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gatifloxacin

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Description

Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes. [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]

Cross-References

ID SourceID
PubMed CID5379
CHEMBL ID31
CHEBI ID5280
SCHEMBL ID22591
MeSH IDM0209340

Synonyms (154)

Synonym
AB00171654-13
AB00171654-14
BRD-A74980173-001-02-8
gatifloxacin & gamma interferon
MLS000040259
am-1155
gatiflo
zymar
zymaxid
cg-5501
bonoq
SPECTRUM_001909
SPECTRUM5_001468
NCGC00178525-01
BSPBIO_002697
112811-59-3
gatifloxacin
C07661
am 1155
gtfx
3-quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-
tequin
am-1155 (*sesquihydrate*)
pd-135432
bms-206584
cg 5501
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-quinoline-3-carboxylic acid
MLS000759493
1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid
DB01044
gatifloxacin anhydrous
1-cyclopropyl-1,4-dihydro-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
cpd000043336
NCGC00095126-02
NCGC00095126-01
gatilox
bms 206584-01
(+-)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
gatispan
gaity
gatifloxacin [usan:inn]
pd 135432
gatiquin
smr000043336
KBIOGR_001613
KBIO3_001917
KBIO2_007578
KBIOSS_002448
KBIO2_002442
KBIO2_005010
SPECTRUM4_001127
SPECTRUM3_000999
SPECTRUM2_000487
SPBIO_000353
SPECTRUM1504272
HMS2090K10
HMS2093G06
AC-1944
bdbm50117914
zymer
nsc-758701
CHEMBL31 ,
gatifloxacin (tn)
zymer (tn)
D08011
gatifloxacin (inn)
CHEBI:5280 ,
gatifloxacinum
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
gatifloxacino
HMS1922J15
KINOME_3137
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
STK801620
NCGC00068236-02
A802657
AKOS004119932
NCGC00068236-04
NCGC00068236-05
NCGC00068236-06
NCGC00068236-03
HMS3259P06
BBL010485
nsc758701
pharmakon1600-01504272
dtxsid5045704 ,
dtxcid3025704
tox21_110984
cas-112811-59-3
HMS2233D20
CCG-39529
81485y3a9a ,
unii-81485y3a9a
nsc 758701
gatifloxin
tequin in dextrose 5% in plastic container
tymer
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
FT-0626635
FT-0631189
NCGC00068236-08
S1340
AKOS016340697
HMS3372J10
HMS3372J12
gatifloxacin [who-dd]
gatifloxacin [inn]
gatifloxacin [mi]
(+/-)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
CS-1841
HY-10581
NC00702
1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
SCHEMBL22591
tox21_110984_1
NCGC00068236-07
KS-1066
G-2380
gatifloxacin, antibiotic for culture media use only
XUBOMFCQGDBHNK-UHFFFAOYSA-N
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid
1-cyclopropyl-7-(3-methyl-1-piperazinyl)-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
MLS006011836
HB3263
c19h22fn3o4.1.5h2o
AB00171654_16
AB00171654_17
gatifloxcin
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazino)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
cg5501
SR-01000610458-3
mfcd00895399
sr-01000610458
SR-01000610458-2
SBI-0206764.P001
HMS3715N03
rkl10068
3-quinolinecarboxylic acid,1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-
FT-0668952
gatifloxacin,(s)
gatifloxacin sesquihydrate,(s)
1-cyclopropyl-6-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-3-quinolinecarboxylic acid
G0325
BCP13408
Q2365016
AMY17781
BRD-A74980173-001-06-9
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic a
gtpl10816
gatifloxacin 100 microg/ml in acetonitrile
1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylicacid
EN300-19768783
Z1824566854
SY070194

Research Excerpts

Overview

Gatifloxacin is a 4th generation fluoroquinolone antibiotic used in the clinic to treat ocular infection. Its adsorption onto iron minerals influenced by coexisting trace elements [e.g., Cu(II)] has not been well investigated.

