg administered twice for 7 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID729218Antibacterial activity against linezolid-resistant Staphylococcus aureus after 16 hrs by NCCLS agar dilution method2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
AID284960Antimicrobial activity against Corynebacterium spp. at 0.5 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID687498Volume of distribution in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID730750Antibacterial activity against macrolides, lincosamides, and streptogramin B-resistant Streptococcus pneumoniae 1243-00 assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
Novel 3-O-carbamoyl erythromycin A derivatives (carbamolides) with activity against resistant staphylococcal and streptococcal isolates.
AID285015Antimicrobial activity against Enterococcus raffinosus at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID1241205Inhibition of pre-miR-372 (unknown origin) cleavage assessed as reduction of oncogenic microRNAs biogenesis by measuring fluorescence every minute for 5 hrs using 5'-FAM,3'-dabcyl-pre-miRNA beacons by FRET assay in presence of recombinant Dicer2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Ribosome-targeting antibiotics as inhibitors of oncogenic microRNAs biogenesis: Old scaffolds for new perspectives in RNA targeting.
AID1687312Synergistic antibacterial activity against wild type Escherichia coli BW25113 in presence of 0.25 times MIC of colistin incubated for 18 to 20 hrs by broth microdilution method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of benzimidazole-based derivatives as antimicrobial agents and their synergistic effect with colistin against gram-negative bacteria.
AID519490Antibacterial activity against Staphylococcus aureus T2019/50 expressing 23S rrn1 G2576T, rrn3 G2576T, rrn4 G2576T and rrn5 G2576T mutants by Etest method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
AID424771Antifungal activity against Candida albicans MY1055 after 20 hrs by twofold serial broth dilution method2009Journal of natural products, May-22, Volume: 72, Issue:5
Thiazomycins, thiazolyl peptide antibiotics from Amycolatopsis fastidiosa.
AID726200Antibacterial activity against methicillin-resistant Staphylococcus aureus C463 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones.
AID576124Antibacterial activity against 2 x 10'8 CFU Enterococcus faecalis u810 infected in ICR mouse systemic infection model assessed as mouse protection administered orally twice after 1 and 4 hrs post infection measured after 48 hrs2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID1126482Antimicrobial activity against penicillin- and erythromycin-resistant Streptococcus pneumoniae2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Synthesis, antibiotic activity and structure-activity relationship study of some 3-enaminetetramic acids.
AID319166Drug level in human urine2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
AID528849Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID576876Bactericidal activity against 12 hrs peripheral compartment culture samples of Enterococcus faecalis Ef1497 MutM3 in two-compartment pharmacokinetic/pharmacodynamic model assessed as effect on bacterial count at 600 mg, bid administered as 0.5 hr infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID23886Plasma clearance in Male Sprague-Dawley Rat (10 mg/kg iv)2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.
AID245008In vitro minimum inhibitory concentration of compound against Mycobacterium smegmatis MTCC 0062005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID1337725Inhibition of MAO activity in human HepG2 cells at 100 ug/mL after 24 hrs by spectrophotometric method2016European journal of medicinal chemistry, Nov-29, Volume: 124New isoxazolidinone and 3,4-dehydro-β-proline derivatives as antibacterial agents and MAO-inhibitors: A complex balance between two activities.
AID1432995Elimination half life in CD1 mouse at 10 mg/kg, po measured over 24 hrs by HPLC/MS/MS method
AID535026Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-26 expressing SCCmec type 2 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID467837Antibacterial activity against floxacin and methicillin-resistant Staphylococcus aureus ATCC 25923 after 24 hrs by agar dilution method2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Novel 4-N-substituted aryl but-3-ene-1,2-dione derivatives of piperazinyloxazolidinones as antibacterial agents.
AID542892fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 600 mg administered every 12 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID558491Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 555 measured on day 15 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID291409Antibacterial activity against methicillin-sensitive Staphylococcus aureus 04-4 after 18 to 24 hrs2007Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
Synthesis and antibacterial activity of novel fluoroquinolones containing substituted piperidines.
AID581670Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth at pH 5.5 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID285007Antimicrobial activity against Enterococcus hirae at <= 0.06 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID575081Antimicrobial activity against Streptococcus pneumoniae serotype 6C assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID558520Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus 873 measured on day 30 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID565490Ratio of MBC to MIC for methicillin-resistant Staphylococcus aureus in presence of 50% human plasma2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
In vitro bactericidal activity of iclaprim in human plasma.
AID560819Cmax in human adults with pulmonary tuberculosis at 600 mg administered once daily for 5 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Population pharmacokinetics of linezolid in adults with pulmonary tuberculosis.
AID66115In vitro antibacterial activity against Enterococcus faecium ATCC 12202 (E.fm 154) vancomycin resistant2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Synthesis of conformationally constrained analogues of linezolid: structure-activity relationship (SAR) studies on selected novel tricyclic oxazolidinones.
AID1400062Bactericidal activity against Bacillus subtilis ATCC 6051 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1778104Antibacterial activity against linezolid resistant Staphylococcus capitis assessed as bacterial growth inhibition after 18 hrs by broth microdilution method
AID1056361Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS271 clinical isolate harboring G2576T mutation in peptidyl transferase center domain V of 23S rRNA gene assessed as parasite growth inhibition by CLSI broth microdilution method2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
AID483196Antibacterial activity against Escherichia coli ATCC 35218 by microbroth dilution technique2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Design, synthesis, and antibacterial activity of 2,5-dihydropyrrole formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
AID535033Antimicrobial activity against vancomycin intermediate Staphylococcus aureus NRS-118 expressing SCCmec type 1 element by microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of ceftaroline against community-associated methicillin-resistant, vancomycin-intermediate, vancomycin-resistant, and daptomycin-nonsusceptible Staphylococcus aureus isolates.
AID1167999Antibacterial activity against vancomycin-resistant Enterococcus faecalis clinical isolate 387702 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID520022Antimicrobial activity against Enterococcus faecalis A63502008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
In vitro activities of the Rx-01 oxazolidinones against hospital and community pathogens.
AID559777Antimicrobial activity against heterogeneous vancomycin-intermediate Staphylococcus aureus assessed as intermediate isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1898408Bactericidal activity against methicillin-resistant Staphylococcus aureus BAA-1707 planktonic cells assessed as planktonic eradication incubated for 24 hrs followed by incubation for overnight in fresh medium by Calgary biofilm device assay2021Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
A Modular Synthetic Route Involving
AID396027Antibacterial activity against drug-resistant Enterobacter cloacae EcDC64 isolate expressing AcrAB-TolC efflux pump in presence of 20 ug/ml efflux pump inhibitor Phe-Arg-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID1151763Antibacterial activity against methicillin-sensitive Staphylococcus aureus isolate 15 in po dosed mouse systemic infection model2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1312938Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS119 clinical isolate after 20 hrs by broth microdilution method2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
AID283637Antimicrobial activity against Staphylococcus aureus RN4220 deltamutS with 23S rRNA G2576U and A2503G mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID562237Chemical stability of the compound assessed as compound degradation at 16 times MIC after 24 hrs by RP-HPLC analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
AID1514454Antitubercular activity against d-cycloserine-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1553380Inhibition of CYP1A2 (unknown origin)2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.
AID1603313Antimicrobial activity against Escherichia coli SQ110 DTC measured after 16 hrs by broth microdilution method2019ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3
Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics.
AID1677797Bactericidal activity against Staphylococcus aureus clinical isolate assessed as reduction in number of colony forming units incubated for 24 hrs followed by re-plating and reincubation on tryptic soy agar plate for 24 hrs2020Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus.
AID295157Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by microdilution broth method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis and antibacterial activity of oxazolidinones containing triazolyl group.
AID303917Antibacterial activity against Streptococcus pneumoniae ATCC 6303 after 24 hrs by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
AID1832941Antibacterial activity against Staphylococcus aureus USA 300 assessed as reduction in bacterial growth incubated for 20 hrs by microplate reader method2021Bioorganic & medicinal chemistry, 11-01, Volume: 49Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents.
AID370007Antibacterial activity against methicillin-susceptible Staphylococcus aureus Smith infected in C3H mouse assessed as eradication at 25 mg/kg/day, po administered within 15 mins of infection assessed per gram of kidney measured after 48 hrs by organ burden2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
AID617500Antibacterial activity against Enterococcus faecalis ATCC 29212 by CLSI method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents. Part II.
AID244990Antibacterial activity against Staphylococcus aureus FDA 209P was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID263964Antibacterial activity against vancomycin-resistant Enterococcus faecalis DRCC 1532006Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9
Synthesis and antibacterial activity of novel oxazolidinones bearing N-hydroxyacetamidine substituent.
AID260738Antibacterial activity against Staphylococcus aureus 252932006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.
AID283396Antimicrobial activity against Nocardia veterana after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID1076818Antitubercular activity against extensive drug-resistant Mycobacterium tuberculosis clinical isolate 7 assessed as growth inhibition by microdilution method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Discovery of novel bis-oxazolidinone compounds as potential potent and selective antitubercular agents.
AID297957AUC in Streptococcus pneumoniae 548 infected mouse lung infection model at 40 mg/kg/day, po2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.
AID1390483Antibacterial activity against Enterococcus faecalis ATCC 194342018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Design, synthesis and biological evaluation of spiropyrimidinetriones oxazolidinone derivatives as antibacterial agents.
AID1519040Antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus aureus assessed as complete reduction in bacterial cell growth by CLSI protocol based broth liquid microdilution method2020European journal of medicinal chemistry, Jan-01, Volume: 185Optimization of biaryloxazolidinone as promising antibacterial agents against antibiotic-susceptible and antibiotic-resistant gram-positive bacteria.
AID574545Antimicrobial activity against community-associated methicillin-resistant Staphylococcus aureus USA3002010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID1853450Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by CLSI based broth microdilution assay2021RSC medicinal chemistry, Nov-17, Volume: 12, Issue:11
SF
AID604287Antibacterial activity against Staphylococcus aureus ATCC 25923 after 16 to 24 hrs by twofold serial dilution method2011Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14
7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity.
AID541072Tmax in cage fluid of Albino guiena pig at 25 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID581665Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU level at up to 10'5 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID745400Antibacterial activity against Haemophilus influenzae SR27914 clinical isolate assessed as growth inhibition by CLSI broth microdilution method2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID1374171Antibacterial activity against Staphylococcus aureus ATCC 43300 incubated at 37 degC for 20 hrs by agar dilution method2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Design, synthesis and antibacterial evaluation of honokiol derivatives.
AID285073Antimicrobial activity against viridans group Streptococcus anginosus at 0.25 ug/ml by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
AID637978Antibacterial activity against Staphylococcus aureus ATCC 25923 after overnight incubation by twofold broth dilution technique2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.
AID1303420Antibacterial activity against vancomycin-resistant Enterococcus faecium infected in po dosed immunosuppressed mouse model assessed as inhibition of systemic infection administered bid for 3 days2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria.
AID1194831Antibacterial activity against Staphylococcus aureus ATCC 292135 incubated for 16 hrs by agar dilution method2015Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
Synthesis and structure-activity relationship studies of novel [6,6,5] tricyclic oxazolidinone derivatives as potential antibacterial agents.
AID1168005Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate 10177 after overnight incubation by two-fold serial dilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of novel peptide BF2 as an antibacterial agent against clinical isolates of vancomycin-resistant enterococci.
AID245104In vitro minimum inhibitory concentration against vancomycin-resistant Enterococcus faecium NCTC 122022005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Effects of positional and geometrical isomerism on the biological activity of some novel oxazolidinones.
AID297127Antibacterial activity against Staphylococcus aureus FDA209P after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID581030Bacteriostatic activity against Staphylococcus aureus ATCC 25923 at 8 times MIC after 30 hrs by time-kill analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Mode of action of Ranbezolid against staphylococci and structural modeling studies of its interaction with ribosomes.
AID753113Antibacterial activity against Bacillus subtilis MTCC 121 assessed as growth inhibition at 20 mg/mL after 24 hrs2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID444259Antibacterial activity against Staphylococcus aureus ATCC 25923 by NCCLS method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis and biological activity of novel oxazolidinones.
AID533404Antimicrobial activity against Clostridium subterminale assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID304009AUC (0 to 24 hrs) in Sprague-Dawley rat plasma at 40 mg/kg/day after 14 days2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound.
AID576402Terminal half-life in two-compartment pharmacokinetic/pharmacodynamic model at 200 mg, bid administered as 0.5 hrs infusion2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
AID542688fT>MIC in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 100 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID245196Minimum inhibitory concentration against heterogeneously methicillin-resistant Staphylococcus aureus A272182005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Synthesis and antibacterial activity of dihydro-1,2-oxazine and 2-pyrazoline oxazolidinones: novel analogs of linezolid.
AID542679fCmax in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 800 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID1180587Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC2398-1F to MIC for Staphylococcus aureus ARC23982014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1327117Antitubercular activity against dormant stage Mycobacterium tuberculosis H37Ra at 30 ug/ml measured after 12 days by XTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Design, synthesis and biological evaluation of novel azaspiro analogs of linezolid as antibacterial and antitubercular agents.
AID1361112Bactericidal activity against vancomycin-intermediate Staphylococcus aureus NRS1 clinical isolate preincubated for 20 hrs followed by TSA plating and measured after 18 hrs2018European journal of medicinal chemistry, Jul-15, Volume: 155N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria.
AID519085Antimicrobial activity against Escherichia coli KM85-86 harboring Lys157Gln mutation in rplC gene by agar dilution method in presence of 16 ug/ml polymyxin B nonapeptide2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Linezolid and tiamulin cross-resistance in Staphylococcus aureus mediated by point mutations in the peptidyl transferase center.
AID542684fAUC (24 hrs) in Bacillus anthracis infected in vitro hollow fiber PK/PD model at simulated dose of 500 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
AID575048Cmin in medical patient plasma at 600 mg, iv or 600 mg, po administered every 12 hrs by HPLC2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID558504Antimicrobial activity against methicillin-resistant Staphylococcus aureus 547 measured on day 20 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1271224Antibacterial activity against Streptococcus pneumoniae ATCC 6303 by microbroth dilution method2015ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11
Design, Synthesis, and Identification of Silicon Incorporated Oxazolidinone Antibiotics with Improved Brain Exposure.
AID283622Antimicrobial activity against Enterococcus faecium 3 with homozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID541064AUC (0 to 24 hrs) in cage fluid of Albino guiena pig at 25 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID561244Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as resistant isolates by CLSI M100-S17 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
AID205586Compound was evaluated for minimum inhibitory concentration against Staphylococcus epidermidis 9759 strain2002Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
Synthesis and antibacterial activity of linezolid analogues.
AID387461Half life in Swiss albino mouse at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel and potent oxazolidinone antibacterials featuring 3-indolylglyoxamide substituents.
AID562392Antimicrobial activity against Staphylococcus haemolyticus clinical isolates assessed as percent susceptible isolates by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Comparative in vitro activity profile of oritavancin against recent gram-positive clinical isolates.
AID1180584Ratio of MIC for 2 times drug resistance selected Staphylococcus aureus ARC1692-2F to MIC for Staphylococcus aureus ARC16922014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).
AID1596561Bactericidal activity against Staphylococcus aureus NRS107 assessed as reduction in bacterial cell growth incubated for 18 to 20 hrs followed by re-plating on tryptic soy agar plates at 37 degC for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID562166Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 543 by macrodilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
AID1151626Toxicity in female rat assessed as effect on mean corpuscular hemoglobin level at 100 mg/kg/day, po bid administered for 4 weeks (Rvb = 19.5 pg)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
AID1311361Antibacterial activity against Enterobacter cloacae ATCC 13047 measured after 18 hrs by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID1233138Antibacterial activity against patient-derived methicillin-resistant Staphylococcus aureus 7386 after 18 to 20 hrs by microbroth dilution method2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Thiol activated prodrugs of sulfur dioxide (SO2) as MRSA inhibitors.
AID745381Antibacterial activity against methicillin-resistant Staphylococcus aureus SR3637 infected in JCL/ICR mouse systemic infection model assessed as mortality administered as po measured over 7 days2013European journal of medicinal chemistry, May, Volume: 63Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
AID1174912Cytotoxicity against human HepG2 cells at 100 ug/ml after 48 hrs by presto-blue staining-based assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles.
AID1400047Bactericidal activity against Enterococcus faecalis ATCC 349 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID373838Antimicrobial activity against vancomycin-intermediate Staphylococcus aureus 504 after 50 passages with vancomycin measured after 10 times antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents.
AID1400036Bactericidal activity against Mycobacterium smegmatis ATCC 607 incubated for 48 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1603312Antimicrobial activity against Escherichia coli SQ110 measured after 16 hrs by broth microdilution method2019ACS medicinal chemistry letters, Mar-14, Volume: 10, Issue:3
Expanded Structure-Activity Studies of Lipoxazolidinone Antibiotics.
AID548471Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 after 48 hrs by Etest2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
AID583884Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus isolate 152 by broth microdilution assay2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Comparative efficacies of human simulated exposures of telavancin and vancomycin against methicillin-resistant Staphylococcus aureus with a range of vancomycin MICs in a murine pneumonia model.
AID528835Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID532807Antibacterial activity against vancomycin-susceptible Staphylococcus aureus BR1 after 24 hrs by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Improved antimicrobial activity of linezolid against vancomycin-intermediate Staphylococcus aureus.
AID283615Antimicrobial activity against Enterococcus faecium Ho 5114-0276 with heterozygous 23S rRNA G2576U mutation2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
AID1904922Antibacterial activity against Vancomycin-resistant Staphylococcus aureus 12 incubated for 18 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1161140Antimicrobial activity against Staphylococcus epidermidis after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,741)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's43 (1.15)18.2507
2000's1307 (34.94)29.6817
2010's1720 (45.98)24.3611
2020's671 (17.94)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 113.60

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index113.60 (24.57)
Research Supply Index8.33 (2.92)
Research Growth Index5.87 (4.65)
Search Engine Demand Index211.03 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (113.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials222 (5.67%)5.53%
Reviews457 (11.67%)6.00%
Case Studies730 (18.64%)4.05%
Observational50 (1.28%)0.25%
Other2,457 (62.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (146)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Evaluator-Blinded, Phase 2 Study to Compare the Safety and Efficacy of PTK 0796 With Linezolid (Zyvox®) in the Treatment of Adults With Complicated Skin and Skin Structure Infection (cSSSI) [NCT03716024]Phase 2234 participants (Actual)Interventional2007-07-18Completed
Patient-reported Experiences and Quality of Life Outcomes in the TB-PRACTECAL Clinical Trial [NCT03942354]Phase 2/Phase 354 participants (Anticipated)Interventional2019-09-01Recruiting
Population Pharmacokinetics of Linezolid in Intensive Care Units Patients Treated for Methicillin-Resistant Staphylococcus Aureus (MRSA) Infections [NCT01200654]Phase 460 participants (Actual)Interventional2007-11-30Completed
A Multicenter, Randomized, Double-blind, Parallel-group, Clinical Study of S-649266 Compared With Meropenem for the Treatment of Hospital-acquired Bacterial Pneumonia, Ventilator-associated Bacterial Pneumonia, or Healthcare-associated Bacterial Pneumonia [NCT03032380]Phase 3300 participants (Actual)Interventional2017-10-24Completed
Retrospective Real-word Study of Linezolid for the Treatment of Tuberculous Meningitis [NCT03898635]150 participants (Anticipated)Observational2018-01-01Recruiting
Evaluating Newly Approved Drugs for Multidrug-resistant TB (endTB): A Clinical Trial [NCT02754765]Phase 3754 participants (Actual)Interventional2016-12-31Completed
A Phase 3 Randomized, Double-Blind, Multi-Center Study to Compare the Safety and Efficacy of Oral Omadacycline to Oral Linezolid for Treating Adult Subjects With Acute Bacterial Skin and Skin Structure Infection (ABSSSI) [NCT02877927]Phase 3735 participants (Actual)Interventional2016-08-31Completed
Pilot Study of Linezolid for Early Syphilis Treatment [NCT05548426]Phase 224 participants (Anticipated)Interventional2023-09-28Recruiting
Single-Dose Linezolid Pharmacokinetics In Critically Ill Patients With Impaired Renal Function Especially Chronic Haemodialysis Patients [NCT02087566]18 participants (Actual)Interventional2013-10-31Completed
Linezolid or Vancomycin Surgical Site Infection Prophylaxis [NCT05571722]Phase 41,160 participants (Anticipated)Interventional2023-04-03Not yet recruiting
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
A Randomized, Observer-blinded, Active-controlled, Phase Illb Study to Compare IV / Oral Delafloxacin Fixed-dose Monotherapy With Best Available Treatments in a Microbiologically Enriched Population With Surgical Site Infections [NCT04042077]Phase 3268 participants (Actual)Interventional2019-09-25Terminated(stopped due to COVID-19 seriously affected the study execution as required by the protocol)
Cost Study of Linezolid Versus Vancomycin Among Previously Hospitalized Patients [NCT01363271]7,260 participants (Actual)Observational2011-05-31Completed
Cost Effectiveness Of Linezolid Vs Vancomycin In The Treatment Of Ventilator Acquired Pneumonia In Central America [NCT01040585]0 participants (Actual)Observational2010-07-31Withdrawn
Linezolid In The Treatment Of Subjects With Nosocomial Pneumonia Proven To Be Due To Methicillin-Resistant Staphylococcus Aureus [NCT00084266]Phase 41,225 participants (Actual)Interventional2004-10-31Completed
A Phase 3, Randomized, Double-Blind, Double-Dummy Study to Compare the Efficacy and Safety of Lefamulin (BC 3781) Versus Moxifloxacin (With or Without Adjunctive Linezolid) in Adults With Community-Acquired Bacterial Pneumonia [NCT02559310]Phase 3551 participants (Actual)Interventional2015-09-30Completed
The Incidence of Linezolid-induced Thrombocytopenia (LIT) in Critically Ill Patients, the Risk Factors for LIT and Time to Events (LIT, Recovery) [NCT05944445]310 participants (Anticipated)Observational2023-07-13Recruiting
A Randomized, Controlled, Double-Blind, Double Dummy, Multicenter Phase 2 Study of the Safety/Tolerability and Efficacy of JNJ-32729463 Compared With Linezolid (Zyvox) for the Treatment of Complicated Skin and Skin Structure Infection [NCT01128530]Phase 2161 participants (Actual)Interventional2010-06-30Completed
Six- Versus Twelve-Week Therapy for Non-Surgically-Treated Diabetic Foot Osteomyelitis: A Multicenter Open-Label Controlled Randomized Study [NCT02123628]Phase 440 participants (Actual)Interventional2007-06-30Completed
Population Pharmacokinetics of Meropenem and Linezolid in Children With Severe Infectious Diseases [NCT03643497]800 participants (Anticipated)Observational [Patient Registry]2018-07-01Recruiting
Evaluating Newly Approved Drugs in Combination Regimens for Multidrug-Resistant TB With Fluoroquinolone Resistance (endTB-Q) [NCT03896685]Phase 3323 participants (Actual)Interventional2020-04-06Active, not recruiting
A Randomized, Double-blind, Multi-center Study to Evaluate the Safety and Efficacy of Oral Sodium Fusidate (CEM-102) Compared to Oral Linezolid in the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT02570490]Phase 3716 participants (Actual)Interventional2015-11-30Completed
A Phase 2, Partially-blinded, Randomised Trial Assessing the Safety and Efficacy of TBAJ876 or Bedaquiline, in Combination With Pretomanid and Linezolid in Adult Participants With Newly Diagnosed, Drug-sensitive, Smear-positive Pulmonary Tuberculosis [NCT06058299]Phase 2300 participants (Anticipated)Interventional2023-10-31Not yet recruiting
A Seamless Phase 2B/C Platform Trial to Evaluate Multiple Regimens and Durations of Treatment in Pulmonary Tuberculosis [NCT06114628]Phase 22,500 participants (Anticipated)Interventional2023-12-08Not yet recruiting
A Phase 3, Double-blinded, Randomized, Comparator Trial of the Safety and Efficacy of a Single Dose of Dalbavancin to Twice Daily Linezolid for the Treatment of Community Acquired Bacterial Pneumonia [NCT02269644]Phase 30 participants (Actual)Interventional2015-11-30Withdrawn
A Phase 3 Randomized Double-Blind Study Of Ceftobiprole Medocaril Versus Linezolid Plus Ceftazidime In The Treatment Of Nosocomial Pneumonia [NCT00229008]Phase 3106 participants (Actual)Interventional2005-11-30Completed
A Phase 2, Randomized, Double-blind, Multi-center Study to Evaluate the Safety and Efficacy of CEM-102 Compared to Linezolid in the Treatment of Acute Bacterial Skin Structure Infections [NCT00948142]Phase 2198 participants (Actual)Interventional2009-08-31Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) [NCT04310930]Phase 2/Phase 3300 participants (Anticipated)Interventional2020-03-02Recruiting
Phase IIA Trial of the Safety and Tolerability of Increased Dose Rifampicin and Adjunctive Linezolid With or Without Aspirin, for HIV-associated Tuberculous Meningitis [NCT03927313]Phase 252 participants (Actual)Interventional2019-06-12Completed
Postoperative Antibiotic Management Duration Following Surgery for Intravenous Drug Abuse (IVDA) Endocarditis (OPTIMAL) [NCT05156437]Phase 420 participants (Anticipated)Interventional2022-03-16Enrolling by invitation
A Phase 2, Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of Contezolid Acefosamil Compared to Linezolid Administered Intravenously and Orally to Adult Subjects With Acute Bacterial Skin and Skin Structure Infection [NCT03747497]Phase 2196 participants (Actual)Interventional2018-11-15Completed
Pharmacokinetics/Pharmacodynamics of Oral Linezolid 300 mg/Day in Healthy Volunteers [NCT03841721]Phase 130 participants (Actual)Interventional2018-05-01Active, not recruiting
Oral and Neuro-Penetrative Alternative Antibiotics for Patients With Syphilis [NCT05069974]Phase 3224 participants (Anticipated)Interventional2021-10-14Recruiting
Comparing Oral Versus Parenteral Antimicrobial Therapy (COPAT) Trial [NCT05977868]Phase 4135 participants (Anticipated)Interventional2023-08-04Enrolling by invitation
A Multicenter, Randomized, Double-blind, Placebo-controlled Phase II Clinical Study of the Efficacy and Safety of 9MW1411 Injection Combined With Antibiotics in Patients With Acute Staphylococcus Aureus Skin and Skin Structure Infection [NCT05339802]Phase 290 participants (Anticipated)Interventional2022-02-16Recruiting
A Phase 3, Multicenter, Randomized, Double-Blind, Comparator-Controlled Study to Evaluate the Safety and Efficacy of Intravenous to Oral Delafloxacin in Adult Subjects With Community-Acquired Bacterial Pneumonia [NCT02679573]Phase 3860 participants (Actual)Interventional2016-12-14Completed
A Randomized, Double-Blind, Multicenter Study of Ceftobiprole Medocaril Versus Placebo in the Treatment of Subjects Hospitalized With Community-Acquired Pneumonia [NCT00326287]Phase 3638 participants (Actual)Interventional2006-06-30Completed
Comparative Effectiveness of Adjunctive Clindamycin Versus Linezolid for β-lactam Treated Patients With Invasive Group A Streptococcal Infections: A Target Trial Emulation [NCT06126263]1,000 participants (Anticipated)Observational2023-01-01Active, not recruiting
Linezolid vs Vancomycin/Cefazolin in the Treatment of Hemodialysis Patients With Catheter-Related Gram-Positive Bloodstream Infections [NCT00108433]Phase 361 participants (Actual)Interventional2005-09-30Terminated(stopped due to See Detailed Description)
A Multicenter,Investigator-blinded,Randomized, Comparative Study to Evaluate the Efficacy and Safety of Oral NXL103 Versus Oral Linezolid in the Treatment of Acute Bacterial Skin and Skin Structure Infections (ABSSSI) [NCT00949130]Phase 2180 participants (Actual)Interventional2009-11-30Completed
A Phase 1, Double-Blind, Randomized, Placebo-Controlled Study To Evaluate The Safety, Tolerability, Pharmacokinetics And Pharmacodynamics Of PNU-100480 (PF-02341272) After Administration Of Multiple Escalating Oral Doses To Healthy Adult Subjects [NCT00990990]Phase 159 participants (Actual)Interventional2009-10-31Completed
Determination of Pharmacokinetic and Therapeutic Adaptation of Linezolid in the Treatment of Multi-Resistant Tuberculosis MDR-TB [NCT02778828]31 participants (Actual)Interventional2015-11-04Completed
Antibiotics in Cerebrospinal Fluid Following Intravenous Injection [NCT00925093]Phase 10 participants (Actual)Interventional2011-09-30Withdrawn(stopped due to Primary investigator left institution)
A Double-Blind, Placebo and Active Controlled, Single and Multiple Rising Dose, Safety, Tolerance, and Pharmacokinetic Study of TR-701 in Normal Healthy Adults [NCT00671814]Phase 180 participants (Actual)Interventional2008-01-06Completed
Linezolid Pharmacokinetics and Pharmacodynamics in the Treatment of Multi-Drug Resistant and Extensively-Drug Resistant Tuberculosis [NCT00691392]Phase 1/Phase 226 participants (Actual)Interventional2009-04-30Completed
Prospective Study Of Ophthalmologic Function In Patients Receiving Linezolid For Six Weeks Or Greater [NCT00359632]Phase 334 participants (Actual)Interventional2008-11-30Terminated(stopped due to Study was stopped due to poor enrollment on 28 Feb 2012. Reason for termination was not due to safety concerns.)
A Randomized, Double-Blind, Double Dummy, Comparative, Multicenter Study to Assess the Safety and Efficacy of Topical Retapamulin Ointment, 1%, Versus Oral Linezolid in the Treatment of Secondarily-Infected Traumatic Lesions and Impetigo Due to Methicilli [NCT00852540]Phase 3410 participants (Actual)Interventional2009-04-30Completed
TBTC Study 30: A Phase I/II Pilot Study for Evaluation of Low Dose, Once Daily, Linezolid Plus Optimized Background Therapy (OBT) Versus Placebo Plus OBT for the Treatment of Multi-drug Resistant Tuberculosis [NCT00664313]Phase 1/Phase 236 participants (Actual)Interventional2009-04-30Completed
A Randomized, Evaluator-Blinded, Phase 3 Study to Compare the Safety and Efficacy of PTK 0796 With Linezolid in the Treatment of Adults With Complicated Skin and Skin Structure Infection [NCT00865280]Phase 3143 participants (Actual)Interventional2009-04-04Terminated(stopped due to Terminated)
Pharmacokinetics and Pharmacodynamics Sub-study for TB-PRACTECAL Clinical Trial ( PRACTECAL-PKPD) [NCT04081077]Phase 2/Phase 3240 participants (Anticipated)Interventional2019-08-06Active, not recruiting
Antibiotic Pharmacokinetics in Critically Ill Patients [NCT02609646]1,500 participants (Actual)Observational2016-01-31Completed
Prospective Study Evaluating Plasma Exposure of Optimized Antibiotic Therapy According to TDM in Patients With Subarachnoid Haemorrhage (ES) and Cerebral Haemorrhage (EC) [NCT04132115]104 participants (Anticipated)Observational2019-10-01Recruiting
A Randomised, Controlled, Open-Label, Phase II-III Trial to Evaluate the Safety and Efficacy of Regimens Containing Bedaquiline and Pretomanid for the Treatment of Adult Patients With Pulmonary Multidrug Resistant Tuberculosis [NCT02589782]Phase 2/Phase 3552 participants (Actual)Interventional2017-01-31Active, not recruiting
Randomized Clinical Trial to Compare a Regimen of Trimethoprim-sulfamethoxazole (TMP-SMX) Plus Rifampicin With a Regimen of Linezolid in the Treatment of Infections Caused by Methicillin-resistant Staphylococcus Aureus (MRSA) [NCT00711854]Phase 4150 participants (Actual)Interventional2009-01-31Completed
Linezolid vs. Vancomycin/Oxacillin/Dicloxacillin in the Treatment of Catheter-Related Gram-Positive Bloodstream Infections [NCT00037050]Phase 3739 participants (Actual)Interventional2002-04-30Completed
Repurposing Clinically Approved Drugs for Yaws With an Insight Into the Cutaneous Ulcer Disease Syndrome (Trep-AByaws) [NCT05764876]Phase 3360 participants (Anticipated)Interventional2023-03-14Recruiting
A Randomized, Evaluator-Blinded, Phase 3 Study to Compare the Safety and Efficacy of PTK 0796 With Linezolid in the Treatment of Adults With Complicated Skin and Skin Structure Infection [NCT00876850]Phase 30 participants (Actual)Interventional2009-07-31Withdrawn(stopped due to Terminated)
An Open Label, Single Dose, 2-Way, Randomized Cross-Over Bioequivalence Study Comparing Linezolid 600 Mg Oral Suspension With 600 Mg Tablet In Chinese Healthy Male Subjects [NCT01055769]Phase 120 participants (Actual)Interventional2010-03-31Completed
A Multicenter, Randomized, Observer-Blinded, Active-Controlled Study to Evaluate the Safety, Tolerability, Efficacy, and Pharmacokinetics of Ceftaroline Versus Comparator in Pediatric Subjects With Acute Bacterial Skin and Skin Structure Infections [NCT01400867]Phase 2/Phase 3163 participants (Actual)Interventional2011-12-31Completed
Delamanid, Linezolid, Levofloxacin, and Pyrazinamide for the Treatment of Patients With Fluoroquinolone-sensitive MDR-TB: A Phase 2/3, Multicenter, Randomized, Open-label, Clinical Trial [NCT02619994]Phase 2238 participants (Anticipated)Interventional2016-01-31Recruiting
Drug Use Investigation Of Zyvox (Linezolid) (Regulatory Post Marketing Commitment Plan) [NCT00666276]1,004 participants (Actual)Observational2007-02-28Completed
The Effects of Linezolid and Vancomycin on Inflammation and Cellular Signaling Vents [NCT00811980]60 participants (Actual)Observational2009-01-31Completed
Linezolid (PNU-10766/PNU10766SS) in the Treatment of MRSA Infections in Patients Whose Conventional Therapy Has Failed, or Who Are Intolerant to Conventional Therapy; an Open-label, Multi-center Trial [NCT00150332]Phase 324 participants (Actual)Interventional2003-01-31Completed
A Phase 2, Multicenter, Randomized, Open-Label, Comparative Study to Evaluate the Safety and Efficacy of RX-1741 Versus Linezolid in the Outpatient Treatment of Adult Patients With Uncomplicated Skin and Skin Structure Infection [NCT00646958]Phase 2150 participants (Actual)Interventional2007-12-31Completed
A Single Center Four Part Study in Healthy Adult Subjects to Evaluate: the Safety, Tolerability and Pharmacokinetics of a Single Oral Dose and Repeat Escalating Oral Doses of GSK945237; the Effect of Linezolid on Hematology Safety Parameters; and the Effe [NCT01039610]Phase 10 participants (Actual)Interventional2009-11-30Withdrawn(stopped due to Internal decision to progress alternate molecule with more preferable profile)
Randomized, Open Label, Multiple Dose Phase I Study of the Early Bactericidal Activity of Linezolid, Gatifloxacin, Levofloxacin, and Moxifloxacin in HIV-non-infected Adults With Initial Episodes of Sputum Smear-Positive Pulmonary Tuberculosis [NCT00396084]Phase 1/Phase 270 participants (Actual)Interventional2004-02-10Completed
Linezolid in the Treatment of Subjects With Complicated Skin and Soft Tissue Infections Proven to be Due to Methicillin-Resistant Staphylococcus Aureus [NCT00087490]Phase 41,077 participants (Actual)Interventional2004-10-31Completed
Evaluation of the Early Bactericidal Activity of Tedizolid and Linezolide Against Mycobacterium Tuberculosis [NCT05534750]Phase 260 participants (Anticipated)Interventional2023-04-20Recruiting
Substitution of Ethambutol With Linezolid During the Intensive Phase of Treatment of Pulmonary Tuberculosis: A Prospective, Multicenter, Randomized, Open-label Phase II Trial [NCT01994460]Phase 2429 participants (Anticipated)Interventional2014-01-31Recruiting
A Randomized, Open Label, Multi-Center Clinical Trial, Comparing Microbiologic Response To Linezolid And Vancomycin In Ventilator-Associated Pneumonia (VAP) Due To Methicillin Resistant Staphylococcus Aureus (MRSA) [NCT00572559]Phase 4149 participants (Actual)Interventional2002-11-30Completed
Efficacy and Safety of Continuous Infusion of Linezolid Compared With Intermittent Dosing in Critically Ill Pneumonic Patients [NCT04531332]169 participants (Anticipated)Interventional2019-11-15Recruiting
A Randomized, Controlled, Multi-center Clinical Trial of Short Course Treatment for Newly Diagnosed Rifampicin Resistant Tuberculosis [NCT04545788]200 participants (Anticipated)Interventional2020-08-01Recruiting
Pharmacokinetics and Tolerability of Adjunctive Linezolid for the Treatment of Tuberculous Meningitis [NCT04021121]Phase 260 participants (Anticipated)Interventional2021-05-05Active, not recruiting
A Phase 2a, Randomized, 2-Arm, Open-Label, Clinical Trial of the Efficacy of Linezolid Combined With Antituberculous Therapy in Subjects With Extensively Drug-Resistant (XDR) Pulmonary Tuberculosis [NCT00727844]Phase 241 participants (Actual)Interventional2008-07-31Completed
Economic Evaluation of New MDR TB Regimens (PRACTECAL EE) [NCT04207112]Phase 2/Phase 3200 participants (Anticipated)Interventional2020-10-20Recruiting
A Phase 3 Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of 6-Day Oral TR-701 Free Acid and 10-Day Oral Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT01170221]Phase 3667 participants (Actual)Interventional2010-08-15Completed
An Open-label, Placebo-controlled Phase 1 Study to Evaluate the Effect of Linezolid on Ex Vivo Neutrophil and Monocyte Function in Healthy Male Subjects [NCT01544673]Phase 118 participants (Actual)Interventional2012-03-31Completed
A Prospective, Randomized, Open, Active-controlled, Interventional, Exploratory, Phase II Trial to Evaluate the EBA, Safety and PK of Orally Administered LCB01-0371 in Adult Patients With Smear-positive Pulmonary Tuberculosis [NCT02836483]Phase 279 participants (Actual)Interventional2016-12-10Completed
An Investigator Initiated, Phase IV Single-Center, Randomized, Open-Label, Prospective Study to Determine the Impact of Serial Procalcitonin on Improving Antimicrobial Stewardship and on the Efficacy, Safety, and Tolerability of Imipenem - Relebactam Plus [NCT04983901]Phase 2100 participants (Actual)Interventional2021-09-14Active, not recruiting
[NCT01756924]Phase 214 participants (Actual)Interventional2012-12-31Terminated(stopped due to This study has been terminated; alternative study designs are being considered. Fusidic acid remains available under an Expanded Access Protocol.)
Antibiotic Concentrations in Serum and Epithelial Lining Fluid Under Continous Infusion [NCT00435305]40 participants (Anticipated)Observational2006-11-30Terminated(stopped due to difficulties by enrolling patients fundings consumed, no staff could be recruited and payed to continue enrolling patients,)
Short Intervention and Measurement of Pharmacokinetics of Linezolid in Tuberculosis Meningitis: a Pharmacokinetics and Safety/Tolerability Study [NCT03537495]Phase 236 participants (Actual)Interventional2021-06-21Completed
A Phase 2 Exploratory Study of Objective Endpoints in Subjects With Acute Bacterial Skin and Skin Structure Infections Treated With Delafloxacin, Vancomycin, or Linezolid [NCT01283581]Phase 2256 participants (Actual)Interventional2011-01-31Completed
Refining MDR-TB Treatment (T) Regimens (R) for Ultra(U) Short(S) Therapy(T) (TB-TRUST)-PLUS [NCT04717908]89 participants (Actual)Interventional2021-01-20Active, not recruiting
Phase 3, Randomized, Investigator-Blind, Multi-Center Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Linezolid in Complicated Skin and Skin Structure Infections (ASSIST-2) [NCT00303550]Phase 30 participants Interventional2006-03-31Completed
Prospective,Randomized,Open Label,European Multicenter Study of the Efficacy of the Linezolid-rifampin Combination Versus Standard of Care in the Treatment of Gram-positive. [NCT01757236]Phase 2100 participants (Anticipated)Interventional2012-10-31Recruiting
A Randomized, Double Blind, Double Dummy Multicenter Phase IIa Study to Assess Safety, Tolerability and Efficacy of GSK1322322 Versus Linezolid in the Treatment of Acute Bacterial Skin and Skin Structure Infection [NCT01209078]Phase 284 participants (Actual)Interventional2010-08-17Completed
Clinical Usefulness of Mic/Breakpoint Ratio and Penetration in Tissues. A Prospective Study of Clinical Validation [NCT01551719]0 participants (Actual)Interventional2012-03-31Withdrawn
A Phase I Clinical Study, Randomized, Double-blind, Placebo-controlled, Single Dose, Dose Escalation Study of the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of LCB01-0371 in Healthy Male Subjects [NCT01554995]Phase 170 participants (Actual)Interventional2012-03-31Completed
A Randomized, Double-Blind Trial Comparing Linezolid To Vancomycin In The Empiric Treatment Of Febrile Neutropenic Oncology Patients With Suspected Gram-Positive Infections [NCT00035425]Phase 3120 participants (Actual)Interventional2001-11-30Completed
Linezolid IV/PO for the Treatment of Vancomycin-Resistant Enterococcus Infections in Children [NCT00035854]Phase 313 participants (Actual)Interventional2002-02-28Completed
Time To Efficacy and Onset Of Action Of Linezolid In Skin and Soft Tissue Infections [NCT00147511]Phase 4118 participants (Actual)Interventional2003-06-30Completed
Concentration and Antibiotic Activity in Antibiotic Lock Solutions [NCT01592032]Phase 4125 participants (Anticipated)Interventional2012-05-31Active, not recruiting
A Phase 3 Partially-blinded, Randomized Trial Assessing the Safety and Efficacy of Various Doses and Treatment Durations of Linezolid Plus Bedaquiline and Pretomanid in Participants With Pulmonary Infection of Either Extensively Drug-resistant Tuberculosi [NCT03086486]Phase 3181 participants (Actual)Interventional2017-11-21Completed
"DART: Sivextro® in Acute Bacterial Skin anD Skin Structure Infection (ABSSSI) in Hospitalized Patients. A Global ObseRvational STudy." [NCT02991131]108 participants (Actual)Observational2016-12-17Terminated(stopped due to Company decision)
Single Dose Safety, Tolerability And Pharmacokinetics Of Escalating Intravenous Doses Of Linezolid Followed By Evaluation Of The Effect Of Single Intravenous Doses Of Linezolid On QTc Interval In Healthy Subjects [NCT00795145]Phase 149 participants (Actual)Interventional2008-12-31Completed
A Phase 2, Multicenter, Randomized, Double-blind Study to Evaluate the Safety and Efficacy of MRX-I Versus Linezolid in Adult Subjects With Acute Bacterial Skin and Skin Structure Infection [NCT02269319]Phase 2120 participants (Actual)Interventional2015-02-28Completed
Clinical Implication of Next Generation Sequencing of Urinary Bacteria in Patients With Low Colony Forming Units of Bacteria in Traditional Urine Culture [NCT05206500]Phase 4100 participants (Anticipated)Interventional2022-05-17Recruiting
An Open Label Parallel Group Study To Investigate The Pharmacokinetics Of Intravenous Linezolid, An Oxazolidinone, Administered To Healthy Volunteers And Patients With Major Thermal Injuries [NCT00255996]Phase 116 participants (Actual)Interventional2006-05-31Completed
Zyvox (Linezolid) Special Investigation For Vancomycin-Resistant Enterococci (VRE)(Regulatory Post Marketing Commitment Plan) [NCT01224626]41 participants (Actual)Observational2006-05-31Completed
Pharmacokinetic and Pharmacodynamic Evaluation of Linezolid Administered Intravenously in MRSA-positive, Morbidly Obese Patients With Pneumonia [NCT01805284]Phase 415 participants (Actual)Interventional2013-02-28Completed
A Phase 2 Dose-ranging Trial to Evaluate the Bactericidal Activity, Safety, Tolerability and Pharmacokinetics of Linezolid in Adult Subjects With Newly Diagnosed Drug-Sensitive, Smear-Positive Pulmonary Tuberculosis. [NCT02279875]Phase 2113 participants (Actual)Interventional2014-11-30Completed
Phase 3, Randomized, Investigator-Blind, Multi-Center Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Linezolid in Complicated Skin and Skin Structure Infections.(ASSIST-1) [NCT00299520]Phase 30 participants Interventional2005-06-30Completed
Continuous Infusion Versus Intermittent Administration of Linezolid - Impact on Clinical Outcome and Adverse Reactions in Critically Ill Patients: a Pharmacokinetic and Pharmacodynamic Prospective Study [NCT05801484]60 participants (Anticipated)Interventional2022-07-01Recruiting
A Phase 3, Randomized, Double-Blind, Double-Dummy Study to Compare the Efficacy and Safety of Dalbavancin to a Comparator Regiment (Vancomycin and Linezolid) for the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT01339091]Phase 3573 participants (Actual)Interventional2011-03-31Completed
Early Oral Switch Therapy in Low-risk Staphylococcus Aureus Bloodstream Infection [NCT01792804]Phase 3215 participants (Actual)Interventional2013-12-31Completed
A Pragmatic Randomized Controlled Trial to Evaluate the Efficacy and Safety of an Oral Short-course Regimen Including Bedaquiline for the Treatment of Patients With Multidrug-resistant Tuberculosis in China [NCT05306223]Phase 4212 participants (Anticipated)Interventional2022-05-10Recruiting
A Phase 2, Multicenter, Randomized, Open-label, Comparative Study to Evaluate the Efficacy and Safety of Intramuscular Ceftaroline Versus Intravenous Linezolid in Adult Subjects With Complicated Skin and Skin Structure Infections [NCT00633152]Phase 2150 participants (Actual)Interventional2008-02-29Completed
A Phase 3, Randomized, Double-Blind, Double-Dummy Study to Compare the Efficacy and Safety of Dalbavancin to a Comparator Regimen (Vancomycin and Linezolid) for the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT01431339]Phase 3739 participants (Actual)Interventional2011-07-31Completed
Clinical Outcomes Among a National Veterans Affairs Methicillin Resistant Staphylococcus Aureus (MRSA) Pneumonia Cohort Treated With Linezolid Or Vancomycin [NCT01819935]5,271 participants (Actual)Observational2012-12-31Completed
Safety and Efficacy of Strategy to Prevent Drug-Induced Nephrotoxicity in High-Risk Patients [NCT01734694]Phase 4100 participants (Actual)Interventional2011-10-31Terminated(stopped due to Independent biostatistician recommended early termination of the trial due to low probability of success.)
Antimicrobial Treatment in Patients With Ventilator-associated Tracheobronchitis: a Prospective Randomized Placebo-controlled Double-blind Multicenter Trial [NCT03012360]Phase 4154 participants (Anticipated)Interventional2018-02-08Recruiting
Population Pharmacokinetics of Commonly Used Antimicrobial Agents in Children of Bacterial Meningitis With Augmented Renal Clearance [NCT04771884]300 participants (Anticipated)Observational2020-10-01Recruiting
A Phase 3 Randomized Double-blind Study Comparing TR-701 FA and Linezolid in Ventilated Gram-positive Nosocomial Pneumonia [NCT02019420]Phase 3726 participants (Actual)Interventional2014-01-06Completed
Pharmacokinetics of Linezolid in Children With Cystic Fibrosis [NCT00625703]Phase 245 participants (Actual)Interventional2010-12-31Completed
Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis [NCT03474198]Phase 2/Phase 3675 participants (Actual)Interventional2018-03-21Completed
Prospective, Randomized, Open Label Phase 3 Study of the Efficacy and Tolerability of Delamanid, Linezolid, Pyrazinamide and Levofloxacin for Treatment of Patients With Fluoroquinolone-susceptible Multidrugresistant--Tuberculosis (MDR-TB) [NCT02975570]Phase 30 participants (Actual)Interventional2017-08-31Withdrawn(stopped due to The study could not be conducted since funding was not obtained.)
A Prospective Implementation of an IV-oral Switch Policy to Treat Proven or Suspected Infections Due to Resistant Gram Positive Bacteria in a London Hospital Trust [NCT00501150]211 participants (Actual)Interventional2005-09-30Completed
An Open Label, Randomized Controlled Trial to Establish the Efficacy and Safety of a Study Strategy Consisting of 6 Months of Bedaquiline (BDQ), Delamanid (DLM), and Linezolid (LNZ), With Levofloxacin (LVX) and Clofazimine (CFZ) Compared to the Current So [NCT04062201]Phase 3402 participants (Actual)Interventional2019-08-22Active, not recruiting
Asymptomatic Colonization With S. Aureus After Therapy With Linezolid or Clindamycin for Acute S. Aureus Skin and Skin Structure Infections in Patients With Comorbid Conditions: A Randomized Trial [NCT01619410]25 participants (Actual)Interventional2012-01-31Terminated(stopped due to slow accrual)
A Multicenter, Randomized, Open-Label Study To Evaluate The Efficacy And Safety Of A Contezolid, Delamanid and Bedaquiline-Containing Short Regimen For The Treatment Of Rifampicin-Resistant Pulmonary Tuberculosis [NCT06081361]Phase 3186 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Prospective, Randomized, Partially Blinded, Phase 2 Study of the Efficacy and Tolerability of Bedaquiline, Delamanid, Levofloxacin, Linezolid, and Clofazimine for Treatment of Patients With MDR-TB [NCT03828201]Phase 2220 participants (Anticipated)Interventional2022-06-07Recruiting
Multicenter, Retrospective, Observational Study to Evaluate Clinical and Economic Outcomes of Patients With MRSA Hospital-Acquired Pneumonia Treated With Linezolid Or Vancomycin [NCT01561469]188 participants (Actual)Observational2008-11-30Completed
A Phase III Randomized Double-Blind Study Of Ceftobiprole Versus Linezolid Plus Ceftazidime In The Treatment Of Nosocomial Pneumonia [NCT00210964]Phase 3781 participants (Actual)Interventional2005-04-30Completed
A Phase III, Randomized, Double-Blind, Active Comparator-Controlled Clinical Trial to Study the Safety, Tolerability, and Efficacy of Imipenem/Cilastatin/Relebactam (MK-7655A) Versus Piperacillin/Tazobactam in Subjects With Hospital-Acquired Bacterial Pne [NCT02493764]Phase 3537 participants (Actual)Interventional2015-11-24Completed
Impact of Aggressive Empiric Antibiotic Therapy and Duration of Therapy on the Emergence of Antimicrobial Resistance During the Treatment of Hospitalized Subjects With Pneumonia Requiring Mechanical Ventilation [NCT01570192]Phase 243 participants (Actual)Interventional2010-09-30Terminated(stopped due to NIAID terminated the study due to low subject enrollment)
A Phase 3 Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of IV to Oral 6-Day TR-701 Free Acid and IV to Oral 10-Day Linezolid for the Treatment of ABSSSI [NCT01421511]Phase 3666 participants (Actual)Interventional2011-09-15Completed
A Phase II, Prospective, Randomized, Multicenter Trial to Evaluate the Efficacy and Safety/Tolerability of Two Linezolid Dosing Strategies in Combination With a Short Course Regimen for the Treatment of Drug-Resistant Pulmonary Tuberculosis [NCT05007821]Phase 2132 participants (Anticipated)Interventional2022-08-11Recruiting
A Prospective, Randomized, Open-label, Active-controlled, Multicenter Study to Evaluate the Efficacy and Safety of BAY 1192631 in Japanese Patients With MRSA Infections (Skin and Soft Tissue Infection [SSTI] and SSTI-related Bacteremia) [NCT01967225]Phase 3125 participants (Actual)Interventional2013-11-23Completed
A Phase III, Multi-centre, Randomized Study to Compare the Efficacy and Safety of Levonadifloxacin (IV and Oral) With Linezolid (IV and Oral) in Acute Bacterial Skin and Skin Structure Infections (ABSSSI) [NCT03405064]Phase 3501 participants (Actual)Interventional2017-08-25Completed
A Phase 3, Multicenter, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of Contezolid Acefosamil and Contezolid Compared to Linezolid Administered Intravenously and Orally to Adults With Moderate or Severe Diabetic Foot Infections (DFI) [NCT05369052]Phase 3865 participants (Anticipated)Interventional2022-05-03Recruiting
Evaluating a New Treatment Regimen for Patients With Multidrug-resistant TB (MDR-TB) - a Prospective Open-label Randomised Controlled Trial [NCT02454205]Phase 2/Phase 3154 participants (Actual)Interventional2015-11-12Completed
Post Marketing Surveillance on the Efficacy, Safety and Tolerability of Linezolid (Zyvox) in the Treatment of Gram Positive Infections [NCT01564758]99 participants (Actual)Observational2004-02-29Completed
A Phase 3 Open-label Trial Assessing the Safety and Efficacy of Bedaquiline Plus PA-824 Plus Linezolid in Subjects With Pulmonary Infection of Either Extensively Drug-resistant Tuberculosis (XDR-TB) or Treatment Intolerant / Non-responsive Multi-drug Resi [NCT02333799]Phase 3109 participants (Actual)Interventional2015-03-31Completed
Phase 3 Study of IV to Oral 6-Day Tedizolid Phosphate Compared With 10-day Comparator in Subjects 12 to < 18 Years With cSSTI. [NCT02276482]Phase 3120 participants (Actual)Interventional2015-03-25Completed
Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis [NCT05398679]Phase 4360 participants (Anticipated)Interventional2022-06-01Not yet recruiting
A Phase 2, Randomized, Double-Blind, Multicenter Study of Safety, Tolerability, and Efficacy of Debio 1450 vs Vancomycin (IV)/Linezolid (Oral) in the Treatment of Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Due to Staphylococcus Sensitive [NCT02426918]Phase 2330 participants (Actual)Interventional2015-05-31Completed
A Single-Center, Randomized, Open-label, Prospective, Comparative Study to Determine the Efficacy, Safety, and Tolerability of Ceftazidime-Avibactam (CAZ-AVI) Plus Vancomycin or Linezolid Versus Standard of Care Plus Vancomycin or Linezolid as Empiric The [NCT02732327]Phase 22 participants (Actual)Interventional2016-05-17Terminated(stopped due to No longer aligned with the revised clinical development plan and commercial strategy)
A Phase 3 Randomized, Double-blind, Multi-center Study to Compare the Safety and Efficacy of Omadacycline IV/PO to Linezolid IV/PO for Treating Adults With Acute Bacterial Skin and Skin Structure Infections (ABSSSI) [NCT02378480]Phase 3655 participants (Actual)Interventional2015-06-30Completed
A Phase II, Randomized, Open-Label Trial of a Six-Month Regimen of High-Dose Rifampicin, High-Dose Isoniazid, Linezolid, and Pyrazinamide Versus a Standard Nine-Month Regimen for the Treatment of Adults and Adolescents With Tuberculous Meningitis: Improve [NCT05383742]Phase 2330 participants (Anticipated)Interventional2024-01-02Not yet recruiting
Evaluate the Effectiveness, Safety and Tolerability of Various Doses of Linezolid in Combination With Bedaquiline and Pretomanid in Adults With Pre-Extensively Drug-Resistant (Pre-XDR), Or Treatment Intolerant/Non-responsive Multidrug-Resistant (MDRTI/NR) [NCT05040126]Phase 3400 participants (Anticipated)Interventional2021-10-07Recruiting
A Multi-national Phase 3, Randomized, Double-Blind, Active Comparator-Controlled Clinical Trial to Study the Safety, Tolerability, and Efficacy of Imipenem/Cilastatin/Relebactam (MK-7655A) Versus Piperacillin/Tazobactam in Subjects With Hospital-Acquired [NCT03583333]Phase 3274 participants (Actual)Interventional2018-09-18Completed
A Phase 3 Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of Intravenous to Oral 6-Day Tedizolid Phosphate and Intravenous to Oral 10-Day Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections [NCT02066402]Phase 3598 participants (Actual)Interventional2014-03-04Completed
Efficacy and Safety of Continuous Versus Intermittent Linezolid Infusion in Critically Ill Patients With Septic Shock [NCT05813951]140 participants (Anticipated)Interventional2022-12-02Recruiting
Efficacy of Oral Antibiotic Therapy Compared to Intravenous Antibiotic Therapy for the Treatment of Diabetic Foot Osteomyelitis (CRO-OSTEOMYELITIS) [NCT02168816]Phase 230 participants (Actual)Interventional2014-03-19Terminated(stopped due to The study was stopped for feasibility (i.e., low recruitment))
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00084266 (15) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOT for mITT Population
NCT00084266 (15) [back to overview]Clinical Outcome in Participants With Baseline Methicillin Resistant Staphylococcus Aureus (MRSA) at End of Study (EOS) for PP Population
NCT00084266 (15) [back to overview]Survival Status Estimated by Kaplan-Meier Analysis for ITT Population
NCT00084266 (15) [back to overview]Survival Status Estimated by Kaplan-Meier Analysis for mITT Population
NCT00084266 (15) [back to overview]Survival Status Estimated by Kaplan-Meier Analysis for PP Population
NCT00084266 (15) [back to overview]Clinical Outcome in Participants With Baseline MRSA at EOT for mITT Population
NCT00084266 (15) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOS for mITT Population
NCT00084266 (15) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOS for PP Population
NCT00084266 (15) [back to overview]Number of Participants With Clinical Signs and Symptoms at EOS for mITT Population
NCT00084266 (15) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOT for PP Population
NCT00084266 (15) [back to overview]Number of Participants With Clinical Signs and Symptoms at EOS for PP Population
NCT00084266 (15) [back to overview]Number of Participants With Clinical Signs and Symptoms at EOT for mITT Population
NCT00084266 (15) [back to overview]Number of Participants With Clinical Signs and Symptoms at EOT for PP Population
NCT00084266 (15) [back to overview]Clinical Outcome in Participants With Baseline MRSA at End of Treatment (EOT) for PP Population
NCT00084266 (15) [back to overview]Clinical Outcome in Participants With Baseline MRSA at EOS for mITT Population
NCT00087490 (14) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOT for mITT Population
NCT00087490 (14) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOT for PP Population
NCT00087490 (14) [back to overview]Number of Participants With Clinical Signs and Symptoms at EOT and EOS for mITT Population
NCT00087490 (14) [back to overview]Number of Participants With Clinical Signs and Symptoms at EOT and EOS for PP Population
NCT00087490 (14) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOS for mITT Population
NCT00087490 (14) [back to overview]Clinical Outcome in Participants With Baseline MRSA at EOT for mITT Population
NCT00087490 (14) [back to overview]Clinical Outcome in Participants With Baseline MRSA at EOS for Modified-Intent to Treat (mITT) Population
NCT00087490 (14) [back to overview]Clinical Outcome in Participants With Baseline Methicillin-Resistant Staphylococcus Aureus (MRSA) at End of Study (EOS) for Per-Protocol (PP) Population
NCT00087490 (14) [back to overview]Duration of Intravenous Therapy for PP Population
NCT00087490 (14) [back to overview]Duration of Intravenous Therapy for mITT Population
NCT00087490 (14) [back to overview]Duration of Hospital Stay for PP Population
NCT00087490 (14) [back to overview]Clinical Outcome in Participants With Baseline MRSA at End of Treatment (EOT) for PP Population
NCT00087490 (14) [back to overview]Duration of Hospital Stay for mITT Population
NCT00087490 (14) [back to overview]Microbiological Outcome in Participants With Baseline MRSA at EOS for PP Population
NCT00359632 (2) [back to overview]Percentage of Participants With an Adverse Event
NCT00359632 (2) [back to overview]Percentage of Participants by Clinical Outcome of Infection at End of Study
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration (Cmax)
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC)
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC) Adjusted for Free Drug Concentrations
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentrations (Cmax), Adjusted for Free Drug Concentration
NCT00396084 (19) [back to overview]Percent Dosing Interval Above Minimum Inhibitory Concentration (MIC)
NCT00396084 (19) [back to overview]Area Under the Curve (AUC) Adjusted for Free Drug Concentrations/Minimum Inhibitory Concentration (MIC)
NCT00396084 (19) [back to overview]Area Under the Curve (AUC) During First 12 and 24 Hours Adjusted for Free Drug Concentrations
NCT00396084 (19) [back to overview]Pharmacokinetic Parameters: Area Under the Curve During First 12 and 24 Hours
NCT00396084 (19) [back to overview]Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)
NCT00396084 (19) [back to overview]Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)
NCT00396084 (19) [back to overview]Time to Maximum Plasma Drug Concentration (Tmax) and Half-life
NCT00396084 (19) [back to overview]Time to Maximum Plasma Drug Concentration (Tmax) and Half-life
NCT00396084 (19) [back to overview]Pharmacokinetic Parameters: Area Under the Curve (AUC) During First 12 and 24 Hours
NCT00396084 (19) [back to overview]Area Under the Curve During First 12 or 24 Hours / Minimum Inhibitory Concentration (AUC/MIC)
NCT00396084 (19) [back to overview]Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Fluoroquinolones/Isoniazid (INH) Comparison
NCT00396084 (19) [back to overview]Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Linezolid Once Daily/Linezolid Twice Daily/Isoniazid (INH) Comparison
NCT00396084 (19) [back to overview]Difference in Sputum Bacillary Loads: Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Linezolid Once Daily/Linezolid Twice Daily/INH Comparison
NCT00396084 (19) [back to overview]Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Fluoroquinolones/Isoniazid (INH) Comparison
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration (Cmax)
NCT00633152 (2) [back to overview]Clinical Response at the Test-of-Cure (TOC) Visit in the Clinically Evaluable (CE) Population
NCT00633152 (2) [back to overview]Clinical Response at the Test of Cure (TOC) Visit in the Modified Intent-to-treat (MITT) Population
NCT00646958 (2) [back to overview]Number of Participants With a Clinical Response of Cure
NCT00646958 (2) [back to overview]Number of Patients With Per-Patient Microbiologic Response of Eradicated
NCT00666276 (11) [back to overview]Number of Participants With Adverse Drug Reaction Not Expected From the Japanese Package Insert.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Route of Administration.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Age
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Concomitant Drugs.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Hepatic Dysfunctions.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Duration of Drug Administration.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Gender.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Non-drug Therapies.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Renal Dysfunctions.
NCT00666276 (11) [back to overview]Factors Considered to Affect the Safety of Linezolid - Weight.
NCT00666276 (11) [back to overview]Number of Participants With Adverse Drug Reactions(ADRs).
NCT00727844 (1) [back to overview]Number of Patients Converted to Sputum Culture Negative in Each Arm, With Data Censored at 4 Months.
NCT00795145 (15) [back to overview]Cohort 2: Mean Time-Matched Difference in Time Corresponding to Beginning of Depolarization to Repolarization of the Ventricles, Corrected for Heart Rate Using Fridericia's Formula (QTcF Interval) Between Linezolid 600 mg and 1200 mg Compared to Placebo
NCT00795145 (15) [back to overview]Cohort 1: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC Inf) and Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC Last)
NCT00795145 (15) [back to overview]Cohort 1: Time to Reach Maximum Observed Plasma Concentration (Tmax) and Plasma Decay Half-Life (t1/2)
NCT00795145 (15) [back to overview]Cohort 2: AUC Inf and AUC Last
NCT00795145 (15) [back to overview]Cohort 1: Number of Subjects With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00795145 (15) [back to overview]Cohort 2: Vss
NCT00795145 (15) [back to overview]Cohort 2: Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin and Placebo
NCT00795145 (15) [back to overview]Cohort 2: Cmax
NCT00795145 (15) [back to overview]Cohort 2: CL
NCT00795145 (15) [back to overview]Cohort 1: Steady-State Volume of Distribution (Vss)
NCT00795145 (15) [back to overview]Cohort 1: Maximum Observed Plasma Concentration (Cmax)
NCT00795145 (15) [back to overview]Cohort 2: Mean Time-Matched Difference in Uncorrected QT Intervals Between Linezolid 600 mg and 1200 mg Compared to Placebo
NCT00795145 (15) [back to overview]Cohort 2: Number of Subjects With AEs and SAEs
NCT00795145 (15) [back to overview]Cohort 2: Tmax and t1/2
NCT00795145 (15) [back to overview]Cohort 1: Clearance of Linezolid (CL)
NCT00852540 (11) [back to overview]Number of Baseline Pathogens With the Indicated Microbiological Outcome at the End of Therapy
NCT00852540 (11) [back to overview]Number of Participants With the Indicated Clinical Outcome at the End of Therapy
NCT00852540 (11) [back to overview]Number of Participants With the Indicated Clinical Outcome at the End of Therapy Who Had MRSA as a Baseline Pathogen
NCT00852540 (11) [back to overview]Number of Participants Achieving Clinical Response at Follow-up Who Had Methicillin-resistant Staphlococcus Aureus (MRSA) as a Baseline Pathogen
NCT00852540 (11) [back to overview]Number of Participants Achieving Microbiological Response (MR) at Follow-up (FU) Who Had MRSA as a Baseline Pathogen (BP)
NCT00852540 (11) [back to overview]Number of Participants Who Achieved Microbiological Response (MR) at Follow-up (FU) Who Had a Baseline Pathogen (BP)
NCT00852540 (11) [back to overview]Number of Participants With Clinical Response at Follow-up
NCT00852540 (11) [back to overview]Number of Participants With Therapeutic Response at Follow-up
NCT00852540 (11) [back to overview]Mean Scores on the Skin Infection Rating Scale at Visits 1, 2, 3, 4, and 5
NCT00852540 (11) [back to overview]Mean Wound Size at Visits 1, 2, 3, 4, and 5
NCT00852540 (11) [back to overview]Number of Participants With the Indicated Microbiological Outcome at the End of Therapy Who Had MRSA as a Baseline (BL) Pathogen
NCT00865280 (7) [back to overview]Number of Participants With the Indicated Type of Adverse Event (AE)
NCT00865280 (7) [back to overview]Number of Participants With Wound Infections Classified as a Sponsor-defined Clinical Success in the CE Population at Test of Cure
NCT00865280 (7) [back to overview]Number of Participants Classified as a Sponsor-defined Clinical Success in the Intent-to-Treat (ITT) Population at End of Treatment
NCT00865280 (7) [back to overview]Number of Participants Classified as a Sponsor-defined Clinical Success in the ITT Population at Test of Cure
NCT00865280 (7) [back to overview]Number of Participants With Cellulitis Classified as a Sponsor-defined Clinical Success in the CE Population at End of Treatment
NCT00865280 (7) [back to overview]Number of Participants With Cellulitis Classified as a Sponsor-defined Clinical Success in the CE Population at Test of Cure
NCT00865280 (7) [back to overview]Number of Participants With Wound Infections Classified as a Sponsor-defined Clinical Success in the Clinically Evaluable (CE) Population at End of Treatment
NCT01055769 (5) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0-∞)]
NCT01055769 (5) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
NCT01055769 (5) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax)
NCT01055769 (5) [back to overview]Terminal Half-Life (t1/2)
NCT01055769 (5) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT01170221 (8) [back to overview]Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit in the Clinically Evaluable-End of Therapy Analysis Sets
NCT01170221 (8) [back to overview]Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit.
NCT01170221 (8) [back to overview]Early Clinical Response Rate
NCT01170221 (8) [back to overview]Investigator's Assessment of Clinical Response at the 48-72 Hour Visit
NCT01170221 (8) [back to overview]Investigator's Assessment of Clinical Response at the Day 7 Visit
NCT01170221 (8) [back to overview]Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit
NCT01170221 (8) [back to overview]Change From Baseline in Patient-reported Pain, by Study Visit
NCT01170221 (8) [back to overview]To Compare the Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit in the Clinically Evaluable-Post Treatment Evaluation Analysis Set
NCT01209078 (37) [back to overview]Mean Exudate or Pus Sub-score of SIS at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Hematology Parameter of Hemoglobin, Mean Corpuscle Hemoglobin Concentration (MCHC) at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Hematology Parameter of Mean Corpuscle Hemoglobin (MCH) at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Hematology Parameter of Mean Corpuscle Volume (MCV) at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Hematology Parameter of Red Blood Cell (RBC) Count and Reticulocyte Count at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Hematology Parameters of Basophils, Eosinophils, Lymphocytes, Monocytes, Total Neutrophils, White Blood Cells (WBC) and Platelet Count at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Short Form McGill Pain Questionnaire-2 (SF-MPQ-2) Sub-score of Continuous Pain, Intermittent Pain, Neuropathic Pain and Affective Descriptors at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Total SIS at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Vital Sign Value of Heart Rate (HR) at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Vital Sign Value of Respiratory Rate (RR) at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Vital Sign Value of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Indicated Time Points
NCT01209078 (37) [back to overview]Number of Participants With Abnormal Transition From Baseline in Clinical Chemistry Values Relative to Normal Range
NCT01209078 (37) [back to overview]Number of Participants With Abnormal Transition From Baseline in Hematology Values Relative to Normal Range
NCT01209078 (37) [back to overview]Number of Participants With Any Adverse Events (AE) and Serious Adverse Events (SAE)
NCT01209078 (37) [back to overview]Number of Participants With Clinical Success of Clinical Response
NCT01209078 (37) [back to overview]Percentage of Participants With Clinical Success at End of Therapy by Pathogen Isolated at Baseline
NCT01209078 (37) [back to overview]Percentage of Participants With Clinical Success at End of Therapy by Pathogen Isolated at Baseline
NCT01209078 (37) [back to overview]Percentage of Participants With Clinical Success of Clinical Outcome
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameter of Estradiol at Indicated Time Point
NCT01209078 (37) [back to overview]Percentage of Participants With Microbiological Success of Microbiological Outcome at End of Therapy
NCT01209078 (37) [back to overview]Percentage of Participants With Microbiological Success of Microbiological Outcome at Follow-up
NCT01209078 (37) [back to overview]Percentage of Participants With Therapeutic Success of Therapeutic Outcome
NCT01209078 (37) [back to overview]Mean Change From Baseline in ECG Rhythms at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Change From Baseline in ECG Values at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Change From Baseline in HR at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Change From Baseline in RR at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Change From Baseline in SBP and DBP at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Change From Baseline in Total SIS at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Change From Baseline in Wound Area at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameter of High Sensitivity C-Reactive Protein at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameters of Albumin and Total Protein at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameters of ALT, Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Follicle Stimulating Hormone (FSH), Gamma Glutamyl Transferase (GGT), Lactate Dehydrogenase (LDH) and Creatine Kinase at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameters of ALT, Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Follicle Stimulating Hormone (FSH), Gamma Glutamyl Transferase (GGT), Lactate Dehydrogenase (LDH) and Creatine Kinase at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameters of Creatinine, Uric Acid, Direct Bilirubin and Total Bilirubin at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Clinical Chemistry Parameters of Glucose, Sodium, Calcium, Potassium, Chloride, Carbon Dioxide (CO2) Content /Bicarbonate and Urea/ Blood Urea Nitrogen (BUN) at Indicated Time Points
NCT01209078 (37) [back to overview]Mean ECG Rhythms at Indicated Time Points
NCT01209078 (37) [back to overview]Mean Electrocardiogram (ECG) Values at Indicated Time Points
NCT01224626 (3) [back to overview]Adverse Drug Reactions Unlisted in Japanese Package Insert.
NCT01224626 (3) [back to overview]Number of Participants Categorized as Responders (Cure and Improved) to Zyvox (Linezolid) Treatment.
NCT01224626 (3) [back to overview]Number of Participants With Adverse Drug Reactions.
NCT01283581 (5) [back to overview]Pharmacokinetic (PK) Parameter, Area Under Curve, (AUCinf, ug*h/mL), in Subjects Administered Delafloxacin, Vancomycin, and Linezolid
NCT01283581 (5) [back to overview]Erythema Clinical Success
NCT01283581 (5) [back to overview]The Levels of Inflammation Were Examined by Measuring a Surrogate, C-Reactive Protein (CRP)
NCT01283581 (5) [back to overview]Investigator's Assessment of Clinical Response in the ITT (Intent-to-treat) Population at Follow-up
NCT01283581 (5) [back to overview]Clinical Response in Subjects With Infections Caused by MRSA - Microbiological ITT (MITT) Population
NCT01339091 (4) [back to overview]Clinical Status
NCT01339091 (4) [back to overview]Clinical Status
NCT01339091 (4) [back to overview]>= 20% Reduction in Lesion Area
NCT01339091 (4) [back to overview]Early Clinical Efficacy
NCT01421511 (8) [back to overview]Investigator's Assessment of Clinical Response at the 48-72 Hour Visit
NCT01421511 (8) [back to overview]Change From Baseline in Patient-reported Pain, by Study Visit
NCT01421511 (8) [back to overview]The Early Clinical Response Rate
NCT01421511 (8) [back to overview]Investigator's Assessment of Clinical Success of the Post Therapy Evaluation Visit in Clinically Evaluable-Post Treatment Evaluation Analysis Set.
NCT01421511 (8) [back to overview]Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit
NCT01421511 (8) [back to overview]Investigator's Assessment of Clinical Response at the Day-7 Visit
NCT01421511 (8) [back to overview]Clinical Response at the End of Therapy Visit
NCT01421511 (8) [back to overview]Clinical Response at the End of Therapy Visit in the Clinically Evaluable at End of Therapy Analysis Set
NCT01431339 (4) [back to overview]Early Clinical Efficacy
NCT01431339 (4) [back to overview]Clinical Status
NCT01431339 (4) [back to overview]Clinical Status
NCT01431339 (4) [back to overview]>= 20% Reduction in Lesion Area
NCT01561469 (6) [back to overview]Duration of Hospital Stay
NCT01561469 (6) [back to overview]Duration of Intensive Care Unit (ICU) Stay
NCT01561469 (6) [back to overview]Duration of Mechanical Ventilation
NCT01561469 (6) [back to overview]Percentage of Participants With Clinical Success
NCT01561469 (6) [back to overview]Number of Participants With Microbiological Outcome
NCT01561469 (6) [back to overview]Duration of Antimicrobial Treatment
NCT01564758 (2) [back to overview]Number of Participants With Clinical Response
NCT01564758 (2) [back to overview]Number of Participants With Adverse Events (AEs)
NCT01570192 (9) [back to overview]Number of Participants With Suppression and Emergence of Resistance
NCT01570192 (9) [back to overview]Occurrence of Repeat Negative Cultures
NCT01570192 (9) [back to overview]Clinical Response
NCT01570192 (9) [back to overview]Suppression of the Emergence of Resistance in Other Gram-negative Pathogens
NCT01570192 (9) [back to overview]Pretreatment Pathogen Response
NCT01570192 (9) [back to overview]Overall Microbiologic Response
NCT01570192 (9) [back to overview]Clinical Response in Subjects Who Received Prior Antibiotics
NCT01570192 (9) [back to overview]Mortality
NCT01570192 (9) [back to overview]Mortality
NCT01619410 (1) [back to overview]Number of Participants With Presence of Staphylococcus Aureus After Treatment With Linezolid Versus Clindamycin
NCT01734694 (2) [back to overview]Proportion of Individuals With Acute Kidney Injury Network Modified Definition of Nephrotoxicity
NCT01734694 (2) [back to overview]Proportion of Individuals With Nephrotoxicity
NCT01819935 (8) [back to overview]Clinical Success
NCT01819935 (8) [back to overview]Time to 30-day Methicillin-Resistant Staphylococcus Aureus (MRSA) Re-infection
NCT01819935 (8) [back to overview]Time to 30-day Mortality
NCT01819935 (8) [back to overview]Time to Discharge From the Hospital
NCT01819935 (8) [back to overview]Time to Intubation
NCT01819935 (8) [back to overview]Time to Therapy Change
NCT01819935 (8) [back to overview]Time to Transfer Out From the Intensive Care Unit (ICU)
NCT01819935 (8) [back to overview]Time to 30-day Re-admission
NCT01967225 (6) [back to overview]Change of the Lesion Size From the Screening Visit by Visit (Only Skin and Soft Tissue Infection [SSTI])
NCT01967225 (6) [back to overview]Clinical Response at End of Treatment Visit (EOT)
NCT01967225 (6) [back to overview]Clinical Response at Test of Cure (TOC)
NCT01967225 (6) [back to overview]Microbiological Response at End of Treatment (EOT)
NCT01967225 (6) [back to overview]Reduction Ratio of the Lesion Size From the Screening Visit to Day 3 to Day 4 Visit (Only Skin and Soft Tissue Infection [SSTI])
NCT01967225 (6) [back to overview]Microbiological Response at Test of Cure (TOC)
NCT02019420 (12) [back to overview]Number of Methicillin-Resistant Staphylococcus Aureus (MRSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]Number of Methicillin-Susceptible Staphylococcus Aureus (MSSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]Number of Participants Discontinuing Study Therapy Due to an Adverse Event (AE)
NCT02019420 (12) [back to overview]Number of Participants With ≥1 Adverse Events (AEs)
NCT02019420 (12) [back to overview]Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiologically-Evaluable 1 (ME-1) Population
NCT02019420 (12) [back to overview]Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiologically-Evaluable 2 (ME-2) Population
NCT02019420 (12) [back to overview]Number of Participants With All-Cause Mortality in the Intent-to-Treat (ITT) Population
NCT02019420 (12) [back to overview]Number of Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population
NCT02019420 (12) [back to overview]Clinical Response at Test of Cure (TOC) Visit in the Clinically-Evaluable (CE) Population
NCT02019420 (12) [back to overview]Clinical Response at Test of Cure (TOC) Visit in the Intent-to-Treat (ITT) Population
NCT02019420 (12) [back to overview]Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiological Intent-to-Treat (mITT) Population
NCT02066402 (11) [back to overview]Value of the Visual Analog Scale (VAS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]Percentage of Participants With Early Clinical Response at 48-72 Hours After the First Infusion of Study Drug in the ITT Analysis Set.
NCT02066402 (11) [back to overview]Value of the Faces Rating Scale (FRS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]Change From Baseline in the Faces Rating Scale (FRS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]Change From Baseline in the Visual Analog Scale (VAS) Pain Scores at Each Time Point
NCT02066402 (11) [back to overview]Investigator's Assessment of Clinical Response at 48-72 Hours
NCT02066402 (11) [back to overview]Investigator's Assessment of Clinical Response at Day 7 Visit
NCT02066402 (11) [back to overview]Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the Clinically Evaluable at Post Therapy Evaluation (CE-PTE) Analysis Set
NCT02066402 (11) [back to overview]Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the ITT Analysis Set
NCT02066402 (11) [back to overview]Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the Clinically Evaluable at EOT (CE-EOT) Analysis Set
NCT02066402 (11) [back to overview]Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the ITT Analysis Set
NCT02276482 (9) [back to overview]Number of Participants With Adverse Events on Tedizolid Phosphate and Comparator Drugs
NCT02276482 (9) [back to overview]Change From Baseline in Lesion Size
NCT02276482 (9) [back to overview]Peak Plasma Concentration (Cmax) of Tedizolid
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at TOC Visit (Clinically Evaluable-Test of Cure [CE-TOC] Analysis Set)
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at Test of Cure (TOC) Visit (Intent to Treat Analysis Set)
NCT02276482 (9) [back to overview]Area Under the Plasma Concentration Versus Time Curve Time 0 to 24 Hours (AUC0-24h) of Tedizolid
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at End of Therapy (EOT) Visit (Intent to Treat Analysis Set)
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at EOT Visit (Clinically Evaluable-End of Therapy [CE-EOT] Analysis Set)
NCT02276482 (9) [back to overview]Number of Participants With Early Clinical Responses Measured by Lesion Reduction
NCT02378480 (4) [back to overview]Number of Participants With Early Clinical Response
NCT02378480 (4) [back to overview]Number of Participants With the Indicated Investigator Assessment of Clinical Response in the Clinically Evaluable-Post Therapy Evaluation (CE-PTE) Population
NCT02378480 (4) [back to overview]Number of Participants With the Indicated Investigator Assessment of Clinical Response in the mITT Population at the Post Therapy Evaluation (PTE) Visit
NCT02378480 (4) [back to overview]Number of Participants With the Indicated Type of Adverse Event (AE)
NCT02426918 (5) [back to overview]Percentage of Participants Who Showed Microbiological Evidence of Cure 48 to 72 Hours From Randomization, EOT, and STFU
NCT02426918 (5) [back to overview]Clinical Success Rate: Percentage of Participants Assessed by the Sponsor as Responders After 7 to 10 Days of Treatment at EOT and STFU
NCT02426918 (5) [back to overview]Clinical Success Rate: Percentage of Participants Assessed by the Investigator as Responders at 48 to 72 Hours From Randomization, at End of Treatment (EOT) and Short-term Follow-up (STFU)
NCT02426918 (5) [back to overview]Early Clinical Response Rate (ECRR): Percentage of Responders to Treatment at 48 to 72 Hours From Randomization as Assessed by the Investigator
NCT02426918 (5) [back to overview]Percentage of Participants With a Composite Assessment of Clinical Outcome (CACO) of Success
NCT02493764 (22) [back to overview]Percentage of Participants With ACM in the Microbiological Modified Intention-to-treat (mMITT) Population
NCT02493764 (22) [back to overview]Percentage of Participants With All-cause Mortality (ACM) Through Day 28 in the Modified Intention-to-treat (MITT) Population
NCT02493764 (22) [back to overview]Percentage of Participants in the CE Population With a FCR at OTX2 (Day 6)
NCT02493764 (22) [back to overview]Percentage of Participants in the CE Population With a FCR at EOT Visit
NCT02493764 (22) [back to overview]Percentage of Participants in the CE Population With a FCR at EFU Visit
NCT02493764 (22) [back to overview]Percentage of Participants in the CE Population With a FCR at OTX3 (Day 10)
NCT02493764 (22) [back to overview]Percentage of Participants Discontinuing Study Therapy Due to an AE
NCT02493764 (22) [back to overview]Percentage of Participants in the MITT Population With a FCR at OTX1 (Day 3)
NCT02493764 (22) [back to overview]Percentage of Participants in the mMITT Population With a FMR at EFU Visit
NCT02493764 (22) [back to overview]Percentage of Participants in the Clinically Evaluable (CE) Population With a FCR at On-therapy Visit 1 (OTX1) [Day 3]
NCT02493764 (22) [back to overview]Percentage of Participants in the ME Population With a FMR at EFU Visit
NCT02493764 (22) [back to overview]Percentage of Participants in the Microbiologically Evaluable (ME) Population With a FMR at EOT Visit
NCT02493764 (22) [back to overview]Percentage of Participants in the CE Population With a FCR at Day 28
NCT02493764 (22) [back to overview]Percentage of Participants in the MITT Population With a Favorable Clinical Response (FCR) at Early Follow-up (EFU) Visit
NCT02493764 (22) [back to overview]Percentage of Participants in the MITT Population With a FCR at Day 28
NCT02493764 (22) [back to overview]Percentage of Participants in the MITT Population With a FCR at EOT
NCT02493764 (22) [back to overview]Percentage of Participants in the MITT Population With a FCR at OTX2 (Day 6)
NCT02493764 (22) [back to overview]Percentage of Participants in the MITT Population With a FCR at OTX3 (Day 10)
NCT02493764 (22) [back to overview]Percentage of Participants in the mMITT Population With a Favorable Microbiological Response (FMR) at End of Treatment (EOT) Visit
NCT02493764 (22) [back to overview]Percentage of Participants With ≥1 Adverse Event (AE)
NCT02493764 (22) [back to overview]Percentage of Participants With ACM at EFU in the MITT Population
NCT02493764 (22) [back to overview]Percentage of Participants With ACM at EFU in the mMITT Population
NCT02559310 (1) [back to overview]Early Clinical Response (ECR)
NCT02679573 (4) [back to overview]All-cause Mortality
NCT02679573 (4) [back to overview]Early Clinical Response
NCT02679573 (4) [back to overview]Early Clinical Response Plus Improvement in Vital Signs and no Worsening of the 4 Symptoms
NCT02679573 (4) [back to overview]Microbiologic Response
NCT02877927 (3) [back to overview]Number of Participants With Early Clinical Response
NCT02877927 (3) [back to overview]Number of Participants With the Indicated Investigator Assessment of Clinical Response in the Clinically Evaluable-Post Therapy Evaluation (CE-PTE) Population
NCT02877927 (3) [back to overview]Number of Participants With the Indicated Investigator Assessment of Clinical Response in the mITT Population at the Post Therapy Evaluation (PTE) Visit
NCT03032380 (13) [back to overview]Percentage of Participants With Clinical Cure at Test of Cure
NCT03032380 (13) [back to overview]Percentage of Participants With Clinical Cure at End of Treatment (EOT)
NCT03032380 (13) [back to overview]Percentage of Participants With Clinical Cure at Early Assessment (EA)
NCT03032380 (13) [back to overview]All-cause Mortality Rate at the End of Study
NCT03032380 (13) [back to overview]All-cause Mortality Rate at Day 28
NCT03032380 (13) [back to overview]All-cause Mortality Rate at Day 14
NCT03032380 (13) [back to overview]Total Hospitalization Time
NCT03032380 (13) [back to overview]Percentage of Participants With Sustained Microbiologic Eradication at Follow-up
NCT03032380 (13) [back to overview]Number of Participants With Treatment-Emergent Adverse Events
NCT03032380 (13) [back to overview]Percentage of Participants With Microbiologic Eradication at End of Treatment
NCT03032380 (13) [back to overview]Percentage of Participants With Sustained Clinical Cure at Follow-up (FU)
NCT03032380 (13) [back to overview]Percentage of Participants With Microbiologic Eradication at Test of Cure (TOC)
NCT03032380 (13) [back to overview]Percentage of Participants With Microbiologic Eradication at Early Assessment
NCT03086486 (1) [back to overview]Time to Sputum Culture Conversion to Negative Status Through the Treatment Period
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Clinical Response at End of Therapy (EOT) Visit in the MITT Population
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Clinical Response at EOT Visit in the Clinically Evaluable (CE) Population
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Microbiological Response at EFU Visit in Microbiological-evaluable (ME) Population.
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Microbiological Response at EOT Visit in Microbiological Modified Intent-To-Treat Population (mMITT) Population
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Microbiological Response at EOT Visit in the ME Population
NCT03583333 (10) [back to overview]Percentage of Participants Discontinuing Study Drug Due to AEs
NCT03583333 (10) [back to overview]Percentage of Participants Experiencing Adverse Events (AEs)
NCT03583333 (10) [back to overview]Percentage of Participants With All-cause Mortality Through Day 28 in the Modified Intent to Treat (MITT) Population
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Clinical Response at EFU Visit in the Clinically Evaluable (CE) Population
NCT03583333 (10) [back to overview]Percentage of Participants Achieving a Favorable Clinical Response at Early Follow-up (EFU) Visit in the MITT Population
NCT03716024 (4) [back to overview]Number of Participants With Microbiologic Response in the mITT Population
NCT03716024 (4) [back to overview]Number of Participants With Clinical Response in the Clinically Evaluable (CE) Population
NCT03716024 (4) [back to overview]Number of Participants With Clinical Response in the Modified Intent-to-Treat (mITT) Population
NCT03716024 (4) [back to overview]Number of Participants With Microbiologic Response in the Microbiologically Evaluable (ME) Population
NCT04042077 (5) [back to overview]Microbiological Response
NCT04042077 (5) [back to overview]Number of Participants With Clinical Success at Test Of Cure Visit
NCT04042077 (5) [back to overview]Number of Participants Eligible to Switch to Oral Formulation According to Blinded Observer's Assessment
NCT04042077 (5) [back to overview]Hospital Length of Stay (LOS)
NCT04042077 (5) [back to overview]Hospital Infection Related Length of Stay (IRLOS)

PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.0.15
DTG 50mg q.d.1.25
EVG/COBI 150/150mg q.d.0.91
DRV/COBI 800/150 mg q.d.0.07
ATV/COBI 300/150 mg q.d.0.07
TFV 300mg q.d.0.88

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.55.458.3

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.1.9691.6692.387

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.5.445.10

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. Half-life is defined as 0.693/k, where k, the elimination rate constant, is the slope of the decline in concentrations. (NCT00042289)
Timeframe: Infant plasma samples at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

Interventionhour (Median)
DTG 50mg q.d.32.8
EVG/COBI 150/150mg q.d.7.6
DRV/COBI 800/150 mg q.d.NA
EFV 600 mg q.d. (Outside THA)65.6

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.2.822.203.90
ATV/RTV Arm 1: 300/100mg q.d.NA3.64.1
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.3.114.514.52
DRV/COBI 800/150 mg q.d.4.593.677.04
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.6.226.558.96
DRV/RTV 600/100mg b.i.d.5.645.537.78
DRV/RTV 800/100mg q.d.6.775.788.11
DTG 50mg q.d.3.623.544.85
EFV 600 mg q.d. (Outside THA)3.875.134.41
FPV/RTV 700/100mg b.i.d.5.615.126.75
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)3.893.625.37
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA5.15.0
TFV 300mg q.d.0.2500.2450.298
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.1.22.54.1
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.2.733.565.43

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.701.010.63
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.8.410.714.6
RAL 400mg b.i.d.2.2501.7703.035
RPV 25mg q.d.0.1450.1340.134

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionng/mL (Median)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.448647

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionng/mL (Median)
2nd Trimester3rd TrimesterPostpartum
EVG/COBI 150/150mg q.d.1447.11432.81713.1
TAF 10mg q.d. w/COBI80.491.298.2
TAF 25mg q.d.69.796133
TAF 25mg q.d. w/COBI or RTV Boosting87.8107141

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PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

Interventionng/mL (Geometric Mean)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.108128

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PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.2.842.524.51
DRV/RTV 600/100mg b.i.d.2.122.222.51
FPV/RTV 700/100mg b.i.d.2.121.642.87
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA0.470.52

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PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.360.480.38
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.130.130.28
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.3.75.17.2
RAL 400mg b.i.d.0.06210.0640.0797

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PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

"Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose.~For the TAF 25 mg q.d., 10 mg q.d. w/COBI, and 25 mg q.d. w/COBI or RTV boosting arms, samples were all below the limit of quantification and statistical analyses were not conducted." (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.0.210.210.61
ATV/RTV Arm 1: 300/100mg q.d.2.00.71.2
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.490.710.90
DRV/COBI 800/150 mg q.d.0.330.271.43
DRV/RTV 800/100mg q.d.0.991.172.78
DTG 50mg q.d.0.730.931.28
EFV 600 mg q.d. (Outside THA)1.491.481.94
EVG/COBI 150/150mg q.d.0.02580.04870.3771
TAF 10mg q.d. w/COBI0.001950.001950.00195
TAF 25mg q.d.0.001950.001950.00195
TAF 25mg q.d. w/COBI or RTV Boosting0.001950.001950.00195
TFV 300mg q.d.0.0390.0540.061
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.0.30.50.8
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.440.571.26

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.1.602.05

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.0.0630.0560.081

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. (NCT00042289)
Timeframe: Blood samples were collected at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

,,,
Interventionmcg/mL (Median)
2-10 hours after birth18-28 hours after birth36-72 hours after birth5-9 days after birth
DRV/COBI 800/150 mg q.d.0.351.431.871.72
DTG 50mg q.d.1.731.531.000.06
EFV 600 mg q.d. (Outside THA)1.11.00.90.4
EVG/COBI 150/150mg q.d.0.1320.0320.0050.005

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. For arms with zero overall participants analyzed, samples were below the limit of quantification and ratios could not be calculated. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
TAF 10mg q.d. w/COBI0.97
EFV 600 mg q.d. (Outside THA)0.67
EFV 600mg q.d.0.49
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.0.2
RAL 400mg b.i.d.1.5
ETR 200mg b.i.d.0.52
MVC 150 or 300mg b.i.d.0.33
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.14
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.16
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.0.19
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.12
RPV 25mg q.d.0.55
ATV/RTV 300/100mg q.d. or TFV/ATV/RTV 300/300/100mg q.d.0.18
DRV/RTV 800/100mg q.d. or DRV/RTV 600/100mg b.i.d.0.18

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Plasma Concentration for Contraceptives

Serum concentrations of the contraceptives. Note that no historical controls were provided by team pharmacologists and thus no comparisons were done for contraceptive concentrations in women using hormonal contraceptives and selected ARV drugs as compared to historical controls not using those ARV drugs. (NCT00042289)
Timeframe: Measured at 6-7 weeks after contraceptive initiation postpartum

Interventionpg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG604
LPV/RTV 400/100 b.i.d. With ENG428
EFV 600mg q.d. With ENG125

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Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12h (area-under-the-curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8 and 12 hours post dosing.

Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG115.97100.20

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Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8, 12, and 24 hours post dosing.

,
Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
ATV/RTV/TFV 300/100/300mg q.d. With ENG53.9655.25
EFV 600mg q.d. With ENG53.6456.65

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,
InterventionParticipants (Count of Participants)
3rd TrimesterPostpartum
EFV 600mg q.d.2021
MVC 150 or 300mg b.i.d.87

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,,,,,,,,,,,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
2nd Trimester3rd TrimesterPostpartum
ATV/RTV Arm 1: 300/100mg q.d.11212
DRV/COBI 800/150 mg q.d.3414
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.71622
DRV/RTV 600/100mg b.i.d.71922
DRV/RTV 800/100mg q.d.91922
DTG 50mg q.d.92023
EFV 600 mg q.d. (Outside THA)123334
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.82927
ETR 200mg b.i.d.5137
EVG/COBI 150/150mg q.d.81018
FPV/RTV 700/100mg b.i.d.82622
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)101926
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.93027
ATV/COBI 300/150 mg q.d.125
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA1514
RAL 400mg b.i.d.113330
RPV 25mg q.d.142625
TAF 10mg q.d. w/COBI152322
TAF 25mg q.d.132324
TAF 25mg q.d. w/COBI or RTV Boosting102418
TFV 300mg q.d.22727
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.11112
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.72332

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

Interventionng*hour/mL (Geometric Mean)
2nd Trimester3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.NA27173645

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.55.151.879.6
DRV/RTV 600/100mg b.i.d.45.845.961.7
FPV/RTV 700/100mg b.i.d.43.5032.1551.60
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA34.233.5

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.4.58.35.3
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)14.916.127.1
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.7296133
RAL 400mg b.i.d.6.65.411.6

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24 (area under the curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

,,,,,,,,,,,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.25.3318.8536.20
ATV/RTV Arm 1: 300/100mg q.d.88.241.957.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.30.645.748.8
DRV/COBI 800/150 mg q.d.50.0042.0595.55
DRV/RTV 800/100mg q.d.64.663.5103.9
DTG 50mg q.d.47.649.265.0
EFV 600 mg q.d. (Outside THA)47.3060.0262.70
EVG/COBI 150/150mg q.d.15.314.021.0
TAF 10mg q.d. w/COBI0.1970.2060.216
TAF 25mg q.d.0.1710.2120.271
TAF 25mg q.d. w/COBI or RTV Boosting0.1810.2570.283
TFV 300mg q.d.1.92.43.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.14.528.839.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.26.237.758.7

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Microbiological Outcome in Participants With Baseline MRSA at EOT for mITT Population

Microbiological response assessed at participant level.Eradication:baseline isolate not present in repeat culture from original infection site;Presumed Eradication:clinical response of cure precluded availability of specimen for culture;Persistence:baseline isolate present in repeat culture;Presumed Persistence:culture data not available for participant with clinical response of failure;Superinfection:culture from primary infection site had new pathogen not identified as baseline isolate and clinical response was failure;Indeterminate:any participant who cannot be classified into any of above. (NCT00084266)
Timeframe: EOT (within 72 hours of last dose)

,
InterventionParticipants (Number)
MRSA EradicationPresumed MRSA EradicationMRSA PersistencePresumed MRSA PersistenceMissing/Indeterminate (excluded from analysis)
Linezolid8477192321
Vancomycin656260316

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Clinical Outcome in Participants With Baseline Methicillin Resistant Staphylococcus Aureus (MRSA) at End of Study (EOS) for PP Population

Clinical response was based primarily on global assessment of clinical presentation of participant made by investigator at evaluation timepoint. Clinical response was evaluated at EOS Visit as Cure: resolution of clinical signs/symptoms of pneumonia when compared with baseline; Failure: persistence/progression of baseline signs/symptoms of pneumonia or baseline radiographic abnormalities after atleast 2 days of treatment; development of new pulmonary/extrapulmonary clinical findings consistent with active infection; Unknown:extenuating circumstances precluding classification to 1 of the above. (NCT00084266)
Timeframe: EOS (7-30 days after last dose)

,
InterventionParticipants (Number)
CureFailureUnknown/Missing (excluded from analysis)
Linezolid95707
Vancomycin81932

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Survival Status Estimated by Kaplan-Meier Analysis for ITT Population

For each participant, time to death was estimated from baseline to date of first documented progression or date of death from any cause, whichever came first, assessed up to 60 days after last dose. The distribution of survival was estimated for the treatment groups using the Kaplan-Meier, product-limit method and compared between the treatment groups using the log rank statistic. (NCT00084266)
Timeframe: From baseline until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 60 days after last dose.

InterventionDays (Mean)
Linezolid55.590
Vancomycin55.369

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Survival Status Estimated by Kaplan-Meier Analysis for mITT Population

For each participant, time to death was estimated from baseline to date of first documented progression or date of death from any cause, whichever came first, assessed up to 60 days after last dose. The distribution of survival was estimated for the treatment groups using the Kaplan-Meier, product-limit method and compared between the treatment groups using the log rank statistic. (NCT00084266)
Timeframe: From baseline until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 60 days after last dose.

InterventionDays (Median)
Linezolid58.185
Vancomycin57.072

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Survival Status Estimated by Kaplan-Meier Analysis for PP Population

For each participant, time to death was estimated from baseline to date of first documented progression or date of death from any cause, whichever came first, assessed up to 60 days after last dose. The distribution of survival was estimated for the treatment groups using the Kaplan-Meier, product-limit method and compared between the treatment groups using the log rank statistic. (NCT00084266)
Timeframe: From baseline until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 60 days after last dose.

InterventionDays (Mean)
Linezolid59.196
Vancomycin57.191

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Clinical Outcome in Participants With Baseline MRSA at EOT for mITT Population

Clinical response evaluated at EOT visit as Cure:resolution of clinical sign/symptoms of pneumonia when compared with baseline;Improvement: in 2 or more clinical sign/symptoms of pneumonia when compared with baseline,improvement/lack of progression of all chest X-ray abnormalities,Failure: persistence/ progression of baseline signs/symptoms of pneumonia or baseline radiographic abnormalities after atleast 2 days of treatment; development of new pulmonary/extrapulmonary clinical findings consistent with active infection;Unknown: extenuating circumstances precluding classification to 1 of above. (NCT00084266)
Timeframe: EOT (within 72 hours of last dose)

,
InterventionParticipants (Number)
CureImprovementFailureUnknown/Missing (excluded from analysis)
Linezolid81804023
Vancomycin77686910

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Microbiological Outcome in Participants With Baseline MRSA at EOS for mITT Population

Microbiological response assessed at participant level.Eradication:baseline isolate not present in repeat culture from original infection site;Presumed Eradication:clinical response of cure precluded availability of specimen for culture;Persistence:baseline isolate present in repeat culture;Presumed Persistence:culture data not available for participant with clinical response of failure;Superinfection:culture from primary infection site had new pathogen not identified as baseline isolate and clinical response was failure;Indeterminate:any participant who cannot be classified into any of above. (NCT00084266)
Timeframe: EOS (7-30 days after last dose)

,
InterventionParticipants (Number)
MRSA EradicationPresumed MRSA EradicationMRSA PersistenceMRSA RecurrencePresumed MRSA PersistenceMissing/Indeterminate (excluded from analysis)
Linezolid46659165929
Vancomycin356122127915

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Microbiological Outcome in Participants With Baseline MRSA at EOS for PP Population

Microbiological response assessed at participant level.Eradication:baseline isolate not present in repeat culture from original infection site;Presumed Eradication:clinical response of cure precluded availability of specimen for culture;Persistence:baseline isolate present in repeat culture;Presumed Persistence:culture data not available for participant with clinical response of failure;Superinfection:culture from primary infection site had new pathogen not identified as baseline isolate and clinical response was failure;Indeterminate:any participant who cannot be classified into any of above. (NCT00084266)
Timeframe: EOS (7-30 days after last dose)

,
InterventionParticipants (Number)
MRSA EradicationPresumed MRSA EradicationMRSA PersistenceMRSA RecurrencePresumed MRSA PersistenceMissing/Indeterminate (excluded from analysis)
Linezolid3562715485
Vancomycin26561511662

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Number of Participants With Clinical Signs and Symptoms at EOS for mITT Population

Participant's clinical evaluation of signs and symptoms were based on global assessment by investigator at specific timepoints. Signs and symptoms (mild to severe) of nosocomial pneumonia included cough; production of purulent sputum or change in character of sputum;auscultatory findings on pulmonary examination of rales and/or pulmonary consolidation (dullness on percussion, bronchial breath sounds, or egophony); and dyspnea, tachypnea, or hypoxemia with PaO2 <60 mmHg or worsening gas exchange or increased oxygen requirements; pleuritic chest pain; chills/rigors; and decreased breath sounds. (NCT00084266)
Timeframe: EOS (7-30 days after last dose)

,
InterventionParticipants (Number)
Decreased Breath SoundsHypoxiaPulmonary ConsolidationRalesTachypneaChills/RigorsCoughDyspneaPleuritic Chest PainPurulent Sputum
Linezolid533832364943719748
Vancomycin583827344224023638

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Microbiological Outcome in Participants With Baseline MRSA at EOT for PP Population

Microbiological response assessed at participant level.Eradication:baseline isolate not present in repeat culture from original infection site;Presumed Eradication:clinical response of cure precluded availability of specimen for culture;Persistence:baseline isolate present in repeat culture;Presumed Persistence:culture data not available for participant with clinical response of failure;Superinfection:culture from primary infection site had new pathogen not identified as baseline isolate and clinical response was failure;Indeterminate:any participant who cannot be classified into any of above. (NCT00084266)
Timeframe: EOT (within 72 hours of last dose)

,
InterventionParticipants (Number)
MRSA EradicationPresumed MRSA EradicationMRSA PersistencePresumed MRSA PersistenceMissing/Indeterminate (excluded from analysis)
Linezolid767316171
Vancomycin595550240

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Number of Participants With Clinical Signs and Symptoms at EOS for PP Population

Participant's clinical evaluation of signs and symptoms were based on global assessment by investigator at specific timepoints. Signs and symptoms (mild to severe) of nosocomial pneumonia included cough; production of purulent sputum or change in character of sputum;auscultatory findings on pulmonary examination of rales and/or pulmonary consolidation (dullness on percussion, bronchial breath sounds, or egophony); and dyspnea, tachypnea, or hypoxemia with PaO2 <60 mmHg or worsening gas exchange or increased oxygen requirements; pleuritic chest pain; chills/rigors; and decreased breath sounds. (NCT00084266)
Timeframe: EOS (7-30 days after last dose)

,
InterventionParticipants (Number)
Decreased Breath SoundsHypoxiaPulmonary ConsolidationRalesTachypneaChills/RigorsCoughDyspneaPleuritic Chest PainPurulent Sputum
Linezolid423022273933215536
Vancomycin462919273613319526

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Number of Participants With Clinical Signs and Symptoms at EOT for mITT Population

Participant's clinical evaluation of signs and symptoms were based on global assessment by investigator at specific timepoints. Signs and symptoms (mild to severe) of nosocomial pneumonia included cough; production of purulent sputum or change in character of sputum;auscultatory findings on pulmonary examination of rales and/or pulmonary consolidation (dullness on percussion, bronchial breath sounds, or egophony); and dyspnea, tachypnea, or hypoxemia with PaO2 <60 mmHg or worsening gas exchange or increased oxygen requirements; pleuritic chest pain; chills/rigors; and decreased breath sounds. (NCT00084266)
Timeframe: EOT (within 72 hours of last dose)

,
InterventionParticipants (Number)
Decreased Breath SoundsHypoxiaPulmonary ConsolidationRalesTachypneaChills/RigorsCoughDyspneaPleuritic Chest PainPurulent Sputum
Linezolid736753577656428467
Vancomycin1097377736626433285

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Number of Participants With Clinical Signs and Symptoms at EOT for PP Population

Participant's clinical evaluation of signs and symptoms were based on global assessment by investigator at specific timepoints. Signs and symptoms (mild to severe) of nosocomial pneumonia included cough; production of purulent sputum or change in character of sputum;auscultatory findings on pulmonary examination of rales and/or pulmonary consolidation (dullness on percussion, bronchial breath sounds, or egophony); and dyspnea, tachypnea, or hypoxemia with PaO2 <60 mmHg or worsening gas exchange or increased oxygen requirements; pleuritic chest pain; chills/rigors; and decreased breath sounds. (NCT00084266)
Timeframe: EOT (within 72 hours of last dose)

,
InterventionParticipants (Number)
Decreased Breath SoundsHypoxiaPulmonary ConsolidationRalesTachypneaChills/RigorsCoughDyspneaPleuritic Chest PainPurulent Sputum
Linezolid635643496735324255
Vancomycin996069615805927174

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Clinical Outcome in Participants With Baseline MRSA at End of Treatment (EOT) for PP Population

Clinical response evaluated at EOT visit as Cure:resolution of clinical sign/symptoms of pneumonia when compared with baseline;Improvement: in 2 or more clinical sign/symptoms of pneumonia when compared with baseline,improvement/lack of progression of all chest X-ray abnormalities,Failure: persistence/ progression of baseline signs/symptoms of pneumonia or baseline radiographic abnormalities after atleast 2 days of treatment; development of new pulmonary/extrapulmonary clinical findings consistent with active infection;Unknown: extenuating circumstances precluding classification to 1 of above. (NCT00084266)
Timeframe: EOT (within 72 hours of last dose)

,
InterventionParticipants (Number)
CureImprovementFailureUnknown/Missing (excluded from analysis)
Linezolid7674303
Vancomycin7060562

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Clinical Outcome in Participants With Baseline MRSA at EOS for mITT Population

Clinical response was based primarily on global assessment of clinical presentation of participant made by investigator at evaluation timepoint. Clinical response was evaluated at EOS Visit as Cure: resolution of clinical signs/symptoms of pneumonia when compared with baseline; Failure: persistence/progression of baseline signs/symptoms of pneumonia or baseline radiographic abnormalities after atleast 2 days of treatment; development of new pulmonary/extrapulmonary clinical findings consistent with active infection; Unknown:extenuating circumstances precluding classification to 1 of the above. (NCT00084266)
Timeframe: EOS (7-30 days after last dose)

,
InterventionParticipants (Number)
CureFailureUnknown/Missing (excluded from analysis)
Linezolid1028438
Vancomycin9211319

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Microbiological Outcome in Participants With Baseline MRSA at EOT for mITT Population

"Microbiological outcome dichotomized to success (eradication: absence of baseline isolate (BI) in culture of original infection site (IS); presumed eradication: participant cured and no specimen available for culture; superinfection: clinically failed or improved with new pathogen identified from primary IS other than BI; colonization: isolate was present but not producing infection) and failure (persistence: BI present in original IS; presumed persistence: clinically failed and no specimen available for culture)." (NCT00087490)
Timeframe: EOT (within 72 hours of last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid84.215.8
Vancomycin69.230.8

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Microbiological Outcome in Participants With Baseline MRSA at EOT for PP Population