ExcerptReferenceRelevance
"Gatifloxacin is a 4th generation fluoroquinolone antibiotic used in the clinic to treat ocular infection. "( Ultrasound-assisted gatifloxacin delivery in mouse cornea, in vivo.
Jegal, U; Jeong, H; Kim, KH; Kim, MJ; Lee, J; Lee, JH, 2019
)
2.28
"Gatifloxacin (GAT) is a new generation fluoroquinolone antibiotic and its adsorption onto iron minerals influenced by coexisting trace elements [e.g., Cu(II)] has not been well investigated. "( The impacts of Cu(II) complexation on gatifloxacin adsorption onto goethite and hematite.
Bi, E; Li, X, 2020
)
2.27
"Gatifloxacin is a fourth-generation antibiotic and its antibacterial activity is better. "( Effect of gatifloxacin in the treatment of ophthalmological diseases and continuous nursing intervention.
Chunqing, T; Hezhen, T; Shuying, W; Xiaoli, Z, 2018
)
2.33
"Gatifloxacin is an effective antibacterial drug."( Analysis of the drug therapy of gatifloxacin and levofloxacin in the treatment of acute bacterial conjunctivitis.
Feng, J; Xu, J, 2018
)
1.49
"Gatifloxacin (GFX) is a kind of chiral fluoroquinolones compound due to the methyl group at the C-3 position of the piperazine ring[1]. "( Preparative resolution of gatifloxacin enantiomers with pre-column esterification strategy and comparing their enantioselectivity to bacteria and antibody.
Cai, K; Huang, XL; Lei, HT; Liu, YJ; Sun, YM; Xu, ZL; Zhang, CJ, 2015
)
2.16
"Gatifloxacin is an 8-methoxy fluoroquinolone with broad activity against respiratory tract pathogens, including those commonly associated with community-acquired pneumonia (CAP). "( Oral gatifloxacin in outpatient community-acquired pneumonia: results from TeqCES, a community-based, open-label, multicenter study.
Gotfried, M; Gothelf, S; Nicholson, SC; Quinn, TC; Webb, CD; Wikler, MA, 2002
)
2.27
"Gatifloxacin is an advanced-generation fluoroquinolone with demonstrated efficacy and safety as therapy for community-acquired pneumonia (CAP). "( Gatifloxacin used for therapy of outpatient community-acquired pneumonia caused by Streptococcus pneumoniae.
Andes, DR; Ehrhardt, AF; Gothelf, S; Jones, RN; Mandell, LA; Nicholson, SC, 2002
)
3.2
"Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone approved by the United States Food and Drug Administration in December 1999. "( Bradycardic syncope in 2 patients who recently began gatifloxacin treatment.
Buxton, AE; Nicholson, WJ; Tammaro, D, 2003
)
2.01
"Gatifloxacin is an excellent choice when a fluoroquinolone is being considered for sequential switch therapy in the treatment of CAP requiring hospitalization."( IV-to-oral switch therapy for community-acquired pneumonia requiring hospitalization: focus on gatifloxacin.
Pelly, L,
)
1.07
"Gatifloxacin is a novel fourth-generation fluoroquinolone antibiotic that has MIC90 levels significantly lower than those of other fluoroquinolone agents. "( Vitreous penetration of orally administered gatifloxacin in humans.
Hariprasad, SM; Holz, ER; Mieler, WF, 2002
)
2.02
"Gatifloxacin is an 8-methoxyfluoroquinolone with good activity against respiratory pathogens."( Bacteriologic and clinical efficacy of oral gatifloxacin for the treatment of recurrent/nonresponsive acute otitis media: an open label, noncomparative, double tympanocentesis study.
Dagan, R; Echols, RM; Greenberg, D; Hamed, KA; Jacobs, MR; Ledeine, JM; Leiberman, A; Leibovitz, E; Pierce, PF; Piglansky, L; Press, J; Raiz, S, 2003
)
2.02
"Gatifloxacin is an 8-methoxy fluoroquinolone effective against a broad spectrum of pathogens common in pediatric infections. "( Pharmacokinetics of gatifloxacin in infants and children.
Blumer, JL; Bradley, JS; Capparelli, EV; Damle, BD; Grasela, DM; Jacobs, RF; Kearns, GL; Reed, MD, 2005
)
2.09