"Microbiological outcome dichotomized to success (eradication: absence of baseline isolate (BI) in culture of original infection site (IS); presumed eradication: participant cured and no specimen available for culture; superinfection: clinically failed or improved with new pathogen identified from primary IS other than BI; colonization: isolate was present but not producing infection) and failure (persistence: BI present in original IS; presumed persistence: clinically failed and no specimen available for culture)." (NCT00087490)
Timeframe: EOT (within 72 hours of last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid85.414.6
Vancomycin68.831.2

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Number of Participants With Clinical Signs and Symptoms at EOT and EOS for mITT Population

"Participant's clinical evaluation of signs and symptoms were based on global assessment by investigator at specific timepoints. Signs and symptoms of an active skin or soft tissue infection caused by suspected MRSA included purulent discharge, nonpurulent discharge, erythema, swelling, induration, tenderness, pain and local skin warmth. It was recorded using wound parameter score ranging from 0 to 3; 0= none, 1= mild, 2= moderate and 3= severe." (NCT00087490)
Timeframe: EOT (within 72 hours of last dose of study drug), EOS (6 to 28 days after the last dose of study drug)

,
InterventionPartcipants (Number)
Purulent discharge (mild) (EOT) (n=286, 292)Purulent discharge (moderate) (EOT) (n=286, 292)Purulent discharge (severe) (EOT) (n=286, 292)Non-purulent discharge (mild) (EOT) (n=286, 292)Non-purulent discharge (moderate) (EOT)(n=286,292)Non-purulent discharge (severe) (EOT) (n=286, 292)Erythema (mild) (EOT) (n=286, 292)Erythema (moderate) (EOT) (n=286, 292)Erythema (severe) (EOT) (n=286, 292)Swelling (mild) (EOT) (n=286, 291)Swelling (moderate) (EOT) (n=286, 291)Swelling (severe) (EOT) (n=286, 291)Induration (mild) (EOT) (n=286, 292)Induration (moderate) (EOT) (n=286, 292)Induration (severe) (EOT) (n=286, 292)Tenderness (mild) (EOT) (n=286, 292)Tenderness (moderate) (EOT) (n=286, 292)Tenderness (severe) (EOT) (n=286, 292)Pain (mild) (EOT) (n=286, 292)Pain (moderate) (EOT) (n=286, 292)Pain (severe) (EOT) (n=286, 292)Local skin warmth (mild) (EOT) (n=286, 290)Local skin warmth (moderate) (EOT) (n=286, 290)Local skin warmth (severe) (EOT) (n=286, 290)Purulent discharge (mild) (EOS) (n=286, 270)Purulent discharge (moderate) (EOS) (n=286, 270)Purulent discharge (severe) (EOS) (n=286, 270)Non-purulent discharge (mild) (EOS) (n=285, 270)Non-purulent discharge (moderate) (EOS)(n=285,270)Non-purulent discharge (severe) (EOS) (n=285, 270)Erythema (mild) (EOS) (n=286, 270)Erythema (moderate) (EOS) (n=286, 270)Erythema (severe) (EOS) (n=286, 270)Swelling (mild) (EOS) (n=285, 269)Swelling (moderate) (EOS) (n=285, 269)Swelling (severe) (EOS) (n=285, 269)Induration (mild) (EOS) (n=285, 270)Induration (moderate) (EOS) (n=285, 270)Induration (severe) (EOS) (n=285, 270)Tenderness (mild) (EOS) (n=284, 270)Tenderness (moderate) (EOS) (n=284, 270)Tenderness (severe) (EOS) (n=284, 270)Pain (mild) (EOS) (n=285, 270)Pain (moderate) (EOS) (n=285, 270)Pain (severe) (EOS) (n=285, 270)Local skin warmth (mild) (EOS) (n=285, 269)Local skin warmth (moderate) (EOS) (n=285, 269)Local skin warmth (severe) (EOS) (n=285, 269)
Linezolid27307150723154717360779155100202013414650406033213720496049702000
Vancomycin2593936088101829189608522219420338302871564045120361114461467240732741

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Number of Participants With Clinical Signs and Symptoms at EOT and EOS for PP Population

"Participant's clinical evaluation of signs and symptoms were based on global assessment by investigator at specific timepoints. Signs and symptoms of an active skin or soft tissue infection caused by suspected MRSA included purulent discharge, nonpurulent discharge, erythema, swelling, induration, tenderness, pain and local skin warmth. It was recorded by the sponsor using wound parameter score ranging from 0 to 3; 0= none, 1= mild, 2= moderate and 3= severe." (NCT00087490)
Timeframe: EOT (within 72 hours of last dose of study drug), EOS (6 to 28 days after the last dose of study drug)

,
InterventionParticipants (Number)
Purulent discharge (mild) (EOT) (n=222, 206)Purulent discharge (moderate) (EOT) (n=222, 206)Purulent discharge (severe) (EOT) (n=222, 206)Non-purulent discharge (mild) (EOT) (n=222, 206)Non-purulent discharge (moderate) (EOT)(n=222,206)Non-purulent discharge (severe) (EOT) (n=222, 206)Erythema (mild) (EOT) (n=222, 206)Erythema (moderate) (EOT) (n=222, 206)Erythema (severe) (EOT) (n=222, 206)Swelling (mild) (EOT) (n=222, 205)Swelling (moderate) (EOT) (n=222, 205)Swelling (severe) (EOT) (n=222, 205)Induration (mild) (EOT) (n=222, 206)Induration (moderate) (EOT) (n=222, 206)Induration (severe) (EOT) (n=222, 206)Tenderness (mild) (EOT) (n=222, 206)Tenderness (moderate) (EOT) (n=222, 206)Tenderness (severe) (EOT) (n=222, 206)Pain (mild) (EOT) (n=222, 206)Pain (moderate) (EOT) (n=222, 206)Pain (severe) (EOT) (n=222, 206)Local skin warmth (mild) (EOT) (n=222, 205)Local skin warmth (moderate) (EOT) (n=222, 205)Local skin warmth (severe) (EOT) (n=222, 205)Purulent discharge (mild) (EOS) (n=228, 209)Purulent discharge (moderate) (EOS) (n=228, 209)Purulent discharge (severe) (EOS) (n=228, 209)Non-purulent discharge (mild) (EOS) (n=227, 209)Non-purulent discharge (moderate) (EOS)(n=227,209)Non-purulent discharge (severe) (EOS) (n=227, 209)Erythema (mild) (EOS) (n=228, 209)Erythema (moderate) (EOS) (n=228, 209)Erythema (severe) (EOS) (n=228, 209)Swelling (mild) (EOS) (n=227, 208)Swelling (moderate) (EOS) (n=227, 208)Swelling (severe) (EOS) (n=227, 208)Induration (mild) (EOS) (n=227, 209)Induration (moderate) (EOS) (n=227, 209)Induration (severe) (EOS) (n=227, 209)Tenderness (mild) (EOS) (n=227, 209)Tenderness (moderate) (EOS) (n=227, 209)Tenderness (severe) (EOS) (n=227, 209)Pain (mild) (EOS) (n=227, 209)Pain (moderate) (EOS) (n=227, 209)Pain (severe) (EOS) (n=227, 209)Local skin warmth (mild) (EOS) (n=227, 208)Local skin warmth (moderate) (EOS) (n=227, 208)Local skin warmth (severe) (EOS) (n=227, 208)
Linezolid2110543053103941573062403840140010213530254023012810295032501100
Vancomycin175357506241446167305215243152191021404320316025403710324027401520

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Microbiological Outcome in Participants With Baseline MRSA at EOS for mITT Population

"Microbiological outcome dichotomized to success (eradication: absence of baseline isolate (BI) in culture of original infection site (IS); presumed eradication: participant cured and no specimen available for culture; superinfection: clinically failed or improved with new pathogen identified from primary IS other than BI; colonization: isolate was present but not producing infection) and failure (persistence: BI present in original IS; presumed persistence: clinically failed and no specimen available for culture; recurrence: presence of isolate at EOS, that was eradicated at EOT)." (NCT00087490)
Timeframe: EOS (6 to 28 days after the last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid73.526.5
Vancomycin65.834.2

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Clinical Outcome in Participants With Baseline MRSA at EOT for mITT Population

"CR evaluated at EOT visit as success (cure: resolution of clinical sign/symptoms of infection when compared with baseline; and improvement: 2/more improvement in clinical sign/symptoms of infection when compared with baseline); failure: persistence/progression of baseline signs/symptoms of infection after at least 2 days of treatment/development of new clinical findings consistent with active infection; unknown: extenuating circumstances precluding classification to 1 of above. Unknown: excluded from present analysis." (NCT00087490)
Timeframe: EOT (within 72 hours of last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid89.410.6
Vancomycin84.715.3

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Clinical Outcome in Participants With Baseline MRSA at EOS for Modified-Intent to Treat (mITT) Population

"CR was based primarily on global assessment of clinical presentation of participant made by investigator at evaluation time point. At EOS, CR was evaluated as success (cure: resolution of clinical signs/symptoms of infection when compared to baseline); failure: persistence/progression of baseline signs/symptoms of infection after at least 2 days of treatment/development of new clinical findings consistent with active infection; unknown: extenuating circumstances precluding classification to 1 of above. Unknown was excluded from present analysis." (NCT00087490)
Timeframe: EOS (6 to 28 days after the last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid80.819.2
Vancomycin73.726.3

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Clinical Outcome in Participants With Baseline Methicillin-Resistant Staphylococcus Aureus (MRSA) at End of Study (EOS) for Per-Protocol (PP) Population

"Clinical response (CR) was based primarily on global assessment of clinical presentation of participant made by investigator at evaluation time point. At EOS, CR was evaluated as success (cure: resolution of clinical signs or (/) symptoms of infection when compared to baseline); failure: persistence/progression of baseline signs/symptoms of infection after at least 2 days of treatment/development of new clinical findings consistent with active infection; unknown: extenuating circumstances precluding classification to 1 of above. Unknown was excluded from present analysis." (NCT00087490)
Timeframe: EOS (6 to 28 days after the last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid84.115.9
Vancomycin79.920.1

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Duration of Intravenous Therapy for PP Population

Duration of intravenous antibiotic treatment was measured as the number of days intravenous doses of study medication was administered, before and after discharge. (NCT00087490)
Timeframe: Baseline up to EOS (6 to 28 days after the last dose of study drug)

InterventionDays (Mean)
Linezolid5.6
Vancomycin10.4

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Duration of Intravenous Therapy for mITT Population

Duration of intravenous antibiotic treatment was measured as the number of days intravenous doses of study medication was administered, before and after discharge. (NCT00087490)
Timeframe: Baseline up to EOS (6 to 28 days after the last dose of study drug)

InterventionDays (Mean)
Linezolid5.3
Vancomycin9.8

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Duration of Hospital Stay for PP Population

Duration of Hospital Stay was defined as the number of days the participant was cared as an inpatient in the hospital during the maximum 34 days of the study period. The number of days in the hospital was counted from start of study medication to date of discharge or last date known to be in the hospital (for missing discharge dates and participants who died) or Day 34 for participants who continued hospitalization beyond EOS period. (NCT00087490)
Timeframe: Baseline up to EOS (6 to 28 days after the last dose of study drug)

InterventionDays (Mean)
Linezolid7.6
Vancomycin8.9

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Clinical Outcome in Participants With Baseline MRSA at End of Treatment (EOT) for PP Population

"CR evaluated at EOT visit as success (cure: resolution of clinical sign/symptoms of infection when compared with baseline; and improvement: 2/more improvement in clinical sign/symptoms of infection when compared with baseline); failure: persistence/progression of baseline signs/symptoms of infection after at least 2 days of treatment/development of new clinical findings consistent with active infection; unknown: extenuating circumstances precluding classification to 1 of above. Unknown: excluded from present analysis." (NCT00087490)
Timeframe: EOT (within 72 hours of last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid91.68.4
Vancomycin87.712.3

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Duration of Hospital Stay for mITT Population

Duration of Hospital Stay was defined as the number of days the participant was cared as an inpatient in the hospital during the maximum 34 days of the study period. The number of days in the hospital was counted from start of study medication to date of discharge or last date known to be in the hospital (for missing discharge dates and participants who died) or Day 34 for participants who continued hospitalization beyond EOS period. (NCT00087490)
Timeframe: Baseline up to EOS (6 to 28 days after the last dose of study drug)

InterventionDays (Mean)
Linezolid7.7
Vancomycin8.9

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Microbiological Outcome in Participants With Baseline MRSA at EOS for PP Population

"Microbiological outcome dichotomized to success (eradication: absence of baseline isolate (BI) in culture of original infection site (IS); presumed eradication: participant cured and no specimen available for culture; superinfection: clinically failed or improved with new pathogen identified from primary IS other than BI; colonization: isolate was present but not producing infection) and failure (persistence: BI present in original IS; presumed persistence: clinically failed and no specimen available for culture; recurrence: presence of isolate at EOS, that was eradicated at EOT)." (NCT00087490)
Timeframe: EOS (6 to 28 days after the last dose of study drug)

,
InterventionPercentage of participants (Number)
SuccessFailure
Linezolid75.025.0
Vancomycin68.431.6

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Percentage of Participants With an Adverse Event

(NCT00359632)
Timeframe: Through and including 28 calendar days after the last administration of the investigational product

,
InterventionPercentage of Participants (Number)
Adverse events, %Serious adverse events, %Severe adverse events, %Discontinued due to adverse events, %Dose Reduced or Temporary Discontinuation, %
Control11.10000
Linezolid83.325.012.529.212.5

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Percentage of Participants by Clinical Outcome of Infection at End of Study

Clinical response was evaluated at the End of Study visit (30 days after last dose) as Cure, Improvement, Failure, Unknown or Other. Clinical response was based primarily on the global assessment of the clinical presentation of the subject made by the investigator at that evaluation timepoint. The clinical response classifications were defined as follows. Cure: Resolution of the clinical signs and symptoms of infection, when compared to Baseline. No additional antimicrobial treatment is required for the disease under study. Improvement: Improvement in 2 or more, but not all, of the clinical signs and symptoms of infection, when compared with Baseline. No additional antimicrobial treatment is required for the disease under study. Failure: Persistence or progression of Baseline clinical signs and symptoms of infection, or development of new clinical findings consistent with active infection. Unknown: Inability to assess clinical response. (NCT00359632)
Timeframe: At End of Study visit

InterventionPercentage of Participants (Number)
Cure, %Improvement, %Failure, %Unknown, %Other, %
Linezolid47.642.9009.5

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Maximum Plasma Drug Concentration (Cmax)

Maximum Plasma Drug Concentration (Cmax), given sampling scheme (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Isoniazid 300 mg/Day3.3
Linezolid 600 mg/Once Daily15.0
Linezolid 600 mg/Twice Daily19.4

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Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC)

(NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Gatifloxacin 400 mg/Day9.5
Levofloxacin 1000 mg/Day15.6
Moxifloxacin 400 mg/Day12.3
Isoniazid (INH) 300 mg/Day70.6

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Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC) Adjusted for Free Drug Concentrations

(NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Isoniazid 300 mg/Day62.7
Linezolid 600 mg/Once Daily20.0
Linezolid 600 mg/Twice Daily16.2

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Maximum Plasma Drug Concentrations (Cmax), Adjusted for Free Drug Concentration

Cmax adjusted for free drug concentrations after 5 days of monotherapy with study drugs (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Isoniazid 300 mg/Day3.1
Linezolid 600 mg/Once Daily10.3
Linezolid 600 mg/Twice Daily13.4

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Percent Dosing Interval Above Minimum Inhibitory Concentration (MIC)

Determined by linear extrapolation of concentration-versus-time curve to intersection with MIC. (NCT00396084)
Timeframe: Day 5 (7 time points)

InterventionPercentage (Mean)
Isoniazid (INH) 300 mg/Day95.5
Linezolid 600 mg/Once Daily62.8
Linezolid 600 mg/Twice Daily100.0

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Area Under the Curve (AUC) Adjusted for Free Drug Concentrations/Minimum Inhibitory Concentration (MIC)

Area Under the Curve 0-12 (AUC 0-12) Adjusted for Free Drug Concentrations/Minimum Inhibitory Concentration (MIC) and AUC 0-24/MIC (NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionug/h/ml (Median)
AUC 0-12/MICAUC 0-24/MIC
Isoniazid 300 mg/Day306.7344.6
Linezolid 600 mg/Once Daily107.8116.2
Linezolid 600 mg/Twice Daily121.6243.2

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Area Under the Curve (AUC) During First 12 and 24 Hours Adjusted for Free Drug Concentrations

Median pharmacodynamic parameters (range) adjusted for free drug concentrations. AUC 0-12 and AUC 0-24 = area under the curve during the first 12 and 24 hours after dosing, respectively (NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionug/h/ml (Median)
AUC 0-12AUC 0-24
Isoniazid 300 mg/Day15.317.2
Linezolid 600 mg/Once Daily60.166.8
Linezolid 600 mg/Twice Daily80.3160.7

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Pharmacokinetic Parameters: Area Under the Curve During First 12 and 24 Hours

Median pharmacokinetic parameters (range). AUC 0-12 and AUC 0-24 = area under the curve during the first 12 and 24 hours after dosing, respectively (NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionug/h/ml (Median)
AUC 0-12 (ug/h/ml)AUC 0-24 (ug/h/ml)
Isoniazid 300 mg/Day17.019.2
Linezolid 600 mg/Once Daily87.096.9
Linezolid 600 mg/Twice Daily116.4232.9

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Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)

The adjusted area under the curve (aAUC) for sputum colony forming unit (cfu) for each day on treatment was calculated for patients in the INH arm and those in the Linezolid once daily and Linezolid twice daily arms. The aAUC represents the percentage of the expected AUC given no change in log cfu in response to study drug administration. (NCT00396084)
Timeframe: Study drug administration duration - 7 days monotherapy

,,
InterventionPercentage (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
Isoniazid 300 mg/Day0.940.890.890.850.830.810.83
Linezolid 600 mg/Once Daily0.980.970.960.960.950.950.95
Linezolid 600 mg/Twice Daily0.980.960.950.940.940.930.93

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Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)

The adjusted area under the curve (aAUC) for sputum colony forming units (cfu) for each day on treatment was calculated. The aAUC represents the percentage of the expected AUC given no change in log cfu in response to study drug administration. (NCT00396084)
Timeframe: Study drug administration duration - 7 days monotherapy

,,,
InterventionPercentage (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
Gatifloxacin 400 mg/Day0.980.960.920.890.870.850.82
Isoniazid (INH) 300 mg/Day0.950.900.870.840.810.800.80
Levofloxacin 1000 mg/Day0.980.950.910.880.850.830.81
Moxifloxacin 400 mg/Day0.960.940.910.890.870.850.83

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Time to Maximum Plasma Drug Concentration (Tmax) and Half-life

(NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionhours (Median)
Tmax in h (apparent time of max plasma conc.)Half-life
Isoniazid 300 mg/Day1.03.6
Linezolid 600 mg/Once Daily1.53.20
Linezolid 600 mg/Twice Daily1.04.56

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Time to Maximum Plasma Drug Concentration (Tmax) and Half-life

(NCT00396084)
Timeframe: Day 5 (7 time points)

,,,
Interventionhours (Median)
TmaxHalf-life
Gatifloxacin 400 mg/Day1.56.0
Isoniazid (INH) 300 mg/Day12.5
Levofloxacin 1000 mg/Day1.07.6
Moxifloxacin 400 mg/Day1.08.1

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Pharmacokinetic Parameters: Area Under the Curve (AUC) During First 12 and 24 Hours

Area under the curve (AUC), from time 0-12 hours for INH or 0-24 hours for gatifloxacin, levofloxacin, and moxifloxacin. (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/h/ml (Median)
Gatifloxacin 400 mg/Day42.8
Levofloxacin 1000 mg/Day129.1
Moxifloxacin 400 mg/Day55.3
Isoniazid (INH) 300 mg/Day11.9

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Area Under the Curve During First 12 or 24 Hours / Minimum Inhibitory Concentration (AUC/MIC)

Area Under the Curve (AUC) During First 12 or 24 Hours /Minimum Inhibitory Concentration. AUC reflects total drug (bound and unbound). MIC values were determined using protein-containing media. (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Gatifloxacin 400 mg/Day85.6
Levofloxacin 1000 mg/Day129.1
Moxifloxacin 400 mg/Day110.5
Isoniazid (INH) 300 mg/Day215.2

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Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Fluoroquinolones/Isoniazid (INH) Comparison

Early bactericidal activity (EBA 0-2) was calculated as the rate of fall in sputum colony forming units (cfu) (expressed in log10 units) during the first 2 days of monotherapy. (NCT00396084)
Timeframe: Day 0 to Day 2 Monotherapy

Interventionlog10 cfu/ml/day (Mean)
Gatifloxacin 400 mg/Day0.35
Levofloxacin 1000 mg/Day0.45
Moxifloxacin 400 mg/Day0.33
Isoniazid (INH) 300 mg/Day0.67

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Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Linezolid Once Daily/Linezolid Twice Daily/Isoniazid (INH) Comparison

Early bactericidal activity (EBA 0-2) was calculated as the rate of fall in sputum cfu (expressed in log10 units) during the first 2 days of monotherapy. Mean values for the 3 treatment groups were compared. (NCT00396084)
Timeframe: Day 0 to Day 2 Monotherapy

Interventionlog10 cfu/ml/day (Mean)
Isoniazid 300 mg/Day0.67
Linezolid 600 mg/Once Daily0.18
Linezolid 600 mg/Twice Daily0.26

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Difference in Sputum Bacillary Loads: Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Linezolid Once Daily/Linezolid Twice Daily/INH Comparison

The rate of fall in sputum cfu between day 2 and day 7 of monotherapy was estimated by the slope of the linear regression obtained by fitting the 6 sputum cfu values corresponding to Days 2 through 7. (NCT00396084)
Timeframe: Day 2 to Day 7 Monotherapy

Interventionlog10 cfu/ml (Mean)
Isoniazid 300 mg/Day0.16
Linezolid 600 mg/Once Daily0.09
Linezolid 600 mg/Twice Daily0.04

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Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Fluoroquinolones/Isoniazid (INH) Comparison

The rate of fall in sputum cfu between day 2 and day 7 of monotherapy was estimated by the slope of the linear regression obtained by fitting the 6 sputum cfu values corresponding to Days 2 through 7. (NCT00396084)
Timeframe: Day 2 to Day 7 Monotherapy

Interventionlog10 cfu/ml/day (Mean)
Gatifloxacin 400 mg/Day0.17
Levofloxacin 1000 mg/Day0.18
Moxifloxacin 400 mg/Day0.17
Isoniazid (INH) 300 mg/Day0.08

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Maximum Plasma Drug Concentration (Cmax)

Maximum plasma concentration, given sampling scheme (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Gatifloxacin 400 mg/Day4.8
Levofloxacin 1000 mg/Day15.6
Moxifloxacin 400 mg/Day6.1
Isoniazid (INH) 300 mg/Day3.6

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Clinical Response at the Test-of-Cure (TOC) Visit in the Clinically Evaluable (CE) Population

The coprimary efficacy outcome measures were the per-subject clinical cure rate at the TOC Visit in the CE and MITT Populations. Subjects were considered clinically cured at the TOC Visit if they had total resolution of all signs and symptoms of the baseline infection, or improvement of the infection to such an extent that no further antimicrobial therapy was necessary. (NCT00633152)
Timeframe: Test of Cure Visit (8 to 15 Days after end of therapy)

Interventionpercentage of participants (Number)
Ceftaroline90.7
Linezolid (With or Without Aztreonam)97.4

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Clinical Response at the Test of Cure (TOC) Visit in the Modified Intent-to-treat (MITT) Population

The coprimary efficacy outcome measures were the per-subject clinical cure rate at the Test of Cure (TOC) Visit in the Clinically Evaluable (CE) and (Modified-Intent-to-Treat) MITT Populations. Subjects were considered clinically cured at the Test of Cure (TOC) Visit if they had total resolution of all signs and symptoms of the baseline infection, or improvement of the infection to such an extent that no further antimicrobial therapy was necessary. (NCT00633152)
Timeframe: Test of Cure Visit (8 to 15 days after end of therapy)

Interventionpercentage of participants (Number)
Ceftaroline84.7
Linezolid (With or Without Aztreonam)88.9

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Number of Participants With a Clinical Response of Cure

To qualify as a Cure, participants were required to fulfill the following criteria: all systemic signs and symptoms of uSSSI present at screening were improved or resolved; no further antibiotic therapy was necessary for treatment of uSSSI; and there was no worsening or appearance of new signs and symptoms of uSSSI. (NCT00646958)
Timeframe: Test of Cure (TOC), day 10-20

InterventionParticipants (Number)
Radezolid QD38
Radezolid BID34
Linezolid BID37

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Number of Patients With Per-Patient Microbiologic Response of Eradicated

The microbiological response at the patient level was considered Eradicated (documented or presumed)if no pathogens were present in repeat cultures taken from the original site of infection or a clinical response of cure precluded the ability to obtain a culturable specimen. (NCT00646958)
Timeframe: Test of Cure (TOC), day 10-20

InterventionParticipants (Number)
Radezolid QD20
Radezolid BID23
Linezolid BID21

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Number of Participants With Adverse Drug Reaction Not Expected From the Japanese Package Insert.

The adverse drug reaction that have not been listed in Japanese package insert. (NCT00666276)
Timeframe: Baseline to 8 weeks

Interventionparticipants (Number)
SuperinfectionSepsisThrombocytopeniaLactic acidosisAgitationDeep vein thrombosisHyperbilirubinaemiaAntithrombin III decreasedBlood chloride increasedBlood sodium increased
Linezolid1111111111

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Factors Considered to Affect the Safety of Linezolid - Route of Administration.

Number of participants Route of administration as by oral,injection or oral from injection with adverse drug reaction to determine whether oral, injection or switch is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-oral29
Linezolid-injection116
Linezolid-oral From Injection18

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Factors Considered to Affect the Safety of Linezolid - Age

Number of participants with adverse drug reaction to determine whether over 65 or less than 65 is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-over 65122
Linezolid-less Than 6541

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Factors Considered to Affect the Safety of Linezolid - Concomitant Drugs.

Number of participants with or without Concomitant drugs with adverse drug reaction to determine whether with or without is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-without Concomitant Drugs9
Linezolid-with Concomitant Drugs154

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Factors Considered to Affect the Safety of Linezolid - Hepatic Dysfunctions.

Number of participants with or without Hepatic dysfunctions with adverse drug reaction to determine whether with or without is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-without Hepatic Dysfunctions137
Linezolid- With Hepatic Dysfunctions26

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Factors Considered to Affect the Safety of Linezolid - Duration of Drug Administration.

Number of participants with Duration of drug administration as over 15 days or less than 15 days with adverse drug reaction to determine whether over 15 days or less than 15 days is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-administrated Over 15 Days53
Linezolid-administrated Less Than 15 Days110

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Factors Considered to Affect the Safety of Linezolid - Gender.

Number of participants with adverse drug reaction to determine whether male or female is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-male109
Linezolid-female54

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Factors Considered to Affect the Safety of Linezolid - Non-drug Therapies.

Number of participants with or without Non-drug therapies with adverse drug reaction to determine whether with or without is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid-without Non-drug Therapies87
Linezolid-with Non-drug Therapies76

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Factors Considered to Affect the Safety of Linezolid - Renal Dysfunctions.

Number of participants with or without Renal dysfunctions with adverse drug reaction to determine whether with or without is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid Without Renal Dysfunctions125
Linezolid- With Renal Dysfunctions38

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Factors Considered to Affect the Safety of Linezolid - Weight.

Number of participants Weight as over 40kg or less than 40kg with adverse drug reaction to determine whether over 40kg or less than 40kg Weight is significant risk factor. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid -Over 40kg108
Linezolid -Less Than 40kg20

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Number of Participants With Adverse Drug Reactions(ADRs).

All observed or volunteered adverse events and the investigator's opinion of the causal relationship to the study treatment were reported. Adverse Drug Reactions were evaluated in company with the causal relationship to the investigational product. (NCT00666276)
Timeframe: 8 weeks

Interventionparticipants (Number)
Linezolid163

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Number of Patients Converted to Sputum Culture Negative in Each Arm, With Data Censored at 4 Months.

(NCT00727844)
Timeframe: Sputum smear conversion or max 4 months after the start of Linezolid therapy.

Interventionparticipants (Number)
Immediate Start Linezolid15
Delayed Start Linezolid7

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Cohort 2: Mean Time-Matched Difference in Time Corresponding to Beginning of Depolarization to Repolarization of the Ventricles, Corrected for Heart Rate Using Fridericia's Formula (QTcF Interval) Between Linezolid 600 mg and 1200 mg Compared to Placebo

The time corresponding to the beginning of depolarization to repolarization of the ventricles (QT interval) was adjusted for ventricular rate (VR) using the QT and VR from each electrocardiogram by Fridericia's formula (QTcF = QT divided by cube root of VR in seconds). A measure of dispersion is not available. (NCT00795145)
Timeframe: 0.5, 1, 2, 4, 8, 12, 24 hours post-dose

,,
Interventionmilliseconds (msec) (Number)
0.5 hour1 hour2 hours4 hours8 hours12 hours24 hours
Cohort 2: 1200 mg Linezolid422.34420.89412.30421.92412.25413.45417.27
Cohort 2: 600 mg Linezolid421.31419.71414.27418.85409.75412.99414.83
Cohort 2: Placebo419.84422.67419.80418.45411.13411.98415.47

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Cohort 1: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC Inf) and Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC Last)

"AUC inf = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time.~AUC last = Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)." (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

,
Interventionmicrogram (ug)*hours (hr)/mL (Mean)
AUC infAUC last
Cohort 1: 1200 mg Linezolid346.89332.26
Cohort 1: 900 mg Linezolid223.49211.26

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Cohort 1: Time to Reach Maximum Observed Plasma Concentration (Tmax) and Plasma Decay Half-Life (t1/2)

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

,
Interventionhr (Median)
Tmaxt1/2
Cohort 1: 1200 mg Linezolid1.07.1
Cohort 1: 900 mg Linezolid1.06.9

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Cohort 2: AUC Inf and AUC Last

"AUC inf = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time.~AUC last = Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)." (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

,
Interventionug *hr/mL (Mean)
AUC InfAUC Last
Cohort 2: 1200 mg Linezolid328.75299.40
Cohort 2: 900 mg Linezolid141.75129.52

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Cohort 1: Number of Subjects With Adverse Events (AEs) and Serious Adverse Events (SAEs)

All observed or volunteered AEs and SAEs regardless of treatment group or suspected causal relationship to the investigational product(s) were reported. (NCT00795145)
Timeframe: From the time the subject had taken at least one dose of study treatment up to 5 weeks

,,
Interventionparticipants (Number)
AEsSAEs
Cohort 1: 1200 mg Linezolid20
Cohort 1: 900 mg Linezolid30
Cohort 1: Placebo10

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Cohort 2: Vss

Vss = (mean residence time [The average total time molecules of a given dose spend in the body] extrapolated to infinity) multiplied by CL (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

InterventionL/kg (Mean)
Cohort 2: 600 mg Linezolid0.6418
Cohort 2: 1200 mg Linezolid0.6185

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Cohort 2: Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin and Placebo

A measure of dispersion is not available. (NCT00795145)
Timeframe: 0.5, 1, 2, 4, 8, 12, 24 hours post-dose

,
Interventionmsec (Number)
0.5 hour1 hour2 hours4 hours8 hours12 hours24 hours
Cohort 2: Moxifloxacin423.11429.50430.07428.29420.53419.02421.99
Cohort 2: Placebo419.84422.67419.80418.45411.13411.98415.47

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Cohort 2: Cmax

(NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

Interventionug/mL (Mean)
Cohort 2: 600 mg Linezolid15.06
Cohort 2: 1200 mg Linezolid30.76

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Cohort 2: CL

Drug clearance = Dose / AUC inf (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

InterventionmL/min/kg (Mean)
Cohort 2: 600 mg Linezolid1.2825
Cohort 2: 1200 mg Linezolid1.1000

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Cohort 1: Steady-State Volume of Distribution (Vss)

Vss = (mean residence time [The average total time molecules of a given dose spend in the body] extrapolated to infinity) multiplied by CL (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

InterventionL/kg (Mean)
Cohort 1: 900 mg Linezolid0.6016
Cohort 1: 1200 mg Linezolid0.5776

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Cohort 1: Maximum Observed Plasma Concentration (Cmax)

(NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

Interventionug/mL (Mean)
Cohort 1: 900 mg Linezolid22.3
Cohort 1: 1200 mg Linezolid29.37

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Cohort 2: Mean Time-Matched Difference in Uncorrected QT Intervals Between Linezolid 600 mg and 1200 mg Compared to Placebo

A measure of dispersion is not available. (NCT00795145)
Timeframe: 0.5, 1, 2, 4, 8, 12, 24 hours post-dose

,,
Interventionmsec (Number)
0.5 hour1 hour2 hours4 hours8 hours12 hours24 hours
Cohort 2: 1200 mg Linezolid420.60410.06406.76418.40406.40398.96419.06
Cohort 2: 600 mg Linezolid422.60414.80415.40419.66399.66396.56415.80
Cohort 2: Placebo424.08422.25421.15420.58405.30398.85416.38

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Cohort 2: Number of Subjects With AEs and SAEs

All observed or volunteered AEs and SAEs regardless of treatment group or suspected causal relationship to the investigational product(s) were reported. (NCT00795145)
Timeframe: From the time the subject had taken at least one dose of study treatment up to 5 weeks

,,,
Interventionparticipants (Number)
AEsSAEs
Cohort 2: 1200 mg Linezolid70
Cohort 2: 600 mg Linezolid30
Cohort 2: Placebo40
Moxifloxacin 400 mg100

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Cohort 2: Tmax and t1/2

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. Tmax is the time to reach Cmax. (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

,
Interventionhr (Median)
Tmaxt1/2
Cohort 2: 1200 mg Linezolid1.16.796
Cohort 2: 600 mg Linezolid1.0836.095

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Cohort 1: Clearance of Linezolid (CL)

Drug clearance = Dose / AUC inf (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

InterventionmL/minute (min)/kilogram (kg) (Mean)
Cohort 1: 900 mg Linezolid1.0173
Cohort 1: 1200 mg Linezolid0.8813

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Number of Baseline Pathogens With the Indicated Microbiological Outcome at the End of Therapy

"Eradication is the elimination of BL pathogens. Presumed eradication and presumed improvement are clinical outcomes of success or improvement, respectively, such that no culture was obtained due to lack of culturable material, secondary to adequate clinical response, and is documented in the electronic Case Report Form. Persistence is defined as BL pathogens still being present. Presumed persistence is defined as a participant that is a clinical failure with no obtained culture. Unable to determine was used if no determination of BL pathogen microbiological response could be made." (NCT00852540)
Timeframe: 2-4 days post-therapy; Day 7-9 for retapamulin and Day 12-14 for linezolid

,
Interventionpathogens (Number)
EradicationPresumed eradicationPresumed improvementPersistencePresumed persistenceUnable to determine
Linezolid Plus Placebo Ointment17021110
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo263120791

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Number of Participants With the Indicated Clinical Outcome at the End of Therapy

"Clinical improvement is defined as improvement of signs/symptoms of infection recorded at baseline (BL) to such an extent that no further antimicrobial therapy is necessary. Clinical failure (CF) is defined as insufficient improvement/deterioration of signs/symptoms of the infection recorded at BL, such that additional antibiotic therapy is required. Unable to determine (UTD) is defined as refusal to consent to a clinical examination, lost to follow-up. Participants who are CF/Unable to Determine at end of therapy are considered such at follow-up as well." (NCT00852540)
Timeframe: 2-4 days post-therapy; Day 7-9 for retapamulin and Day 12-14 for linezolid

,
Interventionparticipants (Number)
Clinical successClinical improvementClinical failureUnable to determine
Linezolid Plus Placebo Ointment963442
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo92155165

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Number of Participants With the Indicated Clinical Outcome at the End of Therapy Who Had MRSA as a Baseline Pathogen

"Clinical improvement is defined as improvement of signs/symptoms of infection recorded at baseline (BL) to such an extent that no further antimicrobial therapy is necessary. Clinical failure (CF) is defined as insufficient improvement/deterioration of signs/symptoms of the infection recorded at BL, such that additional antibiotic therapy is required. Unable to determine (UTD) is defined as refusal to consent to a clinical examination, lost to follow-up. Participants who are CF/Unable to Determine at end of therapy are considered such at follow-up as well." (NCT00852540)
Timeframe: 2-4 days post-therapy; Day 7-9 for retapamulin and Day 12-14 for linezolid

,
Interventionparticipants (Number)
Clinical successClinical improvementClinical failureUnable to determine
Linezolid Plus Placebo Ointment28910
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo204282

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Number of Participants Achieving Clinical Response at Follow-up Who Had Methicillin-resistant Staphlococcus Aureus (MRSA) as a Baseline Pathogen

"Follow-up is defined as 7-9 days post-therapy: Day 12-14 for retapamulin; Day 17-19 for linezolid. Clinical success at follow-up was defined as the resolution of clinically meaningful signs and symptoms of infection recorded at baseline, including a pus/exudate skin infection rating scale (SIRS) score of 0. The SIRS is used by the investigator to evaluate infected lesions. Scores on the SIRS range from 0 (absent) to 6 (severe)." (NCT00852540)
Timeframe: 7-9 days post-therapy; Day 12-14 for retapamulin and Day 17-19 for linezolid

Interventionparticipants (Number)
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo41
Linezolid Plus Placebo Ointment32

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Number of Participants Achieving Microbiological Response (MR) at Follow-up (FU) Who Had MRSA as a Baseline Pathogen (BP)

"MR was defined as microbiological success if, (1) for participants (par.) whose clinical outcome at end of therapy (EOT) was clinical success (CS)/improvement, the BP was eradicated/presumed to be eradicated at EOT, or the BP was present at EOT and absent at FU, or the BP was eradicated/presumed to be eradicated at EOT, or the BP was present at EOT and par. was a CS such that no culture was obtained due to lack of culturable material secondary to adequate clinical response; or (2) a pathogen not previously identified at baseline was isolated at FU in a par. identified at FU as a CS." (NCT00852540)
Timeframe: 7-9 days post-therapy; Day 12-14 for retapamulin and Day 17-19 for linezolid

Interventionparticipants (Number)
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo41
Linezolid Plus Placebo Ointment32

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Number of Participants Who Achieved Microbiological Response (MR) at Follow-up (FU) Who Had a Baseline Pathogen (BP)

"MR was defined as microbiological success if, (1) for participants (par.) whose clinical outcome at end of therapy (EOT) was clinical success (CS)/improvement, the BP was eradicated/presumed to be eradicated at EOT, or the BP was present at EOT and absent at FU, or the BP was eradicated/presumed to be eradicated at EOT, or the BP was present at EOT and par. was a CS such that no culture was obtained due to lack of culturable material secondary to adequate clinical response; or (2) a pathogen not previously identified at baseline was isolated at FU in a par. identified at FU as a CS." (NCT00852540)
Timeframe: 7-9 days post-therapy; Day 12-14 for retapamulin and Day 17-19 for linezolid

Interventionparticipants (Number)
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo100
Linezolid Plus Placebo Ointment65

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Number of Participants With Clinical Response at Follow-up

"Follow-up is defined as 7-9 days post-therapy: Day 12-14 for retapamulin; Day 17-19 for linezolid. Clinical success at follow-up was defined as the resolution of clinically meaningful signs and symptoms of infection recorded at baseline, including a pus/exudate skin infection rating scale (SIRS) score of 0. The SIRS is used by the investigator to evaluate infected lesions. Scores on the SIRS range from 0 (absent) to 6 (severe)." (NCT00852540)
Timeframe: 7-9 days post-therapy; Day 12-14 for retapamulin and Day 17-19 for linezolid

Interventionparticipants (Number)
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo161
Linezolid Plus Placebo Ointment112

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Number of Participants With Therapeutic Response at Follow-up

"Therapeutic response is defined as the combined clinical and microbiological response. Therapeutic response iss a measure of the overall efficacy response, and a therapeutic success refers to participants who had been deemed both a clinical success and a microbiological success. All other combinations (other than clinical success + microbiological success) were deemed failures for therapeutic response." (NCT00852540)
Timeframe: 7-9 days post-therapy; Day 12-14 for retapamulin and Day 17-19 for linezolid

Interventionparticipants (Number)
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo100
Linezolid Plus Placebo Ointment65

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Mean Scores on the Skin Infection Rating Scale at Visits 1, 2, 3, 4, and 5

The investigator evaluated skin infections by grading the infected lesion for exudate (a fluid that leaks out of blood vessels into surrounding tissue)/pus, crusting, erythema (redness of the skin)/ inflammation (E/I), tissue warmth, tissue edema (swelling), itching, and pain, according to the Skin Infection Rating Scale. All parameters were graded on a scale of 0 (absent) to 6 (severe). The total score is calculated by summing the individual scores from the 7 parameters; the total score ranges from 0 to 42. (NCT00852540)
Timeframe: Visits 1 (Day 1), 2 (Day 3-4), 3 (Day 7-9), 4 (Day 12-14), and 5 (Day 17-19)

,
Interventionscores on a scale (Mean)
Pus/exudate, Visit 1, n=268, 136Pus/exudate, Visit 2, n=265, 135Pus/exudate, Visit 3, n=255, 130Pus/exudate, Visit 4, n=237, 125Pus/exudate, Visit 5, n=238, 122Crusting, Visit 1, n=268, 136Crusting, Visit 2, n=265, 135Crusting, Visit 3, n=255, 130Crusting, Visit 4, n=237, 125Crusting, Visit 5, n=238, 122E/I, Visit 1, n=268, 136E/I, Visit 2, n=265, 135E/I, Visit 3, n=255, 130E/I, Visit 4, n=237, 125E/I, Visit 5, n=238, 122Tissue warmth, Visit 1, n=268, 136Tissue warmth, Visit 2, n=265, 135Tissue warmth, Visit 3, n=255, 130Tissue warmth, Visit 4, n=237, 125Tissue warmth, Visit 5, n=238, 122Tissue edema, Visit 1, n=268, 136Tissue edema, Visit 2, n=265, 135Tissue edema, Visit 3, n=255, 130Tissue edema, Visit 4, n=237, 125Tissue edema, Visit 5, n=238, 122Itching, Visit 1, n=268, 136Itching, Visit 2, n=265, 135Itching, Visit 3, n=255, 130Itching, Visit 4, n=237, 125Itching, Visit 5, n=238, 122Pain, Visit 1, n=268, 136Pain, Visit 2, n=265, 135Pain, Visit 3, n=255, 130Pain, Visit 4, n=237, 125Pain, Visit 5, n=238, 122Total score, Visit 1, n=268, 136Total score, Visit 2, n=265, 135Total score, Visit 3, n=255, 130Total score, Visit 4, n=237, 125Total score, Visit 5, n=238, 122
Linezolid Plus Placebo Ointment3.61.40.40.10.02.11.20.80.50.33.42.21.00.50.22.61.30.40.10.02.71.50.70.20.11.80.90.60.40.23.01.20.40.10.119.29.74.12.51.6
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo3.61.70.60.20.12.21.30.90.60.33.42.21.10.50.22.81.40.60.10.12.81.60.70.30.11.61.00.70.30.13.21.50.60.20.119.510.75.23.62.5

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Mean Wound Size at Visits 1, 2, 3, 4, and 5

Lesion sized was measured in centimeters squared at Visits 1, 2, 3, 4, and 5. (NCT00852540)
Timeframe: Visits 1 (Day 1), 2 (Day 3-4), 3 (Day 7-9), 4 (Day 12-14), and 5 (Day 17-19)

,
Interventioncentimeters squared (cm^2) (Mean)
Visit 1, n=268, 136Visit 2, n=265, 135Visit 3, n=255, 130Visit 4, n=237, 125Visit 5, n=237, 122
Linezolid Plus Placebo Ointment5.6204.1151.7760.8120.588
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo7.9424.9633.2701.5560.741

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Number of Participants With the Indicated Microbiological Outcome at the End of Therapy Who Had MRSA as a Baseline (BL) Pathogen

"Eradication is the elimination of BL pathogens. Presumed eradication and presumed improvement are clinical outcomes of success or improvement, respectively, such that no culture was obtained due to lack of culturable material, secondary to adequate clinical response, and is documented in the electronic Case Report Form. Persistence is defined as BL pathogens still being present. Presumed persistence is defined as a participant that is a clinical failure with no obtained culture. Unable to determine was used if no determination of BL pathogen microbiological response could be made." (NCT00852540)
Timeframe: 2-4 days post-therapy; Day 7-9 for retapamulin and Day 12-14 for linezolid

,
Interventionparticipants (Number)
EradicationPresumed eradicationPresumed improvementPersistencePresumed persistenceUnable to determine
Linezolid Plus Placebo Ointment0289100
Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo12042441

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Number of Participants With the Indicated Type of Adverse Event (AE)

The assessment of safety was based mainly on the frequency of AEs, and summaries of vital signs and laboratory values (values classified as AE are captured in the AE module). An AE is defined as the appearance or worsening of any undesirable sign, symptom, or medical condition occurring after starting the study drug, whether or not the event was considered causally related to the medical product. An AE could have been a new occurrence or an existing process that increased in intensity or frequency. AEs were deemed treatment-emergent if the start date was on or after the date of the first dose but was not present before that date or if the AE started before the date of the first dose and increased in severity on or after that date. (NCT00865280)
Timeframe: from the time of informed consent to Test of Cure (10 to 17 days after end of treatment [total treatment of up to 14 days)

,
InterventionParticipants (Count of Participants)
Treatment-emergent adverse event (TEAE)Study drug-related TEAEAEs leading to study drug discontinuation
Linezolid58410
Omadacycline56412

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Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0-∞)]

AUC (0-∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-∞). It is obtained from AUC (0-t) plus AUC (t-∞). (NCT01055769)
Timeframe: 0, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, and 48 hours post-dose

Interventionmcg*h/mL (Mean)
Linezolid 600 mg Oral Suspension109.20
Linezolid 600 mg Tablet112.60

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)

Area under the plasma concentration-time curve from time zero (pre-dose) to the time of the last measurable concentration (AUClast). (NCT01055769)
Timeframe: 0, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, and 48 hours post-dose

Interventionmicrogram*hour/milliliter (mcg*h/mL) (Mean)
Linezolid 600 mg Oral Suspension108.90
Linezolid 600 mg Tablet112.00

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Time to Reach Maximum Observed Plasma Concentration (Tmax)

The time of the first occurrence of peak concentration observed directly from data. (NCT01055769)
Timeframe: 0, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, and 48 hours post-dose

Interventionhours (Median)
Linezolid 600 mg Oral Suspension0.63
Linezolid 600mg Tablet1.50

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Terminal Half-Life (t1/2)

Plasma terminal half-life is the time measured for the plasma concentration to decrease by one half. (NCT01055769)
Timeframe: 0, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, and 48 hours post-dose

Interventionhours (Mean)
Linezolid 600 mg Oral Suspension5.08
Linezolid 600 mg Tablet5.13

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Maximum Observed Plasma Concentration (Cmax)

Maximum observed plasma concentration within the dosing interval was directly obtained from the concentration-time data. (NCT01055769)
Timeframe: 0, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, and 48 hours post-dose

Interventionmicrogram/milliliter (mcg/mL) (Mean)
Linezolid 600 mg Oral Suspension15.51
Linezolid 600 mg Tablet13.68

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Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit in the Clinically Evaluable-End of Therapy Analysis Sets

Responder: No increase in lesion surface area from baseline and oral temperature ≤37.6°C (NCT01170221)
Timeframe: EOT Day 11

Interventionparticipants (Number)
Tedizolid Phosphate219
Linezolid232

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Clinical Response at 48-72 Hours That is Sustained at the End of Therapy Visit.

Responder: No increase in lesion surface area from baseline and oral temperature ≤37.6°C. (NCT01170221)
Timeframe: Day 11

Interventionparticipants (Number)
Tedizolid Phosphate230
Linezolid241

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Early Clinical Response Rate

Responder: No increase in lesion surface area from baseline and oral temperature ≤37.6°C (NCT01170221)
Timeframe: 48-72 hours

InterventionResponders (Number)
Tedizolid Phosphate264
Linezolid266

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Investigator's Assessment of Clinical Response at the 48-72 Hour Visit

Clinical improvement was defined as improvement in overall clinical status. (NCT01170221)
Timeframe: 48-72 Hour Visit

Interventionparticipants (Number)
Tedizolid Phosphate299
Linezolid290

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Investigator's Assessment of Clinical Response at the Day 7 Visit

Clinical improvement was defined as improvement in overall clinical status. (NCT01170221)
Timeframe: Day 7

Interventionparticipants (Number)
Tedizolid Phosphate302
Linezolid299

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Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit

Clinical success defined as resolution/near resolution of most disease-specific signs and symptoms, absence/near resolution of systemic signs of infection, if present at baseline, no new signs, symptoms, or complications attributable to the ABSSSIs so no further antibiotic therapy was required for the treatment of the primary lesion. (NCT01170221)
Timeframe: Post-Treatment Evaluation (7-14 days after the End of Therapy)

Interventionparticipants (Number)
Tedizolid Phosphate284
Linezolid288

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Change From Baseline in Patient-reported Pain, by Study Visit

0=no pain, 10=worst pain Only 1 visit per participant for Day 4-6, only 1 visit for Day 7-9, and only 1 visit for Day 10-13. (NCT01170221)
Timeframe: Multiple

,
Interventionunits on a scale (Mean)
Day 2Day 4-6Day 7-9Day 10-13
Linezolid-1.5-3.1-4.6-5.5
Tedizolid Phosphate-1.3-3.4-4.5-5.3

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To Compare the Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit in the Clinically Evaluable-Post Treatment Evaluation Analysis Set

Clinical success defined as resolution/near resolution of most disease-specific signs and symptoms, absence/near resolution of systemic signs of infection, no new signs, symptoms, or complications attributable to the ABSSSIs so no further antibiotic therapy was required for the treatment of the primary lesion. (NCT01170221)
Timeframe: Post-Treatment Evaluation (7-14 days after the End of Therapy)

Interventionparticipants (Number)
Tedizolid Phosphate264
Linezolid267

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Mean Exudate or Pus Sub-score of SIS at Indicated Time Points

The SIS consist of 7 items of exudate or pus, crusting, erythema or inflammation, tissue warmth, tissue edema, itching and pain. The exudate or pus sub-score of SIS was rated on a 7-point scale ranging from 0 to 6, where 0 indicated absence of symptom and 6 indicated severe symptom. Assessments were done at Day 1, Day 2, Day 3, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionScores on scale (Mean)
Day 1Day 2Day 3Day 4Day 8Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg BID3.23.02.11.50.80.20.10.0
Linezolid 600 mg BID3.22.82.21.70.40.00.00.0

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Mean Hematology Parameter of Hemoglobin, Mean Corpuscle Hemoglobin Concentration (MCHC) at Indicated Time Points

Blood samples were obtained for analysis of MCHC at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionGram/Liter (Mean)
Hemoglobin, Day 1Hemoglobin, Day 4Hemoglobin, Day 8Hemoglobin, Day 11Hemoglobin, 7 Day Follow-upHemoglobin, 28 Day Follow-upMCHC, Day 1MCHC, Day 4MCHC, Day 8MCHC, Day 11MCHC, 7 Day Follow-upMCHC, 28 Day Follow-up
GSK1322322 1500 mg BID136.7132.9135.8135.9137.7139.6334.0335.1336.6335.5337.8336.1
Linezolid 600 mg BID134.2133.5134.0136.4135.8136.1331.9333.5335.7336.4335.4334.3

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Mean Hematology Parameter of Mean Corpuscle Hemoglobin (MCH) at Indicated Time Points

Blood samples were obtained for analysis of MCH at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionPicogram (Mean)
Day 1Day 4Day 8Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg BID30.2230.0830.1030.0630.1430.26
Linezolid 600 mg BID30.2430.5830.6330.5930.7130.56

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Mean Hematology Parameter of Mean Corpuscle Volume (MCV) at Indicated Time Points

Blood samples were obtained for analysis of MCV at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionFemtoliter (Mean)
Day 1Day 4Day 8Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg90.589.889.489.789.190.1
Linezolid 600 mg91.191.691.290.791.591.3

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Mean Hematology Parameter of Red Blood Cell (RBC) Count and Reticulocyte Count at Indicated Time Points

Blood samples were obtained for analysis of RBC count and reticulocyte at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionTrillion cells (TI)/Liter (Mean)
RBC count, Day 1RBC count, Day 4RBC count, Day 8RBC count, Day 11RBC count, 7 Day Follow-upRBC count, 28 Day Follow-upReticulocytes, Day 1Reticulocytes, Day 4Reticulocytes, Day 8Reticulocytes, Day 11Reticulocytes, 7 Day Follow-upReticulocytes, 28 Day Follow-up
GSK1322322 1500 mg BID4.534.434.524.524.564.610.070.060.070.070.060.07
Linezolid 600 mg BID4.434.364.374.464.424.440.060.050.050.070.080.06

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Mean Hematology Parameters of Basophils, Eosinophils, Lymphocytes, Monocytes, Total Neutrophils, White Blood Cells (WBC) and Platelet Count at Indicated Time Points

Blood samples were obtained for analysis of basophils, eosinophils, lymphocytes, monocytes, total neutrophils, WBC and platelet count at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionGiga cells/Liter (Mean)
Basophils, Day 1Basophils, Day 4Basophils, Day 8Basophils, Day 11Basophils, 7 Day Follow-upBasophils, 28 Day Follow-upEosinophils, Day 1Eosinophils, Day 4Eosinophils, Day 8Eosinophils, Day 11Eosinophils, 7 Day Follow-upEosinophils, 28 Day Follow-upMonocytes, Day 1Monocytes, Day 4Monocytes, Day 8Monocytes, Day 11Monocytes, 7 Day Follow-upMonocytes, 28 Day Follow-upTotal neutrophils, Day 1Total neutrophils, Day 4Total neutrophils, Day 8Total neutrophils, Day 11Total neutrophils, 7 Day Follow-upTotal neutrophils, 28 Day Follow-upWBC count, Day 1WBC count, Day 4WBC count, Day 8WBC count, Day 11WBC count, 7 Day Follow-upWBC count, 28 Day Follow-upPlatelet count, Day 1Platelet count, Day 4Platelet count, Day 8Platelet count, Day 11Platelet count, 7 Day Follow-upPlatelet count, 28 Day Follow-upLymphocytes, Day 1Lymphocytes, Day 4Lymphocytes, Day 8Lymphocytes, Day 11Lymphocytes, 7 Day Follow-upLymphocytes, 28 Day Follow-up
GSK1322322 1500 mg BID0.0270.0300.0270.0300.0320.0240.1490.1490.1650.1750.1510.1410.4320.3540.3700.3200.3450.3846.5334.7574.3714.4954.1114.7099.157.356.826.776.447.16285.5296.5293.0280.2264.0279.32.0122.0571.8901.7491.8061.907
Linezolid 600 mg BID0.0350.0350.0350.0200.0270.0310.1400.1450.1550.1680.1280.1500.5170.4080.3880.4200.4100.4717.2314.9844.7804.5244.8215.4969.877.547.307.067.488.10255.0273.2268.3253.9249.8240.51.9471.9681.9411.9252.0911.955

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Mean Short Form McGill Pain Questionnaire-2 (SF-MPQ-2) Sub-score of Continuous Pain, Intermittent Pain, Neuropathic Pain and Affective Descriptors at Indicated Time Points

SF-MPQ-2 is composed of 22 items that describes different quantities of pain and related symptoms. Sub-score of continuous pain represents mean of throbbing pain, cramping pain, gnawing pain, aching pain, heavy pain and tender (mean of items 1, 5, 6, 8, 9 and 10). Sub-score of intermittent pain represents mean of shooting pain, stabbing pain, sharp pain, splitting pain, electric-shock pain and piercing (mean of items 2, 3, 4, 11, 16 and 18). Sub-score of neuropathic pain represents mean of hot-burning pain, cold-freezing pain, pain caused by light touch, itching, tingling or pins and needles, numbness (mean of items 7, 17, 19, 20, 21 and 22). Sub-score of affective descriptors represents mean of tiring-exhaustive, sickening, fearful, punishing-cruel (mean of items 12, 13, 14 and 15). Scores ranged from 0 to 10, where 0 indicated absence of symptom and higher score indicated more severe symptoms. Assessments were done at Day 1, Day 2, Day 3, Day 4, Day 8, Day 11 and 7 Day Follow-up. (NCT01209078)
Timeframe: Up to Follow-up (7 Day Follow up, Day 19)

,
InterventionScores on scale (Mean)
Continuous Pain, Day 1Continuous Pain, Day 2Continuous Pain, Day 3Continuous Pain, Day 4Continuous Pain, Day 8Continuous Pain, Day 11Continuous Pain, 7 Day Follow-upIntermittent Pain, Day 1Intermittent Pain, Day 2Intermittent Pain, Day 3Intermittent Pain, Day 4Intermittent Pain, Day 8Intermittent Pain, Day 11Intermittent Pain, 7 Day Follow-upNeuropathic Pain, Day 1Neuropathic Pain, Day 2Neuropathic Pain, Day 3Neuropathic Pain, Day 4Neuropathic Pain, Day 8Neuropathic Pain, Day 11Neuropathic Pain, 7 Day Follow-upAffective Descriptors, Day 1Affective Descriptors, Day 2Affective Descriptors, Day 3Affective Descriptors, Day 4Affective Descriptors, Day 8Affective Descriptors, Day 11Affective Descriptors, 7 Day Follow-up
GSK1322322 1500 mg BID4.4593.4072.8262.6451.4200.8820.7333.8362.3372.0781.9060.8710.5040.5813.5202.7052.3272.3911.5080.8130.6903.3602.2261.9291.6410.8520.6400.483
Linezolid 600 mg BID4.8893.5332.7442.0671.3890.8060.5333.8022.6932.2441.6201.2360.6880.4403.8462.1932.0261.6131.4100.7780.5932.8062.5001.6921.3301.0210.4900.430

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Mean Total SIS at Indicated Time Points

The investigator evaluated the infection by grading the infected lesion according to SIS. The SIS consist of 7 items of exudate or pus, crusting, erythema or inflammation, tissue warmth, tissue edema, itching and pain. The items were rated on a 7-point scale ranging from 0 to 6, where 0 indicated absence of symptom and 6 indicated severe symptom. The total score ranged from 0 to 42, where 0 indicated absence of symptoms and higher score indicated more severe symptoms. Assessments were done at Day 1, Day 2, Day 3, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionScores on scale (Mean)
Day 1Day 2Day 3Day 4Day 8Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg BID25.722.217.214.68.83.72.40.3
Linezolid 600 mg BID26.023.318.114.16.92.31.80.1

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Mean Vital Sign Value of Heart Rate (HR) at Indicated Time Points

Vital sign assessments were conducted at Day 1 (pre-dose), Day 2 (pre-dose), Day 3 (pre-dose), Day 4 (4-12 hours post-dose), Day 8 (pre-dose) and Day 11. The assessments were made with the participant in a semi-supine position, having rested in that position for at least 10 minutes beforehand. Three HR measurements were taken at pre-dose on Day 1. The mean value recorded at pre-dose was classified as Baseline. Single HR was obtained at all other time points during the study. (NCT01209078)
Timeframe: Up to Day 11

,
InterventionBeats per minute (Mean)
Day 1Day 2Day 3Day 4Day 8Day 11
GSK1322322 1500 mg BID74.981.277.671.969.970.9
Linezolid 600 mg BID73.976.276.174.669.274.0

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Mean Vital Sign Value of Respiratory Rate (RR) at Indicated Time Points

Vital sign assessments were conducted at Day 1 (pre-dose), Day 2 (pre-dose), Day 3 (pre-dose), Day 4 (4-12 hours post-dose), Day 8 (pre-dose) and Day 11. The assessments were made with the participant in a semi-supine position, having rested in that position for at least 10 minutes beforehand. Three RR measurements were taken at pre-dose on Day 1. The mean value recorded at pre-dose was classified as Baseline. Single RR was obtained at all other time points during the study. (NCT01209078)
Timeframe: Up to Day 11

,
InterventionBreaths per minute (Mean)
Day 1Day 2Day 3Day 4Day 8Day 11
GSK1322322 1500 mg BID17.117.317.417.317.117.6
Linezolid 600 mg BID17.917.417.317.417.216.8

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Mean Vital Sign Value of Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Indicated Time Points

Vital sign assessments were conducted at Day 1 (pre-dose), Day 2 (pre-dose), Day 3 (pre-dose), Day 4 (4-12 hours post-dose), Day 8 (pre-dose) and Day 11. The assessments were made with the participant in a semi-supine position, having rested in that position for at least 10 minutes beforehand. Three BP measurements were taken at pre-dose on Day 1. The mean value recorded at pre-dose was classified as Baseline. Single BP was obtained at all other time points during the study. (NCT01209078)
Timeframe: Up to Day 11

,
InterventionMillimeters of mercury (mmHg) (Mean)
DBP, Day 1DBP, Day 2DBP, Day 3DBP, Day 4DBP, Day 8DBP, Day 11SBP, Day 1SBP, Day 2SBP, Day 3SBP, Day 4SBP, Day 8SBP, Day 11
GSK1322322 1500 mg BID78.176.073.669.773.573.6125.6119.2120.0119.3122.7122.0
Linezolid 600 mg BID74.576.777.376.872.172.8123.1125.1126.9126.1121.2120.4

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Number of Participants With Abnormal Transition From Baseline in Clinical Chemistry Values Relative to Normal Range

The parameters of clinical chemistry included albumin, total protein, ALT, ALP, AST, GGT, LDH and creatine kinase, creatinine, uric acid, direct bilirubin, total bilirubin, glucose, sodium, calcium, potassium, chloride, CO2 content /bicarbonate and urea/BUN and high sensitivity C-Reactive protein. The assessments were done at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline was defined as the assessment done on Day 1 (pre-dose). Data is reported for number of participants with abnormal transition from Baseline 'to high' or 'to low' relative to normal range. Only those parameters for which at least one value of abnormal transition was reported are summarized. (NCT01209078)
Timeframe: Day 1 (pre-dose, Baseline) up Follow-up (28 Day Follow-up, Day 40)

,
InterventionParticipants (Count of Participants)
Day 2, C-Reactive protein, to highDay 3, C-Reactive protein, to highDay 4, ALT, to highDay 4, ALP, to highDay 4, AST, to highDay 4, Calcium, to lowDay 4, CO2/bicarbonate, to lowDay 4, Chloride, to lowDay 4, Creatine kinase, to highDay 4, Creatinine, to lowDay 4, GGT, to highDay 4, Glucose, to lowDay 4, Glucose, to highDay 4, Potassium, to lowDay 4, Sodium, to lowDay 4, Total protein, to lowDay 4, Urea/BUN, to lowDay 4, Urea/BUN, to highDay 4, Uric acid, to lowDay 8, ALT, to highDay 8, Albumin, to lowDay 8, AST, to highDay 8, Calcium, to lowDay 8, Chloride, to highDay 8, Creatine kinase, to highDay 8, Creatinine, to lowDay 8, GGT, to highDay 8, Glucose, to lowDay 8, Glucose, to highDay 8, Sodium, to lowDay 8, Urea/BUN, to lowDay 8, Uric acid, to lowDay 11, ALT, to highDay 11, AST, to highDay 11, Calcium, to lowDay 11, CO2/bicarbonate, to lowDay 11, Chloride, to lowDay 11, Chloride, to highDay 11, Creatine kinase, to highDay 11, Creatinine, to lowDay 11, GGT, to highDay 11, Glucose, to lowDay 11, Glucose, to highDay 11, C-Reactive protein, to highDay 11, Potassium, to lowDay 11, Sodium, to lowDay 11, Total protein, to highDay 11, Urea/BUN, to lowDay 11, Urea/BUN, to highDay 11, Uric acid, to lowDay 11, Uric acid, to high7 Day Follow-up, ALT, to high7 Day Follow-up, AST, to high7 Day Follow-up, Calcium, to low7 Day Follow-up, Calcium, to high7 Day Follow-up, CO2/bicarbonate, to low7 Day Follow-up, Chloride, to low7 Day Follow-up, Chloride, to high7 Day Follow-up, Creatine kinase, to high7 Day Follow-up, Creatinine, to low7 Day Follow-up, Creatinine, to high7 Day Follow-up, Direct bilirubin, to high7 Day Follow-up, GGT, to high7 Day Follow-up, Glucose, to high7 Day Follow-up, C-Reactive protein, to high7 Day Follow-up, Potassium, to low7 Day Follow-up, Sodium, to low7 Day Follow-up, Total bilirubin, to high7 Day Follow-up, Total protein, to high7 Day Follow-up, Urea/BUN, to low7 Day Follow-up, Urea/BUN, to high7 Day Follow-up, Uric acid, to low7 Day Follow-up, Uric acid, to high28 Day Follow-up, ALT, to high28 Day Follow-up, ALP, to high28 Day Follow-up, AST, to high28 Day Follow-up, Calcium, to low28 Day Follow-up, Calcium, to high28 Day Follow-up, CO2/bicarbonate, to low28 Day Follow-up, Chloride, to low28 Day Follow-up, Chloride, to high28 Day Follow-up, Creatine kinase, to high28 Day Follow-up, Creatinine, to low28 Day Follow-up, Creatinine, to high28 Day Follow-up, GGT, to high28 Day Follow-up, Glucose, to high28 Day Follow-up, Potassium, to low28 Day Follow-up, Sodium, to low28 Day Follow-up, Total protein, to low28 Day Follow-up, Total protein, to high28 Day Follow-up, Urea/BUN, to low28 Day Follow-up, Uric acid, to low28 Day Follow-up, Uric acid, to high
GSK1322322 1500 mg BID111126415232716120511431444171223515012233810012002661140144013401111111520131102521172021101
Linezolid 600 mg BID000010303210200101020200111151002202110200211100110300021133100211001111001100613230131200020

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Number of Participants With Abnormal Transition From Baseline in Hematology Values Relative to Normal Range

The parameters of clinical chemistry included basophils, eosinophils, lymphocytes, monocytes, total neutrophils, WBC count, platelet count, MCV, hemoglobin, MCHC, MCH, RBC count and reticulocyte count. The assessments were done at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline was defined as the assessment done on Day 1 (pre-dose). Data is reported for number of participants with abnormal transition from Baseline 'to high' or 'to low' relative to normal range. Only those parameters for which at least one value of abnormal transition was reported are summarized. (NCT01209078)
Timeframe: Day 1 (pre-dose, Baseline) up Follow-up (28 Day Follow-up, Day 40)

,
InterventionParticipants (Count of Participants)
Day 4, Eosinophils, to lowDay 4, Eosinophils, to highDay 4, Hemoglobin, to lowDay 4, Lymphocytes, to lowDay 4, MCHC, to lowDay 4, Monocytes, to lowDay 4, Monocytes, to highDay 4, Platelet count, to highDay 4, RBC count, to lowDay 4, Reticulocytes, to lowDay 4, Reticulocytes, to highDay 4, Total neutrophils, to lowDay 4, Total neutrophils, to highDay 4, WBC count, to lowDay 4, WBC count, to highDay 8, Eosinophils, to lowDay 8, Hemoglobin, to lowDay 8, Lymphocytes, to lowDay 8, MCHC, to lowDay 8, MCV, to highDay 8, Monocytes, to lowDay 8, Platelet count, to highDay 8, RBC count, to lowDay 8, Reticulocytes, to lowDay 8, Reticulocytes, to highDay 8, Total neutrophils, to lowDay 8, Total neutrophils, to highDay 8, WBC count, to lowDay 11, Eosinophils, to lowDay 11, Hemoglobin, to lowDay 11, Hemoglobin, to highDay 11, Lymphocytes, to lowDay 11, Monocytes, to lowDay 11, Platelet count, to highDay 11, RBC count, to lowDay 11, Reticulocytes, to lowDay 11, Reticulocytes, to highDay 11, Total neutrophils, to lowDay 11, Total neutrophils, to highDay 11, WBC count, to lowDay 11, WBC count, to high7 Day Follow-up, Eosinophils, to low7 Day Follow-up, Hemoglobin, to low7 Day Follow-up, Lymphocytes, to low7 Day Follow-up, Monocytes, to low7 Day Follow-up, Platelet count, to low7 Day Follow-up, RBC count, to low7 Day Follow-up, Reticulocytes, to low7 Day Follow-up, Reticulocytes, to high7 Day Follow-up, Total neutrophils, to low7 Day Follow-up, Total neutrophils, to high7 Day Follow-up, WBC count, to low7 Day Follow-up, WBC count, to high28 Day Follow-up, Eosinophils, to low28 Day Follow-up, Hemoglobin, to low28 Day Follow-up, Hemoglobin, to high28 Day Follow-up, Lymphocytes, to low28 Day Follow-up, Lymphocytes, to high28 Day Follow-up, MCHC, to low28 Day Follow-up, Monocytes, to low28 Day Follow-up, Platelet count, to low28 Day Follow-up, Platelet count, to high28 Day Follow-up, RBC count, to low28 Day Follow-up, Reticulocytes, to low28 Day Follow-up, Reticulocytes, to high28 Day Follow-up, Total neutrophils, to low28 Day Follow-up, Total neutrophils, to high28 Day Follow-up, WBC count, to low28 Day Follow-up, WBC count, to high
GSK1322322 1500 mg BID613123022121121311113210530222135123311210115124111111111111020031112
Linezolid 600 mg BID1030011141100102200000242010120010114100031110101001011300000104140101

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Number of Participants With Any Adverse Events (AE) and Serious Adverse Events (SAE)

An AE is defined as any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life-threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect, may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed in this definition, associated with liver injury and impaired liver function defined as alanine aminotransferase (ALT) >=3 x upper limit of normal (ULN), and total bilirubin >=2 x ULN or international normalised ratio >1.5. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionParticipants (Count of Participants)
Any AEAny SAE
GSK1322322 1500 mg BID491
Linezolid 600 mg BID201

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Number of Participants With Clinical Success of Clinical Response

The clinical response was evaluated by the investigator at end of therapy (within 3 days post therapy; Day 12-14) and Follow-up (7 day Follow-up; Day 16 to 19 and 28 day Follow-up; Day 37 to 40). Clinical response was determined after clinical evaluation of reviewing clinical signs and symptoms. Clinical success was defined as total resolution of all signs and symptoms of infection recorded at Baseline, or improvement to such an extent that no further antimicrobial therapy was necessary, including a pus/exudate skin infection score (SIS) of 0. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionParticipants (Count of Participants)
Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg BID383837
Linezolid 600 mg BID242523

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Percentage of Participants With Clinical Success at End of Therapy by Pathogen Isolated at Baseline

Clinical success was defined as total resolution of all signs and symptoms of infection recorded at Baseline, or improvement to such an extent that no further antimicrobial therapy was necessary, including a pus/exudates SIS of 0. The pathogens isolated at Baseline included staphylococcus aureus (methicillin-resistant staphylococcus aureus [MRSA] and methicillin-susceptible staphylococcus aureus [MSSA] as defined by susceptibility to cefoxitin or oxacilin), streptococcus pyogenes, other streptococcus species, other Gram-positive pathogens and Gram-negative pathogens. Data is categorized for the percentage of participants with clinical success for each of the pathogens, all pathogens and no pathogens. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

InterventionPercentage of participants (Number)
Staphylococcus aureus (all)MRSAMSSAStreptococcus pyogenesGram-negative pathogensAll pathogensNo pathogens
GSK1322322 1500 mg BID58.350.071.433.375.058.180.0

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Percentage of Participants With Clinical Success at End of Therapy by Pathogen Isolated at Baseline

Clinical success was defined as total resolution of all signs and symptoms of infection recorded at Baseline, or improvement to such an extent that no further antimicrobial therapy was necessary, including a pus/exudates SIS of 0. The pathogens isolated at Baseline included staphylococcus aureus (methicillin-resistant staphylococcus aureus [MRSA] and methicillin-susceptible staphylococcus aureus [MSSA] as defined by susceptibility to cefoxitin or oxacilin), streptococcus pyogenes, other streptococcus species, other Gram-positive pathogens and Gram-negative pathogens. Data is categorized for the percentage of participants with clinical success for each of the pathogens, all pathogens and no pathogens. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