"Gatifloxacin (Tequin) is an 8-methoxy fluoroquinolone approved in the US for use in the treatment of community-acquired pneumonia (CAP), acute exacerbations of chronic bronchitis (AECB), acute sinusitis, uncomplicated and complicated urinary tract infections (UTIs), pyelonephritis, gonorrhoea and uncomplicated skin and skin structure infections. "( Gatifloxacin: a review of its use in the treatment of bacterial infections in the US.
Croom, KF; Keam, SJ; Keating, GM, 2005
)
3.21
"Gatifloxacin is a broad spectrum fluoroquinolone that offers enhanced Gram-positive activity and anaerobic coverage to other fluoroquinolones. "( A study to determine the pharmacokinetics of gatifloxacin following a single oral dose.
Banerjee, SN; Chakraborty, M; Chakravarty, M; Chattaraj, TK; Ghosh, A; Jayakumar, M; Mandal, U; Musmade, P; Pal, TK; Rajan, DS; Roy, K, 2004
)
2.03
"Gatifloxacin is a widely used fluoroquinolone antibiotic. "( Hyperglycemia and gatifloxacin: a case report and summary of current literature.
Beste, LA; Mersfelder, TL, 2005
)
2.1
"Gatifloxacin (GAT) is a new 8-methoxy fluoroquinolone with enhanced activity against gram-positive cocci. "( Activity of gatifloxacin in an in vitro pharmacokinetic-pharmacodynamic model against Staphylococcus aureus strains either susceptible to ciprofloxacin or exhibiting various levels and mechanisms of ciprofloxacin resistance.
Arpin, C; Ba, BB; Chausse, A; Quentin, C; Saux, MC; Vidaillac, C, 2006
)
2.16
"Gatifloxacin is a fluoroquinolone antibiotic that has been associated with severe hypoglycemic and hyperglycemic events."( Gatifloxacin-induced hyperglycemia: a case report and summary of the current literature.
Lee, AJ; Yip, C, 2006
)
3.22
"Gatifloxacin (GA) is an alternative, though it has not been thoroughly studied in Pediatrics yet."( Oral gatifloxacin in the outpatient treatment of children with cancer fever and neutropenia.
Alberto Pires Pereira, C; Altruda Carlesse, F; Petrilli, A, 2007
)
1.57
"Gatifloxacin is a flouroquinolone anti-bacterial agent. "( Influence of ethanol water-content on gatifloxacin recrystallisations.
Brits, M; Liebenberg, W; Paxton, E; Perold, Z, 2007
)
2.05
"Gatifloxacin is a 4th-generation fluoroquinolone previously under investigation for the treatment of otitis media in infants and children. "( Pharmacokinetics and pharmacodynamics of gatifloxacin in children with recurrent otitis media: application of sparse sampling in clinical development.
Ambrose, P; Arguedas, A; Cirincione, B; Grasela, DM; Lopez, E; Rubino, CM; Sáez-Llorens, X; Sher, L, 2007
)
2.05
"Gatifloxacin appears to be a promising new fluoroquinolone with acceptable susceptibility testing methods for routine clinical laboratory use."( Gatifloxacin (AM-1155, CG 5501) susceptibility testing interpretive criteria and quality control guidelines for dilution and disk (5-microgram) diffusion methods. The Quality Control Study Group.
Beach, ML; Biedenbach, DJ; Erwin, ME; Jones, RN; Kugler, KC; Pfaller, MA, 1999
)
2.47
"Gatifloxacin appears to be a potent anti-Haemophilus fluoroquinolone compound with in vitro testing interpretive criteria that will produce accurate results (disk diffusion, broth microdilution, and E-test)."( Activity of gatifloxacin against Haemophilus influenzae and Moraxella catarrhalis, including susceptibility test development, E-test comparisons, and quality control guidelines for H. influenzae.
Beach, ML; Biedenbach, DJ; Erwin, ME; Jones, RN; Pfaller, MA, 1999
)
1.4
"Gatifloxacin appears to be a promising new fluoroquinolone for clinical use in respiratory tract infections commonly caused by S."( Antimicrobial activity of gatifloxacin (AM-1155, CG5501), and four other fluoroquinolones tested against 2,284 recent clinical strains of Streptococcus pneumoniae from Europe, Latin America, Canada, and the United States. The SENTRY Antimicrobial Surveill