InterventionPercentage of participants (Number)
Staphylococcus aureus (all)MRSAMSSAStreptococcus pyogenesOther Streptococcus speciesOther Gram-positive pathogensGram-negative pathogensAll pathogensNo pathogens
Linezolid 600 mg BID93.887.5100.0100.0100.0100.0100.095.777.8

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Percentage of Participants With Clinical Success of Clinical Outcome

The clinical response was determined by the investigator after clinical evaluation of reviewing clinical signs and symptoms at end of therapy (within 3 days post therapy; visit window of Day 12-14) and 7 day Follow-up ( visit window of Day 16 to 19), and the resulting clinical outcome was assigned, for each participant. Clinical success was defined as total resolution of all signs and symptoms of infection recorded at Baseline, or improvement to such an extent that no further antimicrobial therapy was necessary, including a pus/exudates SIS of 0. (NCT01209078)
Timeframe: Day 11 (end of therapy) and Follow-up (7 Day Follow-up, Day 19)

,
InterventionPercentage of participants (Number)
End of therapyFollow-up
GSK1322322 1500 mg BID66.764.9
Linezolid 600 mg BID88.988.9

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Mean Clinical Chemistry Parameter of Estradiol at Indicated Time Point

Blood samples were obtained for analysis of estradiol at Day 1. (NCT01209078)
Timeframe: Day 1

InterventionPicomole (pmol)/Liter (Mean)
GSK1322322 1500 mg BID261.8
Linezolid 600 mg BID61.3

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Percentage of Participants With Microbiological Success of Microbiological Outcome at End of Therapy

The 'by pathogen' microbiological response was determined by comparing the Baseline (Day 1) culture results to the culture results at the end of therapy (visit window of Day 12-14), and the corresponding microbiological outcome (success or failure) by participant was then assigned. Microbiological success was defined as: elimination of Baseline pathogens (defined as microbiological eradication in microbiological response); clinical outcome was success such that no culture was obtained due to lack of culturable material, secondary to adequate clinical response, and was documented in the electronic case report form (eCRF) (defined as presumed microbiological eradication in microbiological response); new pathogen not previously identified, was identified at end of therapy in a participant who was a 'clinical success' (defined as colonization in microbiological response). (NCT01209078)
Timeframe: Day 11 (end of therapy)

InterventionPercentage of participants (Number)
GSK1322322 1500 mg BID59.5
Linezolid 600 mg BID94.4

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Percentage of Participants With Microbiological Success of Microbiological Outcome at Follow-up

The 'by pathogen' microbiological response was determined by comparing the Baseline (Day 1) culture results to culture results at Follow-up (Day 16-19), and corresponding microbiological outcome (success or failure) by participant was then assigned. Microbiological success was defined as: Baseline pathogen was eradicated or presumed eradicated at end of therapy, or Baseline pathogens were present at end of therapy and is absent at Follow-up (microbiological eradication in microbiological response); Baseline pathogen was eradicated or presumed eradicated at end of therapy, or the Baseline pathogens were present at end of therapy and, participant was a 'clinical success', such that no culture was obtained due to lack of culturable material, secondary to adequate clinical response, and was documented in the eCRF (microbiological eradication); a new pathogen, not previously identified at Baseline, was identified at Follow-up in a participant who was a 'clinical success' (colonization) (NCT01209078)
Timeframe: Follow-up (7 Day Follow-up, Day 19)

InterventionPercentage of participants (Number)
GSK1322322 1500 mg BID59.5
Linezolid 600 mg BID94.4

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Percentage of Participants With Therapeutic Success of Therapeutic Outcome

Therapeutic outcome was combined clinical and microbiological outcome. Therapeutic outcome was a measure of the overall efficacy response, and a therapeutic success referred to participants who had been deemed both a 'clinical success' and a 'microbiological success'. All other combinations (other than 'clinical success' + 'microbiological success') were deemed failures for therapeutic outcome. Therapeutic outcome was determined programmatically, obtained at 7 day Follow-up. (NCT01209078)
Timeframe: Follow-up (7 day Follow-up, Day 19)

InterventionPercentage of participants (Number)
GSK1322322 1500 mg BID0.8636
Linezolid 600 mg BID1.0000

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Mean Change From Baseline in ECG Rhythms at Indicated Time Points

12-lead ECGs were obtained during the study using an ECG machine that automatically calculated the heart rhythm and measured PR, QRS, RR, QT, and QTc intervals. It was performed with the participant in a semi-supine position having rested in that position for at least 10 minutes beforehand. Three measurements were taken at pre-dose on Day 1 at least 5 minutes apart and the mean of the three measurements was calculated. The assessments were done at Day 1 (pre-dose, 0.25-1.5 hours post-initial dose and 1.5-3 hours post-initial dose), Day 4 (4-12 hours post-morning dose), Day 8 (pre-morning dose) and Day 11 (0 hour). The value recorded pre-dose on Day 1 was the Baseline. The change from Baseline was calculated by subtracting the Baseline value from the individual post-Baseline (Day 1 post-dose, Day 4, Day 8 and Day 11) values. (NCT01209078)
Timeframe: Day 1 (pre-dose, Baseline) up to Day 11

,
InterventionBeats per minute (Mean)
Day 1, 0.25-1.5 h post-doseDay 1, 1.5-3 h post-doseDay 4, 4-12 h post-doseDay 8, pre morning doseDay 11, 0 h
GSK1322322 1500 mg BID4.25.9-3.1-5.2-3.2
Linezolid 600 mg BID-0.92.92.4-3.51.1

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Mean Change From Baseline in ECG Values at Indicated Time Points

12-lead ECGs were obtained during the study using an ECG machine that automatically calculated the heart rate and measured PR, QRS, RR, QT, and QTc intervals. It was performed with the participant in a semi-supine position having rested in that position for at least 10 minutes beforehand. Three measurements were taken at pre-dose on Day 1 at least 5 minutes apart. The mean PR interval, RR interval, QRS duration, uncorrected QT interval (UncQT) and QTcB (QT corrected by Bazett's formula) and QTcF (corrected by Friedericia's formula) was calculated from automated ECG readings. The assessments were done at Day 1 (pre-dose, 0.25-1.5 hours post-initial dose and 1.5-3 hours post-initial dose), Day 4 (4-12 hours post-morning dose), Day 8 (pre-morning dose) and Day 11 (0 hour). Mean value recorded pre-dose on Day 1 was classified as Baseline. Change from Baseline was calculated by subtracting the Baseline value from individual post-Baseline (Day 1 post-dose, Day 4, Day 8 and Day 11) values. (NCT01209078)
Timeframe: Day 1 (pre-dose, Baseline) up to Day 11

,
Interventionmsec (Mean)
PR interval, Day 1, 0.25-1.5 h post dosePR interval, Day 1, 1.5-3 h post dosePR interval, Day 4, 4-12 h post dosePR interval, Day 8, pre morning dosePR interval, Day 11, 0 hQRS duration, Day 1, 0.25-1.5 h post doseQRS duration, Day 1, 1.5-3 h post doseQRS duration, Day 4, 4-12 h post doseQRS duration, Day 8, pre morning doseQRS duration, Day 11, 0 hUncQT interval, Day 1, 0.25-1.5 h post doseUncQT interval, Day 1, 1.5-3 h post doseUncQT interval, Day 4, 4-12 h post doseUncQT interval, Day 8, pre morning doseUncQT interval, Day 11, 0 hQTcB interval, Day 1, 0.25-1.5 h post doseQTcB interval, Day 1, 1.5-3 h post doseQTcB interval, Day 4, 4-12 h post doseQTcB interval, Day 8, pre morning doseQTcB interval, Day 11, 0 hQTcF interval, Day 1, 0.25-1.5 h post doseQTcF interval, Day 1, 1.5-3 h post doseQTcF interval, Day 4, 4-12 h post doseQTcF interval, Day 8, pre morning doseQTcF interval, Day 11, 0 hRR interval, Day 1, 0.25-1.5 h post doseRR interval, Day 1, 1.5-3 h post doseRR interval, Day 4, 4-12 h post doseRR interval, Day 8, pre morning doseRR interval, Day 11, 0 h
GSK1322322 1500 mg BID-1.00.46.37.1-1.2-0.21.61.61.01.2-6.0-7.114.117.68.25.18.58.45.40.01.13.010.69.82.9-49.2-66.423.751.633.9
Linezolid 600 mg BID4.21.32.2-0.01.51.20.3-2.2-0.2-0.2-3.1-7.20.510.51.5-3.81.97.33.33.0-3.4-1.24.95.92.30.4-43.0-12.244.6-5.1

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Mean Change From Baseline in HR at Indicated Time Points

Vital sign assessments were conducted at Day 1 (pre-dose), Day 2 (pre-dose), Day 3 (pre-dose), Day 4 (4-12 hours post-dose), Day 8 (pre-dose) and Day 11. The assessments were made with the participant in a semi-supine position, having rested in that position for at least 10 minutes beforehand. Three HR measurements were taken at pre-dose on Day 1. The mean value recorded at pre-dose was classified as Baseline. Single HR was obtained at all other time points during the study. The change from Baseline was calculated by subtracting the Baseline value from the individual post-Baseline (Day 2, Day 3, Day 4, Day 8 and Day 11) values. If either the Baseline or post-Baseline value was missing, the change from Baseline was set to missing as well. (NCT01209078)
Timeframe: Day 1 (Baseline) up to Day 11

,
InterventionBeats per minute (Mean)
Day 2Day 3Day 4Day 8Day 11
GSK1322322 1500 mg BID6.52.2-1.4-3.0-2.5
Linezolid 600 mg BID3.74.02.5-2.71.7

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Mean Change From Baseline in RR at Indicated Time Points

Vital sign assessments were conducted at Day 1 (pre-dose), Day 2 (pre-dose), Day 3 (pre-dose), Day 4 (4-12 hours post-dose), Day 8 (pre-dose) and Day 11. The assessments were made with the participant in a semi-supine position, having rested in that position for at least 10 minutes beforehand. Three RR measurements were taken at pre-dose on Day 1. The mean value recorded at pre-dose was classified as Baseline. Single RR was obtained at all other time points during the study. The change from Baseline was calculated by subtracting the Baseline value from the individual post-Baseline (Day 2, Day 3, Day 4, Day 8 and Day 11) values. If either the Baseline or post-Baseline value was missing, the change from Baseline was set to missing as well. (NCT01209078)
Timeframe: Day 1 (Baseline) up to Day 11

,
InterventionBreaths per minute (Mean)
Day 2Day 3Day 4Day 8Day 11
GSK1322322 1500 mg BID0.40.50.40.20.6
Linezolid 600 mg BID-0.7-0.7-0.6-0.8-1.2

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Mean Change From Baseline in SBP and DBP at Indicated Time Points

Vital sign assessments were conducted at Day 1 (pre-dose), Day 2 (pre-dose), Day 3 (pre-dose), Day 4 (4-12 hours post-dose), Day 8 (pre-dose) and Day 11. The assessments were made with the participant in a semi-supine position, having rested in that position for at least 10 minutes beforehand. Three BP measurements were taken at pre-dose on Day 1. The mean value recorded at pre-dose was classified as Baseline. Single BP was obtained at all other time points during the study. The change from Baseline was calculated by subtracting the Baseline value from the individual post-Baseline (Day 2, Day 3, Day 4, Day 8 and Day 11) values. If either the Baseline or post-Baseline value was missing, the change from Baseline was set to missing as well. (NCT01209078)
Timeframe: Day 1 (Baseline) up to Day 11

,
InterventionmmHg (Mean)
SBP, Day 2SBP, Day 3SBP, Day 4SBP, Day 8SBP, Day 11DBP, Day 2DBP, Day 3DBP, Day 4DBP, Day 8DBP, Day 11
GSK1322322 1500 mg BID-6.5-5.2-6.5-2.5-2.7-2.6-4.8-8.7-4.7-4.4
Linezolid 600 mg BID1.63.73.1-2.7-2.61.82.72.5-2.8-1.7

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Mean Change From Baseline in Total SIS at Indicated Time Points

The investigator evaluated the infection by grading the infected lesion according to SIS. The SIS consist of 7 items of exudate or pus, crusting, erythema or inflammation, tissue warmth, tissue edema, itching and pain. The items were rated on a 7-point scale ranging from 0 to 6, where 0 indicated absence of symptom and 6 indicated severe symptom. The total score ranged from 0 to 42, where 0 indicated absence of symptoms and higher score indicated more severe symptoms. Baseline was defined as the assessment value done on Day 1. The change from Baseline was calculated by subtracting the Baseline value from the individual post-Baseline (Day 1, Day 2, Day 3, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up) values. If either the Baseline or post-Baseline value was missing, the change from Baseline was set to missing as well. (NCT01209078)
Timeframe: Day 1 (Baseline ) up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionScores on scale (Mean)
Day 2Day 3Day 4Day 8Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg BID-3.4-8.4-10.9-16.8-22.0-23.0-25.1
Linezolid 600 mg BID-3.1-8.0-11.9-19.0-23.6-24.2-26.1

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Mean Change From Baseline in Wound Area at Indicated Time Points

The area of the infected lesion size was calculated as the product between the length (L) and width (W) of the lesion size. The wound was measured by the investigator in centimeters (cm), using a standard metric ruler. Baseline was defined as the assessment value done on Day 1. The change from Baseline was calculated by subtracting the Baseline value from the individual post-Baseline (Day 1, Day 2, Day 3, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up) values. If either the Baseline or post-Baseline value was missing, the change from Baseline was set to missing as well. (NCT01209078)
Timeframe: Day 1 (Baseline) up to Follow-up (28 Day Follow-up, Day 40)

,
Interventioncm^2 (Mean)
Day 2Day 3Day 4Day 8Day 117 Day Follow-up28 Day Follow-up
GSK1322322 1500 mg BID-23.22-67.69-119.96-192.92-234.99-231.32-242.92
Linezolid 600 mg BID-20.71-124.27-209.79-291.86-329.93-335.20-344.99

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Mean Clinical Chemistry Parameter of High Sensitivity C-Reactive Protein at Indicated Time Points

Blood samples were obtained for analysis of high sensitivity C-Reactive protein at Day 1, Day 2, Day 3, Day 4, Day 8, Day 11 and 7 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (7 Day Follow-up, Day 19)

,
Interventionmg/Liter (Mean)
Day 1Day 2Day 3Day 4Day 8Day 117 Day Follow-up
GSK1322322 1500 mg BID38.3933.7627.1315.716.877.5610.25
Linezolid 600 mg BID43.9740.7230.9921.826.024.747.29

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Mean Clinical Chemistry Parameters of Albumin and Total Protein at Indicated Time Points

Blood samples were obtained for analysis of albumin and total protein at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionGram/Liter (Mean)
Albumin, Day 1Albumin, Day 4Albumin, Day 8Albumin, Day 11Albumin, 7 Day Follow-upAlbumin, 28 Day Follow-upTotal protein, Day 1Total protein, Day 4Total protein, Day 8Total protein, Day 11Total protein, 7 Day Follow-upTotal protein, 28 Day Follow-up
GSK1322322 1500 mg BID39.940.040.340.941.441.572.672.072.873.273.573.2
Linezolid 600 mg BID40.340.540.442.242.841.172.272.471.373.474.372.6

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Mean Clinical Chemistry Parameters of ALT, Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Follicle Stimulating Hormone (FSH), Gamma Glutamyl Transferase (GGT), Lactate Dehydrogenase (LDH) and Creatine Kinase at Indicated Time Points

Blood samples were obtained for analysis of ALT, ALP, AST, FSH, GGT, LDH and creatine kinase at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

InterventionInternational units (IU)/Liter (Mean)
ALP, Day 1ALP, Day 4ALP, Day 8ALP, Day 11ALP, 7 Day Follow-upALP, 28 Day Follow-upALT, Day 1ALT, Day 4ALT, Day 8ALT, Day 11ALT, 7 Day Follow-upALT, 28 Day Follow-upAST, Day 1AST, Day 4AST, Day 8AST, Day 11AST, 7 Day Follow-upAST, 28 Day Follow-upCreatine kinase, Day 1Creatine kinase, Day 4Creatine kinase, Day 8Creatine kinase, Day 11Creatine kinase, 7 Day Follow-upCreatine kinase, 28 Day Follow-upFSH, Day 1GGT, Day 1GGT, Day 4GGT, Day 8GGT, Day 11GGT, 7 Day Follow-upGGT, 28 Day Follow-up
Linezolid 600 mg BID97.792.488.289.390.992.927.325.434.032.232.622.726.324.729.328.528.724.0191.1166.7120.3169.3189.1117.516.0552.653.457.753.552.842.1

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Mean Clinical Chemistry Parameters of ALT, Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Follicle Stimulating Hormone (FSH), Gamma Glutamyl Transferase (GGT), Lactate Dehydrogenase (LDH) and Creatine Kinase at Indicated Time Points

Blood samples were obtained for analysis of ALT, ALP, AST, FSH, GGT, LDH and creatine kinase at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

InterventionInternational units (IU)/Liter (Mean)
ALP, Day 1ALP, Day 4ALP, Day 8ALP, Day 11ALP, 7 Day Follow-upALP, 28 Day Follow-upALT, Day 1ALT, Day 4ALT, Day 8ALT, Day 11ALT, 7 Day Follow-upALT, 28 Day Follow-upAST, Day 1AST, Day 4AST, Day 8AST, Day 11AST, 7 Day Follow-upAST, 28 Day Follow-upCreatine kinase, Day 1Creatine kinase, Day 4Creatine kinase, Day 8Creatine kinase, Day 11Creatine kinase, 7 Day Follow-upCreatine kinase, 28 Day Follow-upFSH, Day 1GGT, Day 1GGT, Day 4GGT, Day 8GGT, Day 11GGT, 7 Day Follow-upGGT, 28 Day Follow-upLDH, Day 1
GSK1322322 1500 mg BID102.595.094.895.495.695.226.530.134.339.437.528.425.927.332.034.635.530.2118.1135.2117.3135.8204.7155.321.4752.955.357.755.765.150.1172.0

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Mean Clinical Chemistry Parameters of Creatinine, Uric Acid, Direct Bilirubin and Total Bilirubin at Indicated Time Points

Blood samples were obtained for analysis of creatinine, uric acid, direct bilirubin and total bilirubin at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionMicromoles (µmol)/liter (Mean)
Creatinine, Day 1Creatinine, Day 4Creatinine, Day 8Creatinine, Day 11Creatinine, 7 Day Follow-upCreatinine, 28 Day Follow-upUric acid, Day 1Uric acid, Day 4Uric acid, Day 8Uric acid, Day 11Uric acid, 7 Day Follow-upUric acid, 28 Day Follow-upDirect bilirubin, Day 1Direct bilirubin, Day 4Direct bilirubin, Day 8Direct bilirubin, Day 11Direct bilirubin, 7 Day Follow-upDirect bilirubin, 28 Day Follow-upTotal bilirubin, Day 1Total bilirubin, Day 4Total bilirubin, Day 8Total bilirubin, Day 11Total bilirubin, 7 Day Follow-upTotal bilirubin, 28 Day Follow-up
GSK1322322 1500 mg BID68.7371.4874.8574.1970.8472.77322.5282.2323.2370.5386.0358.32.32.42.42.52.62.38.77.37.68.18.18.5
Linezolid 600 mg BID66.9972.3573.4272.0775.0672.49293.3346.4360.4367.4363.8332.62.52.01.92.13.02.38.46.66.67.68.97.6

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Mean Clinical Chemistry Parameters of Glucose, Sodium, Calcium, Potassium, Chloride, Carbon Dioxide (CO2) Content /Bicarbonate and Urea/ Blood Urea Nitrogen (BUN) at Indicated Time Points

Blood samples were obtained for analysis of glucose, sodium, calcium, potassium, chloride, CO2 content /bicarbonate and urea/BUN at Day 1, Day 4, Day 8, Day 11, 7 Day Follow-up and 28 Day Follow-up. Baseline value was defined as the assessment done on Day 1. (NCT01209078)
Timeframe: Up to Follow-up (28 Day Follow-up, Day 40)

,
InterventionMillimole (mmol)/Liter (Mean)
Glucose, Day 1Glucose, Day 4Glucose, Day 8Glucose, Day 11Glucose, 7 Day Follow-upGlucose, 28 Day Follow-upSodium, Day 1Sodium, Day 4Sodium, Day 8Sodium, Day 11Sodium, 7 Day Follow-upSodium, 28 Day Follow-upCalcium, Day 1Calcium, Day 4Calcium, Day 8Calcium, Day 11Calcium, 7 Day Follow-upCalcium, 28 Day Follow-upPotassium, Day 1Potassium, Day 4Potassium, Day 8Potassium, Day 11Potassium, 7 Day Follow-upPotassium, 28 Day Follow-upChloride, Day 1Chloride, Day 4Chloride, Day 8Chloride, Day 11Chloride, 7 Day Follow-upChloride, 28 Day Follow-upCO2 content/bicarbonate, Day 1CO2 content/bicarbonate, Day 4CO2 content/bicarbonate, Day 8CO2 content/bicarbonate, Day 11CO2 content/bicarbonate, 7 Day Follow-upCO2 content/bicarbonate, 28 Day Follow-upUrea/BUN, Day 1Urea/BUN, Day 4Urea/BUN, Day 8Urea/BUN, Day 11Urea/BUN, 7 Day Follow-upUrea/BUN, 28 Day Follow-up
GSK1322322 1500 mg BID6.216.135.946.275.966.10138.3137.3137.8138.6139.2138.82.2642.2172.2672.3012.3152.3064.184.194.184.124.164.04102.3101.9102.9104.2104.7103.721.722.322.221.621.922.34.904.814.474.694.844.88
Linezolid 600 mg BID6.636.775.776.656.406.76138.3138.3138.4138.2138.5138.82.2512.2572.2732.2822.3032.2634.084.114.134.044.064.13102.4103.0103.8102.7102.6103.721.123.022.522.822.021.54.204.484.734.875.004.85

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Mean ECG Rhythms at Indicated Time Points

12-lead ECGs were obtained during the study using an ECG machine that automatically calculated the heart rhythm and measured PR, QRS, RR, QT, and QTc intervals. It was performed with the participant in a semi-supine position having rested in that position for at least 10 minutes beforehand. Three measurements were taken at pre-dose on Day 1 at least 5 minutes apart and the mean of the three measurements was calculated. The assessments were done at Day 1 (pre-dose, 0.25-1.5 hours post-initial dose and 1.5-3 hours post-initial dose), Day 4 (4-12 hours post-morning dose), Day 8 (pre-morning dose) and Day 11 (0 hour). (NCT01209078)
Timeframe: Up to Day 11

,
InterventionBeats per minute (Mean)
Day 1, mean pre-doseDay 1, 0.25-1.5 h post-doseDay 1,1.5-3 h post-doseDay 4, 4-12 h post-doseDay 8, pre-morning doseDay 11, 0 h
GSK1322322 1500 mg BID75.079.280.470.668.270.9
Linezolid 600 mg BID72.872.073.773.067.272.0

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Mean Electrocardiogram (ECG) Values at Indicated Time Points

12-lead ECGs were obtained during the study using an ECG machine that automatically calculated the heart rate and measured PR, QRS, RR, QT, and QTc intervals. It was performed with the participant in a semi-supine position having rested in that position for at least 10 minutes beforehand. Three measurements were taken at pre-dose on Day 1 at least 5 minutes apart. The mean PR interval, RR interval, QRS duration, uncorrected QT interval (UncQT) and QTcB (QT corrected by Bazett's formula) and QTcF (corrected by Friedericia's formula) was calculated from automated ECG readings. The assessments were done at Day 1 (pre-dose, 0.25-1.5 hours post-initial dose and 1.5-3 hours post-initial dose), Day 4 (4-12 hours post-morning dose), Day 8 (pre-morning dose) and Day 11 (0 hour). The mean value recorded pre-dose on Day 1 was classified as Baseline. (NCT01209078)
Timeframe: Up to Day 11

,
InterventionMillisecond (msec) (Mean)
PR interval, Day 1, mean pre-dosePR interval, Day 1, 0.25-1.5 h post-dosePR interval, Day 1,1.5-3 h post-dosePR interval, Day 4, 4-12 h post-dosePR interval, Day 8, pre morning dosePR interval, Day 11, 0 hQRS duration, Day 1, mean pre-doseQRS duration, Day 1, 0.25-1.5 h post-doseQRS duration, Day 1,1.5-3 h post-doseQRS duration, Day 4, 4-12 h post-doseQRS duration, Day 8, pre morning doseQRS duration, Day 11, 0 hUncQT interval, Day 1, mean pre-doseUncQT interval, Day 1, 0.25-1.5 h post-doseUncQT interval, Day 1,1.5-3 h post-doseUncQT interval, Day 4, 4-12 h post-doseUncQT interval, Day 8, pre morning doseUncQT interval, Day 11, 0 hQTcB interval, Day 1, mean pre-doseQTcB interval, Day 1, 0.25-1.5 h post-doseQTcB interval, Day 1,1.5-3 h post-doseQTcB interval, Day 4, 4-12 h post-doseQTcB interval, Day 8, pre morning doseQTcB interval, Day 11, 0 hQTcF interval, Day 1, mean pre-doseQTcF interval, Day 1, 0.25-1.5 h post-doseQTcF interval, Day 1,1.5-3 h post-doseQTcF interval, Day 4, 4-12 h post-doseQTcF interval, Day 8, pre morning doseQTcF interval, Day 11, 0 hRR interval, Day 1, mean pre-doseRR interval, Day 1, 0.25-1.5 h post-doseRR interval, Day 1,1.5-3 h post-doseRR interval, Day 4, 4-12 h post-doseRR interval, Day 8, pre morning doseRR interval, Day 11, 0 h
GSK1322322 1500 mg BID158.0157.0158.5165.8167.4158.694.093.995.795.795.595.2376.7370.8370.3392.6397.1385.3416.0421.1424.1422.9420.1414.5402.0403.1405.0412.3412.0404.1832.9783.8770.7868.7900.4873.4
Linezolid 600 mg BID155.0159.2157.2159.2158.1159.395.997.196.193.795.396.2378.2375.1374.0378.4390.3382.2411.6407.9412.7413.2411.0413.1399.7396.3399.2400.9403.7402.0854.6855.0825.8860.7918.6865.0

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Adverse Drug Reactions Unlisted in Japanese Package Insert.

The adverse drug reactions that have not been included in Japanese package insert. (NCT01224626)
Timeframe: Baseline to 8 weeks

Interventionparticipants (Number)
SepsisHistiocytosis haematophagicNeuropathy peripheralLiver disorderRenal disorderMulti-organ failure
Linezolid111111

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Number of Participants Categorized as Responders (Cure and Improved) to Zyvox (Linezolid) Treatment.

Clinical overall effectiveness was evaluated by investigators based on clinical symptoms, laboratory test and investigator judgement, at the end of observation period. Clinical rating (cure/improved/not cured/unable to evaluate) was carried out. Definition of cured was disappearance of clinical symptom and/or Laboratory test abnormality. Definition of improved was improvement in clinical symptoms and/or laboratory test abnormality. (NCT01224626)
Timeframe: Baseline to 8 weeks

Interventionparticipants (Number)
Linezolid16

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Number of Participants With Adverse Drug Reactions.

All observed or volunteered adverse events and the investigator's opinion of the causal relationship to the study treatment were reported as adverse events. Definition of adverse drug reaction was treatment related adverse events which were evaluated in company with the causal relationship to the investigational product. (NCT01224626)
Timeframe: Baseline to 8 weeks

Interventionparticipants (Number)
Platelet count decreasedAnaemiaWhite blood cell count decreasedSuperinfectionSepsisHistiocytosis haematophagicPancytopeniaDizziness posturalNeuropathy peripheralDiarrhoeaLiver disorderRenal disorderMulti-organ failureAspartate aminotransferase increasedHaemoglobin decreasedLiver function test abnormalBlood alkaline phosphatase increasedRed blood cell count decreased
Linezolid1033111111111111111

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Pharmacokinetic (PK) Parameter, Area Under Curve, (AUCinf, ug*h/mL), in Subjects Administered Delafloxacin, Vancomycin, and Linezolid

Blood samples for pharmacokinetic analyses were drawn from all subjects on Day 3 (± 1 day) of treatment within 2 hours before the first study drug infusion and at 1, 2, 3, 5, and 12 hours (ie, immediately before the second dose) after the start of the first study drug infusion. An analytical, validated method was used to analyze samples and determine human plasma concentrations. The primary pharmacokinetic parameter calculated was area under the plasma concentration - time curve from time 0 extrapolated to infinity (AUCinf, ug*h/mL). (NCT01283581)
Timeframe: Through Day 3 (± 1 day)

Interventionug*h/mL (Mean)
Delafloxacin23.4
Vancomycin266.8
Linezolid106.0

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Erythema Clinical Success

The number of ITT subjects who had cessation of erythema within 48-72 hours, based on digital measurements, as well as resolution/absence of fever. Cessation was defined as a percentage change from baseline in total area of erythema/induration that is less than or equal to 0%. (NCT01283581)
Timeframe: 48 - 72 hours

InterventionParticipants (Number)
Delafloxacin IV61
Linezolid56
Vancomycin69

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The Levels of Inflammation Were Examined by Measuring a Surrogate, C-Reactive Protein (CRP)

CRP Levels (g/m3) were analyzed from blood samples collected from subjects at Baseline and various time points throughout the study. Change in baseline values were analyzed using an analysis of covariance (ANCOVA) model with treatment, infection category, and prior antimicrobial therapy as fixed effects and the baseline measure as the covariate. (NCT01283581)
Timeframe: Baseline, Days 1, 5, Follow-up (FU), and late Follow-up (LFU)

,,
Interventiong/m3 (Mean)
BaselineDay 1Day 5FULFU
Delafloxacin46.644.219.69.410.8
Linezolid49.349.826.512.112.6
Vancomycin55.249.619.511.99.3

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Investigator's Assessment of Clinical Response in the ITT (Intent-to-treat) Population at Follow-up

The primary efficacy endpoint was the success rate, defined as (cure)/(cure + failure), and expressed as a percentage. Cure was defined as the complete resolution of all baseline signs and symptoms of ABSSSI and follow-up and late follow-up. If erythema was the only sign of infection present at follow-up and it was then absent at late follow-up, the case was classified as a Cure. (NCT01283581)
Timeframe: Follow-up (Day 14 ± 1)

InterventionParticipants (Number)
Delafloxacin IV57
Linezolid50
Vancomycin53

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Clinical Response in Subjects With Infections Caused by MRSA - Microbiological ITT (MITT) Population

The success rate, defined as (cure)/(cure + failure), and expressed as a percentage. Cure was defined as the complete resolution of all baseline signs and symptoms of ABSSSI and follow-up and late follow-up. If erythema was the only sign of infection present at follow-up and it was then absent at late follow-up, the case was classified as a Cure. (NCT01283581)
Timeframe: Follow-up (Day 14 ± 1)

InterventionParticipants (Count of Participants)
Delafloxacin19
Vancomycin21
Linezolid21

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Clinical Status

Compare the clinical efficacy at the day 28 follow-up visit of dalbavancin to the comparator regimen based on lesion size, local signs, temperature and receipt of non-study antibiotics (NCT01339091)
Timeframe: Follow-Up Visit (day 28)

,
Interventionparticipants (Number)
Clinical SuccessClinical Failure
Dalbavancin21214
Vancomycin +/- Oral Linezolid2209

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Clinical Status

Compare the clinical efficacy at end of treatment visit of dalbavancin to the comparator regimen based on lesion size, local signs, temperature and receipt of non-study antibiotics (NCT01339091)
Timeframe: End of Treatment Visit (Day 14-15)

,
Interventionparticipants (Number)
Clinical SuccessClinical Failure
Dalbavancin21432
Vancomycin +/- Oral Linezolid22221

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>= 20% Reduction in Lesion Area

Clinical response at 48-72 hours post study drug initiation, based on measurements of acute bacterial skin and skin structure infections (ABSSSI) lesion size (NCT01339091)
Timeframe: 48-72 hours after the initiation of study therapy

,
Interventionparticipants (Number)
Clinical ResponderClinical Non-Responder
Dalbavancin25929
Vancomycin +/- Oral Linezolid25926

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Early Clinical Efficacy

Clinical response at 48-72 hours post study drug initiation, based on measurements of acute bacterial skin and skin structure infections (ABSSSI) lesion size and temperature (NCT01339091)
Timeframe: 48-72 hours after the initiation of study therapy

,
Interventionparticipants (Number)
Clinical ResponderClinical Non-Responder
Dalbavancin24048
Vancomycin +/- Oral Linezolid23352

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Investigator's Assessment of Clinical Response at the 48-72 Hour Visit

Clinical improvement defined as improvement in overall clinical status. (NCT01421511)
Timeframe: 48-72 Hours

Interventionparticipants (Number)
Tedizolid Phosphate304
Linezolid302

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Change From Baseline in Patient-reported Pain, by Study Visit

0=no pain, 10=worst pain Only 1 visit per participant for Day 4-6, only 1 visit for Day 7-9, and only 1 visit for Day 10-13. (NCT01421511)
Timeframe: Multiple

,
Interventionunits on a scale (Mean)
Day 2Day 4-6Day 7-9Day 10-13
Linezolid-2.1-3.3-4.9-5.6
Tedizolid Phosphate-1.7-3.1-4.9-5.4

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The Early Clinical Response Rate

Responder: No increase in lesion surface area from baseline. (NCT01421511)
Timeframe: 48-72 hours

Interventionparticipants (Number)
Tedizolid Phosphate283
Linezolid276

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Investigator's Assessment of Clinical Success of the Post Therapy Evaluation Visit in Clinically Evaluable-Post Treatment Evaluation Analysis Set.