Beach, ML; Fluit, A; Jones, RN; Odland, BA; Verhoef, J, 1999
)
1.32
"Gatifloxacin is a novel extended-spectrum fluoroquinolone with improved gram-positive and anaerobe coverage compared with older agents such as ciprofloxacin. "( Gatifloxacin.
Barman Balfour, JA; Lamb, HM; Perry, CM, 1999
)
3.19
"Gatifloxacin is an advanced-generation, 8-methoxy fluoroquinolone that is active against a broad spectrum of pathogens, including antibiotic-resistant Streptococcus pneumoniae. "( Clinical pharmacology of gatifloxacin, a new fluoroquinolone.
Grasela, DM, 2000
)
2.05
"Gatifloxacin is a new 8-methoxy-fluoroquinoline antimicrobial agent. "( Gatifloxacin: a new fluoroquinolone.
Blondeau, JM, 2000
)
3.19
"Gatifloxacin is a new 8-methoxy-fluoroquinolone antibiotic approved for use in the United States in December 1999. "( Gatifloxacin, an advanced 8-methoxy fluoroquinolone.
Fish, DN; North, DS, 2001
)
3.2
"Gatifloxacin is a novel fluoroquinolone with a 3-methylpiperazine group at position 7 of the quinolone ring and a methoxy group at position 8 [287520,379131]; the 8-methoxy substituent seems to decrease the rate of development of resistance in Gram-positive bacteria [378631]. "( Gatifloxacin Kyorin Pharmaceutical Co.
Brown, WM, 2000
)
3.19
"Gatifloxacin is a new broad-spectrum fluoroquinolone with excellent activity against prevalent respiratory bacteria, including penicillin-resistant Streptococcus pneumoniae and atypical pathogens."( Multicenter evaluation of the efficacy and safety of gatifloxacin in Mexican adult outpatients with respiratory tract infections.
Casillas, JL; Mascareño, A; Rangel-Frausto, S; Rico, G; Rodríguez-Parga, D,
)
1.1
"Gatifloxacin is an advanced-generation, 8-methoxyfluoroquinolone that is active against a broad spectrum of pathogens, including antiobiotic resistant Streptococcus pneumoniae. "( Determination of gatifloxacin in human plasma by liquid chromatography/electrospray tandem mass spectrometry.
Bartlett, MG; Stewart, JT; Vishwanathan, K, 2001
)
2.09
"Gatifloxacin is an 8-methoxy fluoroquinolone. "( Activity of gatifloxacin against strains resistant to ofloxacin and ciprofloxacin and its ability to select for less susceptible bacterial variants.
Bonner, DP; Fung-Tomc, J; Gradelski, E; Huczko, E; Minassian, B, 2001
)
2.13
"Gatifloxacin is a new 8-methoxy fluoroquinolone. "( Comparative antimicrobial activity of gatifloxacin with ciprofloxacin and beta-lactams against gram-positive bacteria.
Andriole, VT; Bassetti, M; Callan, DA; Dembry, LM; Farrel, PA, 2001
)
2.02
"Gatifloxacin is an 8-methoxy fluoroquinolone antibacterial agent. "( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
3.2
"Gatifloxacin is a useful addition to the fluoroquinolones currently available for use in the clinical setting and has an important role in the management of adult patients with various bacterial infections."( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
2.48
"Gatifloxacin is a fluoroquinolone antibiotic with a broad spectrum of in vitro and in vivo activity against the gram-negative and gram-positive pathogens frequently implicated in urinary tract infections (UTIs)."( A randomized, double-blind, multicenter comparison of gatifloxacin versus ciprofloxacin in the treatment of complicated urinary tract infection and pyelonephritis.
Auerbach, SM; Brown, GL; Cox, CE; Fox, BC; Marbury, TC; Pittman, WG; Yang, JY, 2002
)
2.01
"Gatifloxacin is a new 8-methoxy fluoroquinolone with enhanced activity against gram-positive cocci. "( Pharmacodynamics of the new fluoroquinolone gatifloxacin in murine thigh and lung infection models.
Andes, D; Craig, WA, 2002
)
2.02