Clinical success defined as resolution/near resolution of disease specific signs and symptoms, absence/near resolution of baseline systemic signs of infection, no new signs, symptoms or complications attributable to the ABSSSI and no further antibiotic therapy required for treatment of primary ABSSSI lesion. (NCT01421511)
Timeframe: Post-Treatment Evaluation (7-14 days after the End of Therapy)

Interventionparticipants (Number)
Tedizolid Phosphate268
Linezolid269

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Investigator's Assessment of Clinical Success at the Post Treatment Evaluation Visit

Clinical success defined as resolution/near resolution of disease specific signs and symptoms, absence/near resolution of baseline systemic signs of infection, and no further antibiotic therapy required for treatment of primary ABSSSI lesion. (NCT01421511)
Timeframe: Post-Treatment Evaluation (7-14 days after the End of Therapy)

Interventionparticipants (Number)
Tedizolid Phosphate292
Linezolid293

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Investigator's Assessment of Clinical Response at the Day-7 Visit

Clinical improvement defined as improvement in overall clinical status. (NCT01421511)
Timeframe: Day 7

Interventionparticipants (Number)
Tedizolid Phosphate309
Linezolid308

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Clinical Response at the End of Therapy Visit

Responder: No increase in lesion surface area from baseline. (NCT01421511)
Timeframe: Day 11

Interventionparticipants (Number)
Tedizolid Phosphate289
Linezolid294

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Clinical Response at the End of Therapy Visit in the Clinically Evaluable at End of Therapy Analysis Set

Responder: No increase in lesion surface area from baseline. (NCT01421511)
Timeframe: End of Therapy Day 11

Interventionparticipants (Number)
Tedizolid Phosphate272
Linezolid280

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Early Clinical Efficacy

Clinical response at 48-72 hours post study drug initiation, based on measurements of acute bacterial skin and skin structure infections (ABSSSI) lesion size and temperature (NCT01431339)
Timeframe: After 48-72 hours of therapy

,
Interventionparticipants (Number)
Clinical ResponderClinical Non-Responder
Dalbavancin28586
Vancomycin With Possible Switch to Oral Linezolid28880

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Clinical Status

Compare the clinical efficacy at the short term follow-up visit of dalbavancin to the comparator regimen based on lesion size, local signs temperature and receipt of other therapy (NCT01431339)
Timeframe: Follow-Up Visit (day 28)

,
Interventionparticipants (Number)
Clinical SuccessClinical Failure
Dalbavancin28311
Vancomycin With Possible Switch to Oral Linezolid25715

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Clinical Status

Compare the clinical efficacy at end of treatment visit of dalbavancin to the comparator regimen based on lesion size, local signs, temperature and receipt of other therapy (NCT01431339)
Timeframe: End of Treatment Visit (Day 14-15)

,
Interventionparticipants (Number)
Clinical SucccessClinical Failure
Dalbavancin30321
Vancomycin With Possible Switch to Oral Linezolid28022

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>= 20% Reduction in Lesion Area

Clinical response at 48-72 hours post study drug initiation, based on measurements of acute bacterial skin and skin structure infections (ABSSSI) lesion size (NCT01431339)
Timeframe: 48-72 hours after the initiation of study therapy

,
Interventionparticipants (Number)
Clinical ResponderClinical Non-Responder
Dalbavancin32546
Vancomycin With Possible Switch to Oral Linezolid31652

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Duration of Hospital Stay

Duration of hospital stay was assessed as number of days from VAP diagnosis to discharge from the hospital. (NCT01561469)
Timeframe: Up to 28 days after diagnosis of VAP

Interventiondays (Median)
Linezolid18
Vancomycin16

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Duration of Intensive Care Unit (ICU) Stay

Duration of ICU stay was assessed as number of days from VAP diagnosis to discharge from the ICU. (NCT01561469)
Timeframe: Up to 28 days after diagnosis of VAP

Interventiondays (Median)
Linezolid11
Vancomycin13

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Duration of Mechanical Ventilation

Duration of mechanical ventilation was assessed as number of days from VAP diagnosis to extubation or to discharge if not extubated. (NCT01561469)
Timeframe: Up to 28 days after diagnosis of VAP

Interventiondays (Median)
Linezolid11
Vancomycin13

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Percentage of Participants With Clinical Success

Clinical success was assessed as number of participants cured or improved. Cure = complete resolution of signs and symptoms of pneumonia; Improvement = partial resolution of signs and symptoms of pneumonia. (NCT01561469)
Timeframe: 14 days after diagnosis with VAP or hospital discharge, whichever occurred first

Interventionpercentage of participants (Number)
Linezolid85
Vancomycin69

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Number of Participants With Microbiological Outcome

Microbiological outcome was defined as superinfections (infections diagnosed within 72 hours of the diagnosis of HAP and until day 28) and colonization (positive cultures with a multi-drug resistant organism). (NCT01561469)
Timeframe: 28 days after diagnosis of VAP

,
Interventionparticipants (Number)
SuperinfectionsColonization
Linezolid4234
Vancomycin3732

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Duration of Antimicrobial Treatment

(NCT01561469)
Timeframe: Up to 28 days after diagnosis of VAP

Interventiondays (Mean)
Linezolid11
Vancomycin11

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Number of Participants With Clinical Response

Clinical response assessed by Investigator at EOT visit as Cure: complete resolution of signs or symptoms of infection and no need to start another antibiotic. Improvement: incomplete resolution of signs or symptoms of infection but no need to start another antibiotic. Failure: death, or need to start another antibiotic. For participants previously assessed as failures, the outcome was failure at subsequent time points. (NCT01564758)
Timeframe: EOT (Day 10 up to 28)

Interventionparticipants (Number)
CureImprovementFailure
Linezolid573111

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Number of Participants With Adverse Events (AEs)

Any untoward medical occurrence in a participant who received study treatment was considered an AE without regard to possibility of causal relationship. (NCT01564758)
Timeframe: Baseline up to End of Treatment (EOT) (Day 10 up to 28)

Interventionparticipants (Number)
Linezolid15

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Number of Participants With Suppression and Emergence of Resistance

The emergence of resistance is defined as a change of meropenem MIC or aminoglycoside MIC by two tube dilutions (fourfold) from baseline when assessed at the second BAL procedure on day 5/early extubation. Patients are evaluable for this endpoint IF they had baseline BAL and Day 5/early extubation and if they had positive cultures on baseline and Day/EE. (NCT01570192)
Timeframe: up to 28 days after enrollment

Interventionparticipants (Number)
suppression of emergence of resistanceemergence of resistance
I.V. Meropenem51

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Occurrence of Repeat Negative Cultures

Percentage of patients with successful responses by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: Day 5/Early Extubation

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside3
ME Group - Meropenem Only6
m-MITT Group - Meropenem Plus Aminoglycoside3
m-MITT Group - Meropenem Only7

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Clinical Response

Percentage of patients with successful responses by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: End of treatment - up to 28 days after enrollment

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside2
MEGroup - Meropenem Only8
m-MITT Group - Meropenem Plus Aminoglycoside2
m-MITT Group - Meropenem Only8

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Suppression of the Emergence of Resistance in Other Gram-negative Pathogens

Percentage of patients with successful responses by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: Day 5/Early Extubation

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside1
ME Group - Meropenem Only1
m-MITT Group - Meropenem Plus Aminoglycoside1
m-MITT Group - Meropenem Only2

[back to top]

Pretreatment Pathogen Response

Percentage of patients with successful responses by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: End of treatment - up to 28 days after enrollment

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside3
ME Group - Meropenem Only9
m-MITT Group - Meropenem Plus Aminoglycoside3
m-MITT Group - Meropenem Only11

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Overall Microbiologic Response

Percentage of patients with successful responses by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: End of treatment - up to 28 days after enrollment

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside2
ME Group - Meropenem Only6
m-MITT Group - Meropenem Plus Aminoglycoside2
m-MITT Group - Meropenem Only7

[back to top]

Clinical Response in Subjects Who Received Prior Antibiotics

Percentage of patients with successful responses by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: End of treatment - up to 28 days after enrollment

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside1
ME Group - Meropenem Only2
m-MITT Group - Meropenem Plus Aminoglycoside1
m-MITT Group - Meropenem Only2

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Mortality

Percentage of patients who died by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: 14 days

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside1
ME Group - Meropenem Only0
m-MITT Group - Meropenem Plus Aminoglycoside2
m-MITT Group - Meropenem Only2

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Mortality

Percentage of patients who died by efficacy endpoint, treatment group and population (n/N) (NCT01570192)
Timeframe: 28 days

InterventionParticipants (Count of Participants)
ME Group - Meropenem Plus Aminoglycoside2
ME Group - Meropenem Only1
m-MITT Group - Meropenem Plus Aminoglycoside3
m-MITT Group - Meropenem Only3

[back to top]

Number of Participants With Presence of Staphylococcus Aureus After Treatment With Linezolid Versus Clindamycin

Asymptomatic carriage of Staphylococcus aureus at the 40-day visit will be compared in the patients assigned to receive linezolid to the patients assigned to receive clindamycin. (NCT01619410)
Timeframe: 40 days after completion of treatment

InterventionParticipants (Count of Participants)
Linezolid3
Clindamycin2

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Proportion of Individuals With Acute Kidney Injury Network Modified Definition of Nephrotoxicity

"An abrupt (within 48 hour) reduction in kidney function with one or more of the following 1) Increase in SCr ≥ 0.3 mg/dL 2) Increase SCr ≥ 50% or 3) Decreased urine output (< 0.5 ml/kg/hr x 6 hrs) while on the study drug.~This measure will be reported as proportion of patients with acute kidney injury within each group in relation to the number of patients in each group." (NCT01734694)
Timeframe: Day 1 and daily serum creatinine assessment up to date of discharge, and a median of 7 days.

InterventionParticipants (Count of Participants)
Vancomycin16
Comparator16

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Proportion of Individuals With Nephrotoxicity

"Increase in SCr of 0.5 mg/dL or 50% above baseline for at least two consecutive days while on the study drug and through discharge from hospital.~This measure will be reported as proportion of patients with nephrotoxicity within each group in relation to the number of patients in each group." (NCT01734694)
Timeframe: Day 1 and daily serum creatinine assessment up to date of discharge from hospital, and a median of 7 days.

InterventionParticipants (Count of Participants)
Vancomycin5
Comparator3

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Clinical Success

Clinical success, a composite outcome defined as discharge from the hospital or ICU by day 14 after treatment initiation, in the absence of death, therapy change, or intubation by day 14. Percentage of participants with clinical success was reported. (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventionpercentage of participants (Number)
Linezolid50.9
Vancomycin46

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Time to 30-day Methicillin-Resistant Staphylococcus Aureus (MRSA) Re-infection

Time to MRSA re-infection was defined as readmission with MRSA infection to any veterans affairs hospital facility within 30 days after hospital discharge. (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Median)
Linezolid17
Vancomycin11

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Time to 30-day Mortality

Time to death (all-cause mortality) occurring within 30 days of treatment initiation was reported. Mortality was assessed from admission vital status databases. (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Median)
Linezolid15
Vancomycin14

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Time to Discharge From the Hospital

Time to discharge from hospital was calculated from initiation of therapy (index date) to hospital discharge (event date). (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Mean)
Linezolid19.7
Vancomycin20.3

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Time to Intubation

Time to intubation was calculated from the initiation of therapy (index date) to intubation (event date). (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Median)
Linezolid5
Vancomycin3

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Time to Therapy Change

Time to therapy change was calculated from initiation of therapy (index date) to change in therapy (event date). Therapy change was defined as the discontinuation of linezolid or vancomycin and initiation of a different agent with activity against MRSA (clindamycin, daptomycin, doxycycline, linezolid, minocycline, tigecycline, trimethoprim/sulfamethoxazole, vancomycin). As such, therapy change included switching from linezolid to vancomycin, switching from vancomycin to linezolid, or switching from either linezolid or vancomycin to another anti-MRSA antibiotic. (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Median)
Linezolid4
Vancomycin4

[back to top]

Time to Transfer Out From the Intensive Care Unit (ICU)

Time to discharge from the ICU was calculated from the initiation of therapy (index date) to the time the participant was transferred out from ICU (event date). Transfer out of an ICU was assessed among those participants who had initiated linezolid or vancomycin therapy in the ICU. (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Median)
Linezolid2
Vancomycin4

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Time to 30-day Re-admission

Time to readmission to any veterans affairs hospital facility within 30 days after hospital discharge was reported. (NCT01819935)
Timeframe: Baseline (1 January 2001) up to 3559 Days (30 September 2010)

Interventiondays (Median)
Linezolid10
Vancomycin11

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Change of the Lesion Size From the Screening Visit by Visit (Only Skin and Soft Tissue Infection [SSTI])

Lesion size was measured by the masked investigators of erythema, edema, or induration whichever is largest. (NCT01967225)
Timeframe: Multiple time points up to 7-14 days after the end of treatment

,
Interventioncm^2 (Mean)
Day 3/4Day 5 to 13End of treatmentTest of cure (n=28, 9)
Linezoid - SSTI-173.93-317.66-280.69-314.18
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI-62.05-134.31-174.96-212.63

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Clinical Response at End of Treatment Visit (EOT)

Clinical response was evaluated by the masked investigator as effective, ineffective and indeterminate on the basis of the clinical symptoms/findings, vital sign and laboratory data from screening period to each evaluation point. Measurements for the assessment of clinical response included body temperature, pulse/heart rate, respiration rate, and white blood cell or band cell count. (NCT01967225)
Timeframe: 7-14 days for skin and soft tissue infections (SSTI) or 7-21 days for bacteremia from the study drug administration

,,
InterventionPercentage of participants (Number)
EffectiveIneffectiveIndeterminate
Linezoid - Bacteremia50.00.050.0
Linezoid - SSTI90.010.00.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI93.16.90.0

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Clinical Response at Test of Cure (TOC)

Clinical response was evaluated by the masked investigator as clinical cure, clinical failure and indeterminate on the basis of the clinical symptoms/findings, vital sign and laboratory data from screening period to each evaluation point. Measurements for the assessment of clinical response included body temperature, pulse/heart rate, respiration rate, and white blood cell or band cell count. (NCT01967225)
Timeframe: 7-14 days after the end of treatment (EOT) for skin and soft tissue infections (SSTI) and 4-6 weeks after EOT for bacteremia

,,
InterventionPercentage of participants (Number)
Clinical cureClinical failureIndeterminate
Linezoid - Bacteremia0.00.0100.0
Linezoid - SSTI80.010.010.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI86.26.96.9

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Microbiological Response at End of Treatment (EOT)

Microbiological response was assessed in accordance with the Guidance for the method of microbiological assessment by Japanese Chemotherapy Society. (NCT01967225)
Timeframe: 7-14 days for skin and soft tissue infections (SSTI) or 7-21 days for bacteremia from the study drug administration

,,
InterventionPercentage of participants (Number)
EradicationPersistenceElimination (indeterminate)
Linezoid - Bacteremia100.00.00.0
Linezoid - SSTI100.00.00.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI93.16.90.0

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Reduction Ratio of the Lesion Size From the Screening Visit to Day 3 to Day 4 Visit (Only Skin and Soft Tissue Infection [SSTI])

Lesion size was measured by the masked investigators of erythema, edema, or induration whichever is largest. Reduction ratio (%) = 100 * (the post baseline value - baseline value) / baseline value. Negative values represent reduction of lesion size compared to baseline. (NCT01967225)
Timeframe: Baseline and Day 3/4, Day 5/13, EOT, TOC

,
InterventionPercentage (Mean)
Day3/4Day 5 to 13End of TreatmentTest of Cure
Linezoid - SSTI-61.46-94.61-90.09-99.09
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI-32.32-53.30-67.69-81.82

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Microbiological Response at Test of Cure (TOC)

Microbiological response was assessed in accordance with the Guidance for the method of microbiological assessment by Japanese Chemotherapy Society. (NCT01967225)
Timeframe: 7-14 days after the end of treatment (EOT) for skin and soft tissue infections (SSTI) and 4-6 weeks after EOT for bacteremia

,,
InterventionPercentage of participants (Number)
EradicationPersistenceElimination(indeterminate)Missing
Linezoid - Bacteremia100.00.00.00.0
Linezoid - SSTI90.00.00.010.0
Tedizolid Phosphate (Sivextro, BAY1192631) - SSTI93.13.40.03.4

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Number of Methicillin-Resistant Staphylococcus Aureus (MRSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population

The number of MRSA-infected participants with all-cause mortality within 28 days after randomization was determined in the mITT population. Participants who had confirmed MRSA culture results from respiratory tract or pleural fluid specimens obtained within 72 hours of study Day 1 were included. Any participants who were lost to follow-up and not known to be alive or deceased by Day 28 were imputed as deceased. (NCT02019420)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Tedizolid14
Linezolid20

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Number of Methicillin-Susceptible Staphylococcus Aureus (MSSA)-Infected Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population

The number of MSSA-infected participants with all-cause mortality within 28 days after randomization was determined in the mITT population. Participants who had confirmed MSSA culture results from respiratory tract or pleural fluid specimens obtained within 36 hours of study Day 1 were included. Any participants who were lost to follow-up and not known to be alive or deceased by Day 28 were imputed as deceased. (NCT02019420)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Tedizolid31
Linezolid32

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Number of Participants Discontinuing Study Therapy Due to an Adverse Event (AE)

An AE is any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug related. Safety analysis was based on actual treatment received and not randomization. (NCT02019420)
Timeframe: Up to 14 days

InterventionParticipants (Count of Participants)
Tedizolid4
Linezolid3

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Number of Participants With ≥1 Adverse Events (AEs)

An AE is any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug related. Safety analysis is based on actual treatment received instead of randomization. (NCT02019420)
Timeframe: Up to 32 days

InterventionParticipants (Count of Participants)
Tedizolid327
Linezolid325

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Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiologically-Evaluable 1 (ME-1) Population

The number of patients in the ME-1 population with a favorable response at EOT was determined. Favorable response included eradication (absence of the baseline pathogen) and presumed eradication (no source specimen to culture in a participant assessed as a clinical cure by the investigator). (NCT02019420)
Timeframe: 1-3 days after completing study therapy (Days 8-10 or Days 15-17)

InterventionParticipants (Count of Participants)
Tedizolid123
Linezolid166

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Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiological Intent-to-Treat (mITT) Population

The number of patients in the mITT population with a favorable response at TOC was determined. Favorable response included eradication (absence of the baseline pathogen) and presumed eradication (no source specimen to culture in a participant assessed as a clinical cure by the investigator). (NCT02019420)
Timeframe: 7-14 days after end of therapy - TOC

InterventionParticipants (Count of Participants)
Tedizolid117
Linezolid158

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Number of Participants With a Favorable Response at Test-of-Cure (TOC) Visit in the Microbiologically-Evaluable 2 (ME-2) Population

The number of patients in the ME-2 population with a favorable response at TOC was determined. Favorable response included eradication (absence of the baseline pathogen) and presumed eradication (no source specimen to culture in a participant assessed as a clinical cure by the investigator). (NCT02019420)
Timeframe: 7-14 days after end of therapy - TOC

InterventionParticipants (Count of Participants)
Tedizolid65
Linezolid74

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Number of Participants With All-Cause Mortality in the Intent-to-Treat (ITT) Population

The numbers of participants with all-cause mortality within 28 days after randomization was determined in the ITT population. Any participants who were lost to follow-up and not known to be alive or deceased by Day 28 were imputed as deceased. (NCT02019420)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Tedizolid103
Linezolid95

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Number of Participants With All-Cause Mortality in the Microbiological Intent-to-Treat (mITT) Population

The numbers of participants with all-cause mortality within 28 days after randomization was determined in the mITT population. Any participants who were lost to follow-up and not known to be alive or deceased by Day 28 were imputed as deceased. (NCT02019420)
Timeframe: Up to 28 days

InterventionParticipants (Count of Participants)
Tedizolid46
Linezolid49

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Clinical Response at Test of Cure (TOC) Visit in the Clinically-Evaluable (CE) Population

The clinical response in the CE population at the TOC visit (derived from the Investigator's assessment at the EOT and TOC visits) was determined by the investigator to be either: clinical success, clinical failure, or indeterminate. Clinical success was declared when most or all clinical signs were completely resolved, with no new signs of infection, no additional antibiotic therapy was required, and the participant was alive. Indeterminate was declared when the investigator could not determine success or failure. Clinical failure was declared with progression, relapse, or recurrence of new symptoms of infection, or a persistence or insufficient improvement in signs and symptoms of VNP. (NCT02019420)
Timeframe: 7-14 days after end of therapy - TOC

,
InterventionParticipants (Count of Participants)
Clinical SuccessClinical FailureIndeterminate
Linezolid146970
Tedizolid1431240

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Clinical Response at Test of Cure (TOC) Visit in the Intent-to-Treat (ITT) Population

The clinical response in the ITT population at the TOC visit (derived from the Investigator's assessment at the EOT and TOC visits) was determined by the investigator to be either: clinical success, clinical failure, or indeterminate. Clinical success was declared when most or all clinical signs were completely resolved, with no new signs of infection, no additional antibiotic therapy was required, and the participant was alive. Indeterminate was declared when the investigator could not determine success or failure. Clinical failure was declared with progression, relapse, or recurrence of new symptoms of infection, or a persistence or insufficient improvement in signs and symptoms of VNP. (NCT02019420)
Timeframe: 7-14 days after end of therapy - TOC

,
InterventionParticipants (Count of Participants)
Clinical SuccessClinical FailureIndeterminate
Linezolid23011020
Tedizolid20614416

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Number of Participants With a Favorable Response at End-of-Therapy (EOT) Visit in the Microbiological Intent-to-Treat (mITT) Population

The number of patients in the mITT population with a favorable response at EOT was determined. Favorable response included eradication (absence of the baseline pathogen) and presumed eradication (no source specimen to culture in a participant assessed as a clinical cure by the investigator). (NCT02019420)
Timeframe: 1-3 days after completing study therapy (Days 8-10 or Days 15-17)

InterventionParticipants (Count of Participants)
Tedizolid123
Linezolid166

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Value of the Visual Analog Scale (VAS) Pain Scores at Each Time Point

The patient-reported level of pain were assessed by the visual analog scale (VAS) pain score. VAS pain score ranged from 0 mm (no pain) to 100 mm (worst pain ever). It used a 100 mm VAS to instruct the patient to indicate the point along the line that represents the pain they are feeling. Once the patient indicates how much pain they are feeling, measure the distance from no pain and enter the value. (NCT02066402)
Timeframe: Up to EOT visit (Day 11)

,
InterventionUnits on a scale (Mean)
Day 248-72 hoursDay 7EOT
Linezolid40.130.717.810.3
Tedizolid Phosphate (Sivextro, BAY119-2631)40.930.218.811.6

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Percentage of Participants With Early Clinical Response at 48-72 Hours After the First Infusion of Study Drug in the ITT Analysis Set.

Early clinical response is defined as responder if there is >=20% reduction in the area of erythema, edema, and/or induration (length × width) of the primary acute bacterial skin and skin structure infections (ABSSSI) lesion, compared with baseline at the 48-72 Hour visit. (NCT02066402)
Timeframe: Baseline and 48-72 hours visit

InterventionPercentage of participants (Number)
Tedizolid Phosphate (Sivextro, BAY119-2631)75.3
Linezolid79.9

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Value of the Faces Rating Scale (FRS) Pain Scores at Each Time Point

The patient-reported level of pain were assessed by the faces rating scale (FRS) pain score. Ask the patient to rate their pain from 0 to 10 with 0 being no pain at all and 10 being the worst pain then enter the numerical value. (NCT02066402)
Timeframe: Up to EOT visit (Day 11)

,
InterventionUnits on a scale (Mean)
Day 248-72 hoursDay 7EOT
Linezolid4.23.22.01.3
Tedizolid Phosphate (Sivextro, BAY119-2631)4.13.22.11.3

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Change From Baseline in the Faces Rating Scale (FRS) Pain Scores at Each Time Point

The patient-reported level of pain were assessed by the faces rating scale (FRS) pain score. The patient-reported level of pain were assessed by the faces rating scale (FRS) pain score. Ask the patient to rate their pain from 0 to 10 with 0 being no pain at all and 10 being the worst pain then enter the numerical value. (NCT02066402)
Timeframe: Up to EOT visit (Day 11)

,
InterventionUnits on a scale (Mean)
Day 248-72 hoursDay 7EOT
Linezolid-1.5-2.4-3.6-4.4
Tedizolid Phosphate (Sivextro, BAY119-2631)-1.5-2.4-3.5-4.2

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Change From Baseline in the Visual Analog Scale (VAS) Pain Scores at Each Time Point

The patient-reported level of pain were assessed by the visual analog scale (VAS) pain score. VAS pain score ranged from 0 mm (no pain) to 100 mm (worst pain ever). It used a 100 mm VAS to instruct the patient to indicate the point along the line that represents the pain they are feeling. Once the patient indicates how much pain they are feeling, measure the distance from no pain and enter the value. (NCT02066402)
Timeframe: Up to EOT visit (Day 11)

,
InterventionUnits on a scale (Mean)
Day 248-72 hoursDay 7EOT
Linezolid-13.8-23.2-36.1-43.6
Tedizolid Phosphate (Sivextro, BAY119-2631)-12.5-23.2-34.7-41.6

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Investigator's Assessment of Clinical Response at 48-72 Hours

The Investigator made an assessment of clinical response at the 48-72 Hour Visit based on following definition: Improving (Improvement in overall clinical status of ABSSSI compatible with continuation of study drug therapy); Stable (Signs and symptoms stable, no apparent change in overall clinical status but compatible with continuation of study drug therapy); Other. (NCT02066402)
Timeframe: Baseline and at 48-72 hours

,
InterventionPercentage of participants (Number)
ImprovingStableOtherMissing
Linezolid90.33.00.06.7
Tedizolid Phosphate (Sivextro, BAY119-2631)86.74.70.78.0

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Investigator's Assessment of Clinical Response at Day 7 Visit

The Investigator made an assessment of clinical response at Day 7 Visit based on following definition: Improving (Improvement in overall clinical status of ABSSSI compatible with continuation of study drug therapy); Other. (NCT02066402)
Timeframe: Baseline and Day 7 visit

,
InterventionPercentage of participants (Number)
ImprovingOtherMissing
Linezolid87.60.312.1
Tedizolid Phosphate (Sivextro, BAY119-2631)88.30.311.3

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Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the Clinically Evaluable at Post Therapy Evaluation (CE-PTE) Analysis Set

The Investigator made an assessment of clinical response at the PTE Visit (7-14 days after the EOT Visit +2 days). Participants assessed as a clinical failure at the EOT Visit are considered a clinical failure at the PTE Visit. Percentage of participants with clinical success, clinical failure or indeterminate were reported. (NCT02066402)
Timeframe: Baseline and post-therapy evaluation visit (7-14 days after Day 11)

,
InterventionPercentage of participants (Number)
Clinical successClinical failure or Indeterminate
Linezolid93.56.5
Tedizolid Phosphate (Sivextro, BAY119-2631)90.49.6

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Overall Investigator's Assessment of Clinical Success at Post Therapy Evaluation (PTE) Visit (7-14 Days After EOT Visit) in the ITT Analysis Set

The Investigator made an assessment of clinical response at the PTE Visit (7-14 days after the EOT Visit +2 days). Participants assessed as a clinical failure at the EOT Visit are considered a clinical failure at the PTE Visit. Percentage of participants with clinical success, clinical failure or indeterminate were reported. (NCT02066402)
Timeframe: Baseline and post-therapy evaluation visit (7-14 days after Day 11)

,
InterventionPercentage of participants (Number)
Clinical successClinical failure or Indeterminate
Linezolid81.918.1
Tedizolid Phosphate (Sivextro, BAY119-2631)79.720.3

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Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the Clinically Evaluable at EOT (CE-EOT) Analysis Set

Clinical response will be defined as percentage of participants with clinical success, clinical failure or indeterminate. (NCT02066402)
Timeframe: Baseline and EOT visit (Day 11)

,
InterventionPercentage of participants (Number)
Clinical successClinical failure or Indeterminate
Linezolid91.88.2
Tedizolid Phosphate (Sivextro, BAY119-2631)89.710.3

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Programmatically Defined Clinical Response at End of Therapy (EOT) Visit in the ITT Analysis Set

Clinical Failure: Presence of fever; No lesion size decrease from baseline; Clinician assessment of tenderness worse than mild; Persistent same or great intensity purulent drainage of wound infection; Confounding use of systemic concomitant antibiotic; TEAE lead to study drug discontinuation; Require additional antibiotic treatment for primary lesion; Unplanned major surgical intervention. Clinical Success: Afebrile or fever due to other cause; Lesion size decrease from baseline; Clinician assessment of mild/absent tenderness; None/lesser intensity purulent drainage of wound infection; None confounding use of systemic concomitant antibiotic; None TEAE leading to study drug discontinuation; No additional antibiotic therapy for primary lesion; No unplanned major surgical intervention; No osteomyelitis after baseline; For wound/abscess: no incision/drainage of the ABSSSI site after Day1 unless planned. For cellulitis/ersipelas: no incision/drainage of the ABSSSI site after 48-72 H Visit. (NCT02066402)
Timeframe: Baseline and EOT visit (Day 11)

,
InterventionPercentage of participants (Number)
Clinical successClinical failure or Indeterminate
Linezolid84.215.8
Tedizolid Phosphate (Sivextro, BAY119-2631)82.018.0

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Number of Participants With Adverse Events on Tedizolid Phosphate and Comparator Drugs

An adverse event (AE) refers to a treatment-emergent adverse event (TE-AE). A TE-AE is any AE that newly appeared, increased in frequency, or worsened in severity following initiation of study drug. (NCT02276482)
Timeframe: Up to 40 days (including 30-day follow-up)

InterventionParticipants (Count of Participants)
Tedizolid Phosphate13
Antibiotic Comparator Drug3

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Change From Baseline in Lesion Size

Lesion size is the area in cm^2 of erythema, edema or induration. A negative number corresponds to a decrease in lesion size. (NCT02276482)
Timeframe: Baseline and TOC visit (18 to 25 days after infusion)

,
Interventioncm^2 (Mean)
BaselineChange at Day 25
Antibiotic Comparator Drug83.22-82.51
Tedizolid Phosphate135.44-134.27

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Peak Plasma Concentration (Cmax) of Tedizolid

The Cmax of tedizolid in plasma after the last dose was estimated based on population pharmacokinetic analysis of observed pharmacokinetic data. Blood samples were collected for pharmacokinetic analysis at specific time points. (NCT02276482)
Timeframe: Day 1 at 5-80 minutes (min) and 4-12 hrs post-infusion or 2 samples collected between 4-12 hrs after oral dose, at least 60 min apart; at 48-72 hrs: within 60 min prior to administration and 4-12 hrs after administration; and anytime between Day 7 and 9

Interventionµg/mL (Geometric Mean)
Tedizolid Phosphate3.13

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Number of Participants With Investigator's Assessment Indicating Clinical Success at TOC Visit (Clinically Evaluable-Test of Cure [CE-TOC] Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2)absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: TOC Visit: 18-25 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate87
Antibiotic Comparator Drug26

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Number of Participants With Investigator's Assessment Indicating Clinical Success at Test of Cure (TOC) Visit (Intent to Treat Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2)absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: TOC Visit: 18-25 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate88
Antibiotic Comparator Drug27

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Area Under the Plasma Concentration Versus Time Curve Time 0 to 24 Hours (AUC0-24h) of Tedizolid

AUC0-24h is a measure of the total tedizolid exposure in the plasma from the dose to 24 hours after last dose. AUC0-24h was estimated based on population pharmacokinetic analysis of observed pharmacokinetic data. Blood samples were collected for pharmacokinetic analysis at specific time points. (NCT02276482)
Timeframe: Day 1 at 5-80 min and 4-12 hrs post-infusion or 2 samples collected between 4-12 hrs after oral dose, at least 60 min apart; at 48-72 hrs: within 60 min prior to administration and 4-12 hrs after administration; and anytime between Day 7 and 9

Interventionµg*h/mL (Geometric Mean)
Tedizolid Phosphate28.6

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Number of Participants With Investigator's Assessment Indicating Clinical Success at End of Therapy (EOT) Visit (Intent to Treat Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2)absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: EOT Visit: up to 13 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate88
Antibiotic Comparator Drug28

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Number of Participants With Investigator's Assessment Indicating Clinical Success at EOT Visit (Clinically Evaluable-End of Therapy [CE-EOT] Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2) absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: EOT Visit: up to 13 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate87
Antibiotic Comparator Drug27

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Number of Participants With Early Clinical Responses Measured by Lesion Reduction

Early clinical response is defined as ≥20% reduction from baseline lesion area (defined as length multiplied by the width of the erythema, edema, and/or induration [EEI]) at the 48-72 hour (hr) visit. (NCT02276482)
Timeframe: 48-72 hr after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate84
Antibiotic Comparator Drug28

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Number of Participants With Early Clinical Response

Early clinical response is defined as clinical success, which is categorized as survival with at least a 20% reduction of acute bacterial skin and skin structure infection (ABSSSI) primary lesion size compared to Screening measurements, without receiving any rescue antibacterial therapy. An indeterminate classification is used for a response that could not be adequately inferred because the participant was not assessed because they withdrew consent, were lost to follow-up, or other specified reason. (NCT02378480)
Timeframe: Screening; 48 to 72 hours after the first dose of test article

,
InterventionParticipants (Count of Participants)
Clinical successClinical failureIndeterminate
Linezolid2661926
Omadacycline2682325

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Number of Participants With the Indicated Investigator Assessment of Clinical Response in the Clinically Evaluable-Post Therapy Evaluation (CE-PTE) Population

At the PTE Visit the investigator indicated one of the following outcomes relating to the primary infection under study: Clinical Success: participant was alive; the infection was sufficiently resolved such that further antibacterial therapy was not needed. These participants may have had some residual changes related to infection requiring ancillary treatment. Clinical Failure was defined as meeting any of the following criteria: infection required additional treatment with alternative antibacterial therapy; participant received antibacterial therapy between the EOT Visit and the PTE Visit that may have been effective for the infection under study for a different infection from the one under study; unplanned major surgical intervention for the infection under study between the EOT and PTE Visits; participant died before evaluation. (NCT02378480)
Timeframe: Screening; 7 to 14 days after the last day of therapy

,
InterventionParticipants (Count of Participants)
Clinical successClinical failure
Linezolid24317
Omadacycline25910

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Number of Participants With the Indicated Investigator Assessment of Clinical Response in the mITT Population at the Post Therapy Evaluation (PTE) Visit

At the PTE Visit the investigator indicated one of the following outcomes relating to the primary infection under study: Clinical Success: participant was alive; the infection was sufficiently resolved such that further antibacterial therapy was not needed. These participants may have had some residual changes related to infection requiring ancillary treatment. Clinical Failure was defined as meeting any of the following criteria: infection required additional treatment with alternative antibacterial therapy; participant received antibacterial therapy between the End-of-Treatment (EOT) Visit and the PTE Visit that may have been effective for the infection under study for a different infection from the one under study; unplanned major surgical intervention for the infection under study between the EOT and PTE Visits; participant died before evaluation. Indeterminate: clinical response to test article could not be adequately inferred. (NCT02378480)
Timeframe: Screening; 7 to 14 days after the last day of therapy

,
InterventionParticipants (Count of Participants)
Clinical successClinical failureIndeterminate
Linezolid2602724
Omadacycline2722024

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Number of Participants With the Indicated Type of Adverse Event (AE)

An AE is defined as any untoward, undesired, or unplanned event in the form of signs, symptoms, disease, or laboratory or physiologic observations occurring in a person given a test article or in a clinical study. The event does not need to be causally related to the test article or clinical study. A serious adverse event (SAE) is defined as an event that resulted in death, was life-threatening, required hospitalization or prolongation of an existing hospitalization, resulted in a persistent or significant disability or incapacity, resulted in cancer, or resulted in a congenital anomaly or birth defect. A treatment-emergent AE (TEAE) is defined as any AE that newly appeared, increased in frequency, or worsened in severity on or after the initiation of active test article. Vital sign measurements, electrocardiogram findings, and laboratory values classified as adverse events were included in the analysis. Data are presented as the number of participants with at least 1 of the event. (NCT02378480)
Timeframe: 0 to 37 days

,
InterventionParticipants (Count of Participants)
AETEAEDrug-releated AESevere TEAESerious TEAEDrug-related serious TEAESerious TEAE leading to deathTEAE leading to premature drug discontinuationTEAE leading to premature discontinuation of studyTEAE leading to dose interruptionSerious TEAEs leading to drug discontinuation
Linezolid15714759108027703
Omadacycline15815658612016623

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Percentage of Participants Who Showed Microbiological Evidence of Cure 48 to 72 Hours From Randomization, EOT, and STFU

The microbiological outcome was assessed by the sponsor at 48 to 72 hours from randomization, EOT and STFU. It was based on blood and skin lesion identification results from baseline samples and skin lesion identification results from baseline samples and skin lesion identification results from follow-up samples as well as on, molecular typing results, and the IACO. Microbiological eradication rate was defined as proportion of participants with 'Documented Eradication' (absence of baseline pathogen(s) in follow-up cultures of the original site of infection.) or 'Presumed Eradication' (no material available for culture and an IACO of 'Success') in relation to the total number of participants in the respective treatment group. (NCT02426918)
Timeframe: 48 to 72 hours after randomization (Day 4), EOT (Day 12) and STFU (Day 19)

,,
Interventionpercentage of participants (Number)
48 to 72 hours after randomizationEOTSTFU
Debio 1450 160 mg/240 mg BID69.286.883.5
Debio 1450 80 mg/120 mg BID72.892.484.8
Vancomycin/Linezolid BID75.291.191.1

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Clinical Success Rate: Percentage of Participants Assessed by the Investigator as Responders at 48 to 72 Hours From Randomization, at End of Treatment (EOT) and Short-term Follow-up (STFU)

The Investigator Assessment of Clinical Outcome (IACO) of treatment was assessed for each participant as success or failure at 48 to 72 hours after randomization at EOT and STFU visits. Clinical success was resolution or near resolution of most disease-specific signs and symptoms and no new signs, symptoms, or complications attributable to ABSSSI such that no further antibiotic therapy is required for treatment of original site of infection. Clinical failure was requirement for additional antibiotic therapy for treatment of the original site of infection or incision and drainage of ABSSSI site that was not both anticipated and completed within a 48- to 72-hour window following randomization, or unplanned major surgical intervention required due to failure of study medication or development of osteomyelitis after baseline. Participants who met both success criteria and none of failure criteria were considered as a clinical success for IACO. (NCT02426918)
Timeframe: 48 to 72 hours after randomization (Day 4), EOT (Day 12) and STFU (Day 19)

,,
Interventionpercentage of participants (Number)
48 to 72 hours after randomizationEOTSTFU
Debio 1450 160 mg/240 mg BID81.387.983.5
Debio 1450 80 mg/120 mg BID83.792.484.8
Vancomycin/Linezolid BID86.192.192.1

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Early Clinical Response Rate (ECRR): Percentage of Responders to Treatment at 48 to 72 Hours From Randomization as Assessed by the Investigator

ECRR was defined as the percentage of responders to treatment at 48 to 72 hours from randomization. Responders were the participants who showed greater than or equal to (≥) 20% reduction in area of the primary lesion involving erythema, edema, or induration of the primary ABSSSI lesion (as assessed by the ruler method) at 48 to 72 hours compared to baseline. (NCT02426918)
Timeframe: At 48 to 72 hours from randomization (Day 4)

Interventionpercentage of participants (Number)
Debio 1450 80 mg/120 mg BID94.6
Debio 1450 160 mg/240 mg BID90.1
Vancomycin/Linezolid BID91.1

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Percentage of Participants With a Composite Assessment of Clinical Outcome (CACO) of Success

CACO of treatment was determined as a combined outcome of early response to treatment (at 48 to 72 hours from randomization) and IACO at the STFU visit. Participants had a CACO of success if they met both of the following criteria: An early response to treatment (at 48 to 72 hours from randomization) (ECR = responder) and a clinical outcome of success at the STFU visit (7 to 14 days after EOT) based on IACO (IACO = success). (NCT02426918)
Timeframe: 48 to 72 hours after randomization (Day 4) and STFU (Day 19)

Interventionpercentage of participants (Number)
Debio 1450 80 mg/120 mg BID83.7
Debio 1450 160 mg/240 mg BID81.3
Vancomycin/Linezolid BID88.1

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Percentage of Participants With ACM in the Microbiological Modified Intention-to-treat (mMITT) Population

The percentage of participants in the mMITT population with mortality due to any cause from randomization through Day 28 was determined for each arm. (NCT02493764)
Timeframe: Up to 28 days

InterventionPercentage of participants (Number)
IMI/REL16.7
PIP/TAZ20.2

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Percentage of Participants With All-cause Mortality (ACM) Through Day 28 in the Modified Intention-to-treat (MITT) Population

The percentage of participants in the MITT population with mortality due to any cause from randomization through Day 28 was determined for each arm. (NCT02493764)
Timeframe: Up to 28 days

InterventionPercentage of participants (Number)
IMI/REL15.9
PIP/TAZ21.3

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Percentage of Participants in the CE Population With a FCR at OTX2 (Day 6)

"The percentage of participants with a FCR at OTX2 was determined for each arm. Favorable clinical response at OTX2 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 6 (OTX2)

InterventionPercentage of participants (Number)
IMI/REL85.5
PIP/TAZ87.8

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Percentage of Participants in the CE Population With a FCR at EOT Visit

"The percentage of participants with a FCR at EOT was determined for each arm. Favorable clinical response at EOT was defined as either cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required) or improved (the majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: From Day 7 to Day 14

InterventionPercentage of participants (Number)
IMI/REL84.7
PIP/TAZ85.3

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Percentage of Participants in the CE Population With a FCR at EFU Visit

"The percentage of participants with a FCR at EFU was determined for each arm. Favorable clinical response at EFU was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to Day 30)

InterventionPercentage of participants (Number)
IMI/REL74.3
PIP/TAZ79.4

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Percentage of Participants in the CE Population With a FCR at OTX3 (Day 10)

"The percentage of participants with a FCR at OTX3 was determined for each arm. Favorable clinical response at OTX3 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 10 (OTX3)

InterventionPercentage of participants (Number)
IMI/REL89.6
PIP/TAZ83.6

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Percentage of Participants Discontinuing Study Therapy Due to an AE

An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02493764)
Timeframe: Up to 14 days

InterventionPercentage of participants (Number)
IMI/REL5.6
PIP/TAZ8.2

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Percentage of Participants in the MITT Population With a FCR at OTX1 (Day 3)

"The percentage of participants with a FCR at OTX1 was determined for each arm. Favorable clinical response at OTX1 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 3 (OTX1)

InterventionPercentage of participants (Number)
IMI/REL68.0
PIP/TAZ64.7

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Percentage of Participants in the mMITT Population With a FMR at EFU Visit

"The percentage of participants with a FMR at EFU was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EFU showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to Day 30)

InterventionPercentage of participants (Number)
IMI/REL67.9
PIP/TAZ61.9

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Percentage of Participants in the Clinically Evaluable (CE) Population With a FCR at On-therapy Visit 1 (OTX1) [Day 3]

"The percentage of participants with a FCR at OTX1 was determined for each arm. Favorable clinical response at OTX1 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 3 (OTX1)

InterventionPercentage of participants (Number)
IMI/REL70.8
PIP/TAZ72.8

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Percentage of Participants in the ME Population With a FMR at EFU Visit

"The percentage of participants with a FMR at EOT was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EOT showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to Day 30)

InterventionPercentage of participants (Number)
IMI/REL89.9
PIP/TAZ86.4

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Percentage of Participants in the Microbiologically Evaluable (ME) Population With a FMR at EOT Visit

"The percentage of participants with a FMR at EOT was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EOT showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: From Day 7 to Day 14

InterventionPercentage of participants (Number)
IMI/REL87.1
PIP/TAZ85.5

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Percentage of Participants in the CE Population With a FCR at Day 28

"The percentage of participants with a FCR at Day 28 was determined for each arm. Favorable clinical response at Day 28 was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Day 28

InterventionPercentage of participants (Number)
IMI/REL70.5
PIP/TAZ75.6

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Percentage of Participants in the MITT Population With a Favorable Clinical Response (FCR) at Early Follow-up (EFU) Visit

"The percentage of participants with a FCR at EFU was determined for each arm. Favorable clinical response at EFU was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to 30 days)

InterventionPercentage of participants (Number)
IMI/REL61.0
PIP/TAZ55.8

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Percentage of Participants in the MITT Population With a FCR at Day 28

"The percentage of participants with a FCR at Day 28 was determined for each arm. Favorable clinical response at Day 28 was defined as either sustained cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] with no evidence of resurgence and no additional antibiotics are required) or cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: Day 28

InterventionPercentage of participants (Number)
IMI/REL51.9
PIP/TAZ50.6

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Percentage of Participants in the MITT Population With a FCR at EOT

"The percentage of participants with a FCR at EOT was determined for each arm. Favorable clinical response at EOT was defined as either cure (all pre-therapy signs and symptoms of the index infection have resolved [or returned to pre-infection status] and no additional antibiotics are required) or improved (the majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status] and no additional antibiotics are required)." (NCT02493764)
Timeframe: From Day 7 to Day 14

InterventionPercentage of participants (Number)
IMI/REL74.2
PIP/TAZ69.7

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Percentage of Participants in the MITT Population With a FCR at OTX2 (Day 6)

"The percentage of participants with a FCR at OTX2 was determined for each arm. Favorable clinical response at OTX2 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 6 (OTX2)

InterventionPercentage of participants (Number)
IMI/REL83.5
PIP/TAZ83.1

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Percentage of Participants in the MITT Population With a FCR at OTX3 (Day 10)

"The percentage of participants with a FCR at OTX3 was determined for each arm. Favorable clinical response at OTX3 was defined as improved (majority of pre-therapy signs and symptoms of the index infection have improved or resolved [or returned to pre-infection status])." (NCT02493764)
Timeframe: Day 10 (OTX3)

InterventionPercentage of participants (Number)
IMI/REL83.5
PIP/TAZ80.4

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Percentage of Participants in the mMITT Population With a Favorable Microbiological Response (FMR) at End of Treatment (EOT) Visit

"The percentage of participants with a FMR at EOT was determined for each arm. Favorable microbiological response at EOT was defined as either eradication (a lower respiratory tract culture taken at EOT showing eradication of baseline pathogen) or presumed eradication (no specimen collected because the participant deemed clinically cured or improved)." (NCT02493764)
Timeframe: From Day 7 to Day 14

InterventionPercentage of participants (Number)
IMI/REL77.2
PIP/TAZ67.9

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Percentage of Participants With ≥1 Adverse Event (AE)

An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. (NCT02493764)
Timeframe: Up to 30 days

InterventionPercentage of participants (Number)
IMI/REL85.0
PIP/TAZ86.6

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Percentage of Participants With ACM at EFU in the MITT Population

The percentage of participants in the MITT population with mortality due to any cause from randomization through EFU was determined for each arm. (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to 30 days)

InterventionPercentage of participants (Number)
IMI/REL14.8
PIP/TAZ19.5

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Percentage of Participants With ACM at EFU in the mMITT Population

The percentage of participants in the mMITT population with mortality due to any cause from randomization through EFU was determined for each arm. (NCT02493764)
Timeframe: Up to 16 days after end of therapy (up to 30 days)

InterventionPercentage of participants (Number)
IMI/REL15.3
PIP/TAZ18.3

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Early Clinical Response (ECR)

ECR was defined as survival with improvement in at least 2 signs and symptoms of CABP (relative to baseline), no worsening of any CABP sign or symptom, and no use of concomitant antibiotics (other than adjunctive linezolid, as allowed by the study protocol) for the treatment of CABP through the ECR assessment. (NCT02559310)
Timeframe: ECR was assessed 96 +/- 24 hours after the first dose of study drug.

,
InterventionParticipants (Count of Participants)
ResponderNon-ResponderIndeterminate
Lefamulin241296
Moxifloxacin ± Linezolid248216

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All-cause Mortality

Time to all-cause Mortality was assessed on Day 28. (NCT02679573)
Timeframe: Day 28 (+/- 2 days)

InterventionParticipants (Count of Participants)
Delafloxacin8
Moxifloxacin/Linezolid6

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Early Clinical Response

Early clinical response defined as improvement in at least 2 of the following symptoms (as assessed by the investigator): chest pain, frequency or severity of cough, amount and quality of productive sputum, and difficulty breathing, and no worsening of the other symptoms in the ITT population. Symptom severity evaluated by the investigator on a 4-point scale: Absent (0), Mild (1), Moderate (2), Severe (3). Improvement defined as at least a 1-point decrease from baseline. (NCT02679573)
Timeframe: 96 (+/- 24) hours after the first dose of study drug

InterventionParticipants (Count of Participants)
Delafloxacin383
Moxifloxacin/Linezolid381

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Early Clinical Response Plus Improvement in Vital Signs and no Worsening of the 4 Symptoms

Early clinical response with the addition of improvement in vital signs and no worsening of the following 4 symptoms: chest pain, cough, productive sputum, and difficulty breathing in the ITT population. Symptom severity evaluated by the investigator on a 4-point scale: Absent (0), Mild (1), Moderate (2), Severe (3). Improvement defined as at least a 1-point decrease from baseline. Improvement in vital signs defined as a return to normal of any abnormal vital signs at baseline, and no worsening (ie, be abnormal) of any vital sign that was normal at baseline. (NCT02679573)
Timeframe: 96 (+/- 24) hours after the first dose of study drug

InterventionParticipants (Count of Participants)
Delafloxacin227
Moxifloxacin/Linezolid184

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Microbiologic Response

Microbiological response for subjects in the MITT set will be based on results of the baseline and follow-up cultures and susceptibility testing or serology. (NCT02679573)
Timeframe: 5 to 10 days after the last dose of study drug

InterventionParticipants (Count of Participants)
Delafloxacin231
Moxifloxacin/Linezolid235

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Number of Participants With Early Clinical Response

Early clinical response is defined as clinical success, which is categorized as survival with at least a 20% reduction of acute bacterial skin and skin structure infection (ABSSSI) primary lesion size compared to Screening measurements, without receiving any rescue antibacterial therapy. An indeterminate classification is used for a response that could not be adequately inferred because the participant was not assessed because they withdrew consent, were lost to follow-up, or other specified reason. (NCT02877927)
Timeframe: Screening; 48 to 72 hours after the first dose of test article

,
InterventionParticipants (Count of Participants)
Clinical successClinical failureIndeterminate
Linezolid2973231
Omadacycline3152619

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Number of Participants With the Indicated Investigator Assessment of Clinical Response in the Clinically Evaluable-Post Therapy Evaluation (CE-PTE) Population

At the PTE Visit the investigator indicated one of the following outcomes relating to the primary infection under study: Clinical Success: participant was alive; infection was sufficiently resolved such that further antibacterial therapy was not needed. Participants may have had some residual changes related to infection requiring ancillary treatment. Clinical Failure was defined as meeting any of the following criteria: infection required additional treatment with alternative antibacterial therapy; participant received antibacterial therapy between the EOT Visit and the PTE Visit that may have been effective for the infection under study for a different infection from the one under study; unplanned major surgical intervention for the infection under study between the EOT and PTE Visits; participant died before evaluation; other specified reason. (NCT02877927)
Timeframe: Screening; 7 to 14 days after the last day of therapy

,
InterventionParticipants (Count of Participants)
Clinical successClinical failure
Linezolid27913
Omadacycline2786

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Number of Participants With the Indicated Investigator Assessment of Clinical Response in the mITT Population at the Post Therapy Evaluation (PTE) Visit

At the PTE Visit the investigator indicated one of the following outcomes relating to the primary infection under study: Clinical Success: participant was alive; infection was sufficiently resolved such that further antibacterial therapy was not needed. Participants may have had some residual changes related to infection requiring ancillary treatment. Clinical Failure was defined as meeting any of the following criteria: infection required additional treatment with alternative antibacterial therapy; participant received antibacterial therapy between the End-of-Treatment (EOT) Visit and the PTE Visit that may have been effective for the infection under study for a different infection from the one under study; unplanned major surgical intervention for the infection under study between the EOT and PTE Visits; participant died before evaluation; other specified reason. Indeterminate The clinical response to test article could not be adequately inferred. (NCT02877927)
Timeframe: Screening; 7 to 14 days after the last day of therapy

,
InterventionParticipants (Count of Participants)
Clinical successClinical failureIndeterminate
Linezolid2912148
Omadacycline3031245

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Percentage of Participants With Clinical Cure at Test of Cure

"Clinical outcome was assessed by the investigator as either Clinical Cure, Clinical Failure, or Indeterminate.~Clinical Cure: Resolution or substantial improvement of Baseline signs and symptoms of pneumonia, including a reduction in Sequential Organ Failure Assessment (SOFA) and Clinical Pulmonary Infection Score (CPIS) scores, and improvement or lack of progression of chest radiographic abnormalities such that no additional antibacterial therapy was required for the treatment of the current infection." (NCT03032380)
Timeframe: Test of cure (7 days after the end of treatment; equivalent to Study Day 14 to 21)

Interventionpercentage of participants (Number)
Cefiderocol64.8
Meropenem66.7

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Percentage of Participants With Clinical Cure at End of Treatment (EOT)

"Clinical outcome was assessed by the investigator as either Clinical Cure, Clinical Failure, or Indeterminate.~Clinical Cure: Resolution or substantial improvement of Baseline signs and symptoms of pneumonia, including a reduction in Sequential Organ Failure Assessment (SOFA) and Clinical Pulmonary Infection Score (CPIS) scores, and improvement or lack of progression of chest radiographic abnormalities such that no additional antibacterial therapy was required for the treatment of the current infection." (NCT03032380)
Timeframe: End of treatment (Day 7 to 14)

Interventionpercentage of participants (Number)
Cefiderocol77.2
Meropenem81.0

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Percentage of Participants With Clinical Cure at Early Assessment (EA)

"Clinical outcome was assessed by the investigator as either Clinical Cure, Clinical Failure, or Indeterminate.~Clinical Cure: Resolution or substantial improvement of Baseline signs and symptoms of pneumonia, including a reduction in Sequential Organ Failure Assessment (SOFA) and Clinical Pulmonary Infection Score (CPIS) scores, and improvement or lack of progression of chest radiographic abnormalities such that no additional antibacterial therapy was required for the treatment of the current infection." (NCT03032380)
Timeframe: Early assessment (Day 3-4 after the start of treatment)

Interventionpercentage of participants (Number)
Cefiderocol82.8
Meropenem83.0

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All-cause Mortality Rate at the End of Study

The all-cause mortality rate during both the treatment and follow-up period (up to the end of study [EOS] visit) was calculated as the percentage of participants who experienced mortality, regardless of the cause, from the first infusion of study drug up to EOS. If a participant discontinued from the study before EOS and survival information was not available, then the survival status for this endpoint for the participant was considered unknown. (NCT03032380)
Timeframe: From first dose of study drug through end of study (28 days after end of treatment, up to 42 days)

Interventionpercentage of participants (Number)
Cefiderocol26.8
Meropenem23.3

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All-cause Mortality Rate at Day 28

The all-cause mortality (ACM) rate at Day 28 was calculated as the percentage of participants who experienced mortality, regardless of the cause, from the first dose of study drug up to Day 28. (NCT03032380)
Timeframe: From first dose of study drug to Day 28

Interventionpercentage of participants (Number)
Cefiderocol21.0
Meropenem20.5

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All-cause Mortality Rate at Day 14

"The all-cause mortality (ACM) rate at Day 14 was calculated as the percentage of participants in each treatment group who experienced mortality, regardless of the cause, from the first infusion of study drug up to Day 14.~The Modified Intent-to-Treat Population included all randomized participants who met either of the following criteria:~Evidence of Gram-negative infection of the lower respiratory tract based on a culture, Gram-stain, or other diagnostic test~Evidence of a lower respiratory tract infection but culture or other diagnostic tests did not provide a microbiologic diagnosis" (NCT03032380)
Timeframe: From first dose of study drug to Day 14

Interventionpercentage of participants (Number)
Cefiderocol12.4
Meropenem11.6

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Total Hospitalization Time

The length of hospital stay attributable to the study-qualifying infection. (NCT03032380)
Timeframe: From first dose of study drug to test of cure (7 days after end of treatment; equivalent to Study Day 14 to 21) and to follow-up (14 days after the end of treatment; Day 21 to 28)

,
Interventiondays (Mean)
Test of CureFollow-up
Cefiderocol11.5413.49
Meropenem11.4712.98

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Percentage of Participants With Sustained Microbiologic Eradication at Follow-up

"Microbiological outcome by Baseline pathogen at Follow-up was determined by the sponsor as either Sustained Eradication, Persistence, Recurrence, or Indeterminate. Overall per-participant microbiological outcome was determined based on the individual microbiological outcomes for each Baseline pathogen.~Sustained eradication: Absence of all Baseline Gram-negative pathogens from an appropriate clinical specimen (sputum, tracheal aspirate, BAL fluid, protected specimen brush, pleural fluid, or lung biopsy) after TOC. If it was not possible to obtain an appropriate clinical culture and the participant had a successful clinical response after TOC, the response was presumed to be eradication." (NCT03032380)
Timeframe: Follow-up (14 days after the end of treatment, Days 21 to 28)

Interventionpercentage of participants (Number)
Cefiderocol43.5
Meropenem38.6

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Number of Participants With Treatment-Emergent Adverse Events

"The severity of each adverse event (AE) was graded by the investigator according to the following definitions:~Mild: A finding or symptom is minor and does not interfere with usual daily activities.~Moderate: The event causes discomfort and interferes with usual daily activity or affects clinical status.~Severe: The event causes an interruption of the participant's usual daily activities or has a clinically significant effect.~The relationship of each AE to the study treatment was determined by the investigator based on whether the AE could be reasonably explained as having been caused by the study drug (treatment related AE [TRAE]).~An SAE is defined as any AE occurring at any dose that resulted in any of the following outcomes:~Death~Life-threatening condition~Hospitalization or prolongation of existing hospitalization for treatment~Persistent or significant disability/incapacity~Congenital anomaly/birth defect~Other medically important condition" (NCT03032380)
Timeframe: From first dose of study drug through the end of study, up to 42 days.

,
InterventionParticipants (Count of Participants)
Any adverse eventMild adverse eventsModerate adverse eventsSevere adverse eventsTreatment-related adverse eventsSerious adverse eventsTreatment-related serious adverse eventsAEs leading to discontinuation of study drugTRAE leading to discontinuation of study drugAdverse events leading to death
Cefiderocol1303341561454312239
Meropenem1293747451745514235

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Percentage of Participants With Microbiologic Eradication at End of Treatment

"Microbiological outcome by Baseline pathogen at End of Treatment was determined by the sponsor as either: Eradication, Persistence, or Indeterminate. Overall per-participant microbiological outcome was determined based on the individual microbiological outcomes for each Baseline pathogen.~Eradication: Absence of all Baseline Gram-negative pathogens from an appropriate clinical specimen (sputum, tracheal aspirate, BAL fluid, protected specimen brush, pleural fluid, or lung biopsy). If it was not possible to obtain an appropriate clinical culture, and the participant had a successful clinical outcome, the response was presumed as eradication." (NCT03032380)
Timeframe: End of treatment, Day 7 to 14

Interventionpercentage of participants (Number)
Cefiderocol63.7
Meropenem66.9

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Percentage of Participants With Sustained Clinical Cure at Follow-up (FU)

"Clinical outcome was assessed by the investigator at follow-up as either Sustained Clinical Cure, Relapse, or Indeterminate.~Sustained Clinical Cure: Continued resolution or substantial improvement of Baseline signs and symptoms of pneumonia, such that no antibacterial therapy was required for the treatment of pneumonia in a participant assessed as cured at TOC." (NCT03032380)
Timeframe: Follow-up (14 days after the end of treatment; Day 21 to 28)

Interventionpercentage of participants (Number)
Cefiderocol57.9
Meropenem57.8

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Percentage of Participants With Microbiologic Eradication at Test of Cure (TOC)

"Lower respiratory tract specimens (eg, sputum, endotracheal aspiration [ETA], endobronchial culture specimens collected by bronchoalveolar lavage [BAL], or protected specimen brush [PSB], lung biopsy tissue, pleural effusions, etc) were sent to the local microbiology laboratory for isolation and identification of pathogens.~Microbiological outcome by Baseline pathogen at TOC was determined by the sponsor as either Eradication, Persistence, or Indeterminate. Overall per-participant microbiological outcome was determined based on the individual microbiological outcomes for each Baseline pathogen.~Eradication: Absence of all Baseline Gram-negative pathogens from an appropriate clinical specimen (sputum, tracheal aspirate, bronchoalveolar lavage (BAL) fluid, protected specimen brush, pleural fluid, or lung biopsy). If it was not possible to obtain an appropriate clinical culture, and the participant had a successful clinical outcome, the response was presumed as eradication." (NCT03032380)
Timeframe: Test of cure (7 days after end of treatment; equivalent to Study Day 14 to 21)

Interventionpercentage of participants (Number)
Cefiderocol47.6
Meropenem48.0

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Percentage of Participants With Microbiologic Eradication at Early Assessment

"Microbiological outcome by Baseline pathogen at Early Assessment was determined by the sponsor as either Eradication, Persistence, or Indeterminate. Overall per-participant microbiological outcome was determined based on the individual microbiological outcomes for each Baseline pathogen.~Eradication: Absence of all Baseline Gram-negative pathogens from an appropriate clinical specimen (sputum, tracheal aspirate, BAL fluid, protected specimen brush, pleural fluid, or lung biopsy). If it was not possible to obtain an appropriate clinical culture, and the participant had a successful clinical outcome, the response was presumed as eradication." (NCT03032380)
Timeframe: Early Assessment, Days 3 to 4

Interventionpercentage of participants (Number)
Cefiderocol41.9
Meropenem53.5

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Time to Sputum Culture Conversion to Negative Status Through the Treatment Period

"Culture conversion is a diagnostic criteria indicating the point at which samples taken from a patient infected with tuberculosis can no longer produce tuberculosis cell cultures.~Note:~Culture conversion requires at least 2 consecutive culture negative/positive samples at least 7 days apart.~Participants who are documented at a visit as unable to produce sputum and who are clinically considered to be responding well to treatment will be considered to be culture negative at that visit." (NCT03086486)
Timeframe: 26 weeks

Interventionweeks (Median)
1200mg L x 26 Weeks + Pa + B4
1200 mg L x 9 Weeks + Pa + B4
600 mg L x 26 Weeks + Pa + B6
600 mg L x 9 Weeks + Pa + B6
Total6

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Percentage of Participants Achieving a Favorable Clinical Response at End of Therapy (EOT) Visit in the MITT Population

"Clinical response was defined as Improved (The majority of pre-therapy signs and symptoms of the index infection have improved or resolved or returned to pre-infection status AND no additional antibiotic therapy was required) or Cure (All pretherapy signs and symptoms of the index infection have resolved or returned to preinfection status AND no additional antibiotic therapy was required for the index infection). The percentage of participants achieving a favorable clinical response at EOT visit in the MITT population is presented." (NCT03583333)
Timeframe: Up to approximately 14 days

InterventionPercentage of Participants (Number)
IMI/REL FDC71.6
PIP/TAZ FDC68.4

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Percentage of Participants Achieving a Favorable Clinical Response at EOT Visit in the Clinically Evaluable (CE) Population

"Clinical response was defined as Improved (The majority of pre-therapy signs and symptoms of the index infection have improved or resolved or returned to pre-infection status AND no additional antibiotic therapy is required) or Cure (All pretherapy signs and symptoms of the index infection have resolved or returned to preinfection status) AND no additional antibiotic therapy is required for the index infection. The percentage of participants achieving a favorable clinical response at End of Treatment (EOT) visit in the CE population is presented." (NCT03583333)
Timeframe: Up to approximately 14 days

InterventionPercentage of Participants (Number)
IMI/REL FDC77.4
PIP/TAZ FDC82.3

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Percentage of Participants Achieving a Favorable Microbiological Response at EFU Visit in Microbiological-evaluable (ME) Population.

"A favorable by-pathogen microbiological response at EFU visit required eradication (A lower respiratory tract culture taken at the EFU visit showed eradication of the pathogen found at study entry) or presumed eradication (No specimen taken because participant was deemed clinically cured or improved) of the baseline pathogen. The percentage of participants achieving a favorable microbiological response at EFU visit in the ME population is presented." (NCT03583333)
Timeframe: Up to approximately 27 days

InterventionPercentage of Participants (Number)
IMI/REL FDC80.0
PIP/TAZ FDC78.4

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Percentage of Participants Achieving a Favorable Microbiological Response at EOT Visit in Microbiological Modified Intent-To-Treat Population (mMITT) Population

"Favorable overall microbiological response rates were defined as eradication (A lower respiratory tract culture taken at the EOT visit showed eradication of the pathogen found at study entry) OR presumed eradication (No specimen taken because participant was deemed clinically cured or improved) of the baseline pathogen. The percentage of participants achieving a favorable microbiological response at EOT visit in the mMITT population is presented." (NCT03583333)
Timeframe: Up to approximately 14 days

InterventionPercentage of Participants (Number)
IMI/REL FDC57.5
PIP/TAZ FDC60.3

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Percentage of Participants Achieving a Favorable Microbiological Response at EOT Visit in the ME Population

"Favorable overall microbiological response rates was defined as eradication (A lower respiratory tract culture taken at the EOT visit showed eradication of the pathogen found at study entry) OR presumed eradication (No specimen taken because participant was deemed clinically cured or improved) of the baseline pathogen. The percentage of participants achieving a favorable microbiological response at End of Treatment (EOT) visit in the ME population is presented." (NCT03583333)
Timeframe: Up to approximately 14 days

InterventionPercentage of Participants (Number)
IMI/REL FDC71.9
PIP/TAZ FDC74.5

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Percentage of Participants Discontinuing Study Drug Due to AEs

An AE was defined as any untoward medical occurrence in a participant, temporally associated with the use of study treatment, whether or not considered related to the study treatment. The percentage of participants that discontinued study therapy due to an AE was reported for each arm. (NCT03583333)
Timeframe: Up to approximately 14 days

InterventionPercentage of Participants (Number)
IMI/REL FDC3.7
PIP/TAZ FDC8.1

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Percentage of Participants Experiencing Adverse Events (AEs)

An AE was defined as any untoward medical occurrence in a participant, temporally associated with the use of study treatment, whether or not considered related to the study treatment. The percentage of participants experiencing an AE was reported for each arm. (NCT03583333)
Timeframe: Up to approximately 98 days

InterventionPercentage of Participants (Number)
IMI/REL FDC86.6
PIP/TAZ FDC84.6

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Percentage of Participants With All-cause Mortality Through Day 28 in the Modified Intent to Treat (MITT) Population

For each participant, survival status was assessed at Day 28 post-randomization and recorded on the electronic Case Report Form. The percentage of participants with all-cause mortality through Day 28 in the MITT population is presented. (NCT03583333)
Timeframe: Up to approximately 28 days

InterventionPercentage of Participants (Number)
IMI/REL FDC11.2
PIP/TAZ FDC5.9

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Percentage of Participants Achieving a Favorable Clinical Response at EFU Visit in the Clinically Evaluable (CE) Population

"Clinical response was defined as Sustained cure (All pretherapy signs and symptoms of the index infection have resolved or returned to preinfection status with no evidence of resurgence) AND no additional antibiotic therapy was required for the index infection or Cure (All pretherapy signs and symptoms of the index infection have resolved or returned to preinfection status) AND no additional antibiotic therapy was required for the index infection. The percentage of participants achieving a favorable clinical response at EFU visit in the CE population is presented." (NCT03583333)
Timeframe: Up to approximately 27 days

InterventionPercentage of Participants (Number)
IMI/REL FDC64.6
PIP/TAZ FDC62.2

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Percentage of Participants Achieving a Favorable Clinical Response at Early Follow-up (EFU) Visit in the MITT Population

"Clinical response was defined as Sustained cure (All pretherapy signs and symptoms of the index infection have resolved or returned to preinfection status with no evidence of resurgence AND no additional antibiotic therapy was required for the index infection) or Cure (All pretherapy signs and symptoms of the index infection have resolved or returned to preinfection status AND no additional antibiotic therapy was required for the index infection). The percentage of participants achieving a favorable clinical response at EFU visit in the MITT population is presented." (NCT03583333)
Timeframe: Up to approximately 27 days

InterventionPercentage of Participants (Number)
IMI/REL FDC50.7
PIP/TAZ FDC47.8

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Number of Participants With Microbiologic Response in the mITT Population

Microbiological response to treatment was determined using the following classification: (a) microbiologic success: all infecting pathogens isolated at Baseline were eradicated or presumed eradicated at the Test of Cure evaluation and no superinfecting pathogen was isolated from the site of infection under study; (b) microbiological failure: persistence or presumed persistence of one or more infecting pathogens or isolation of a superinfecting pathogen from the site of infection under study. (NCT03716024)
Timeframe: 10 to 17 days after the last dose of test article (intravenous or oral) (total treatment of up to 14 days)

,
Interventionparticipants (Number)
Microbiological successMicrobiological failure
Linezolid5721
Omadacycline7311

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Number of Participants With Clinical Response in the Clinically Evaluable (CE) Population

Clinical response is defined as CS, which was categorized as a determination by a BE that the infection had sufficiently resolved such that antibiotics were no longer needed, the participant received ≥1 dose of test article, the participant did not receive non-study antibiotics on >2 calendar days from Day 1 to the Test of Cure assessment, and the participant did not meet any of the criteria for clinical failure. CF was categorized as a determination by a BE that the infection had responded inadequately such that alternative antibiotics were needed, the BE discontinued test article due to an adverse event that was possibly/probably related to test article, the primary site of infection was surgically removed, or the participant received potentially effective antibiotics for treatment of the primary infection site on >2 days after study enrollment. A classification of indeterminate is used for any outcome that was not classified as CS or CF. (NCT03716024)
Timeframe: 10 to 17 days after the last dose of test article (intravenous or oral) (total treatment of up to 14 days)

,
Interventionparticipants (Number)
Clinical successClinical failure
Linezolid826
Omadacycline982

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Number of Participants With Clinical Response in the Modified Intent-to-Treat (mITT) Population

Clinical response is defined as clinical success (CS), which is categorized as a determination by a blinded evaluator (BE) that the infection had sufficiently resolved such that antibiotics were no longer needed, the participant (par.) received ≥1 dose of test article, the par. did not receive non-study antibiotics on >2 calendar days from Day 1 to the Test of Cure assessment, and the par. did not meet any of the criteria for clinical failure. Clinical failure (CF) is categorized as a determination by a BE that the infection had responded inadequately such that alternative antibiotics were needed, the BE discontinued test article due to an adverse event that was possibly/probably related to test article, the primary site of infection was surgically removed, or the par. received potentially effective antibiotics for treatment of the primary infection site on >2 days after study enrollment. A classification of indeterminate is used for any outcome that was not classified as CS or CF. (NCT03716024)
Timeframe: 10 to 17 days after the last dose of test article (intravenous or oral) (total treatment of up to 14 days)

,
Interventionparticipants (Number)
Clinical successClinical failureClinical failure: failureClinical failure: non-evaluable
Linezolid5919415
Omadacycline75927

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Number of Participants With Microbiologic Response in the Microbiologically Evaluable (ME) Population

Microbiological response to treatment was determined using the following classification: (a) microbiologic success: all infecting pathogens isolated at Baseline were eradicated or presumed eradicated at the Test of Cure evaluation and no superinfecting pathogen was isolated from the site of infection under study; (b) microbiological failure: persistence or presumed persistence of one or more infecting pathogens or isolation of a superinfecting pathogen from the site of infection under study. (NCT03716024)
Timeframe: 10 to 17 days after the last dose of test article (intravenous or oral) (total treatment of up to 14 days)

,
Interventionparticipants (Number)
Microbiological successMicrobiological failure
Linezolid576
Omadacycline734

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Microbiological Response

Documented or presumed eradication or persistence (NCT04042077)
Timeframe: up to 14 days (End Of Treatment visit) and 7-14 days after last dose (Test Of Cure visit)

InterventionParticipants (Count of Participants)
TOC Visit72552475TOC Visit72552474EOT Visit72552474EOT Visit72552475
EradicatedPersisted
Delafloxacin94
Best Available Therapy81
Delafloxacin11
Best Available Therapy21
Delafloxacin80
Best Available Therapy64
Delafloxacin25
Best Available Therapy38

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Number of Participants With Clinical Success at Test Of Cure Visit

"Clinical Success defined as the clinical response of Cure or improved. Below the definitions:~Cure: The complete resolution of all baseline signs and symptoms of SSI~Improved: two or more signs and/or symptoms (but not all) were considered resolved thus the patient had improved to an extent that no additional antibiotic treatment was necessary." (NCT04042077)
Timeframe: 7-14 days after last dose

InterventionParticipants (Count of Participants)
Delafloxacin123
Best Available Therapy119

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Number of Participants Eligible to Switch to Oral Formulation According to Blinded Observer's Assessment

"Blinded assessment based on patient stabilization and ability to tolerate OS diet. In particular, the following details had to be met:~Systolic blood pressure normal/not clinically significant abnormal No infection related tachycardia Afebrile status; body temperature <38°C for at least 24 hours* WBC count normalized/not clinically significant abnormal Patient able to tolerate PO diet/to take PO treatment and no GI absorption problem~The measure counts only the participants eligible to switch, without taking into account the actually switched. Indeed, only linezolid in the BAT has an equivalent oral formulation suitable for the switch." (NCT04042077)
Timeframe: up to 14 days

InterventionParticipants (Count of Participants)
Delafloxacin129
Best Available Therapy129

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Hospital Length of Stay (LOS)

Length of Stay since Screening till actual hospital discharge (NCT04042077)
Timeframe: up to 45 days (Late Follow Up visit)

Interventionhours (Mean)
Delafloxacin178.8
Best Available Therapy193.5

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