Effects

Gatifloxacin has a broad spectrum of antibacterial activity in vitro and good clinical and bacteriological efficacy in patients with indicated infections. The eye drop has a good therapeutic effect to the bacterial conjunctivitis.

Gatifloxacin has been reported to cause dysglycaemia, especially in the elderly and in diabetics. The eye drop has a good therapeutic effect to the bacterial conjunctivitis.

ExcerptReferenceRelevance
"Gatifloxacin has a susceptible dose-dependent zone at MICs 0.5-2 mg/L."( Gatifloxacin Pharmacokinetics/Pharmacodynamics-based Optimal Dosing for Pulmonary and Meningeal Multidrug-resistant Tuberculosis.
Ambrose, PG; Bendet, P; Bhavnani, SM; Deshpande, D; Gumbo, T; Gumusboga, M; Koeuth, T; McIlleron, H; Pasipanodya, JG; Smythe, W; Srivastava, S; Thwaites, G; Van Deun, A, 2018
)
2.64
"The gatifloxacin eye drop has a good therapeutic effect to the bacterial conjunctivitis. "( [Comparative research of the efficacy of the gatifloxacin and levofloxacin for bacterial conjunctivitis in human eyes].
Gong, L; Qiu, XD; Qu, J; Sun, XH; Xiong, QC; Yuan, ZL; Zhang, YQ, 2010
)
1.18
"Gatifloxacin has a broad spectrum of antibacterial activity in vitro and good clinical and bacteriological efficacy in patients with indicated infections following once-daily administration by the intravenous or oral routes."( Gatifloxacin: a review of its use in the treatment of bacterial infections in the US.
Croom, KF; Keam, SJ; Keating, GM, 2005
)
2.49
"Gatifloxacin has a large volume of distribution ( approximately 1.8 L/kg), low protein binding ( approximately 20%), and broad tissue distribution and is primarily excreted unchanged in the urine (>80%)."( Clinical pharmacology of gatifloxacin, a new fluoroquinolone.
Grasela, DM, 2000
)
1.33
"Gatifloxacin has a higher probability of achieving target AUC:MIC ratios than levofloxacin. "( The use of Monte Carlo simulation to examine pharmacodynamic variance of drugs: fluoroquinolone pharmacodynamics against Streptococcus pneumoniae.
Ambrose, PG; Grasela, DM, 2000
)
1.75
"Gatifloxacin has a long plasma elimination half-life, thus allowing once-daily administration."( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
2.48
"Gatifloxacin has an extended spectrum of antibacterial activity and provides better coverage of Gram-positive organisms (e.g. "( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
3.2
"Gatifloxacin has a susceptible dose-dependent zone at MICs 0.5-2 mg/L."( Gatifloxacin Pharmacokinetics/Pharmacodynamics-based Optimal Dosing for Pulmonary and Meningeal Multidrug-resistant Tuberculosis.
Ambrose, PG; Bendet, P; Bhavnani, SM; Deshpande, D; Gumbo, T; Gumusboga, M; Koeuth, T; McIlleron, H; Pasipanodya, JG; Smythe, W; Srivastava, S; Thwaites, G; Van Deun, A, 2018
)
2.64
"Gatifloxacin has been reported to cause dysglycaemia, especially in the elderly and in diabetics. "( Gatifloxacin-induced severe hyperglycaemia and ketoacidosis in a non-diabetic renal transplant recipient.
Agarwal, SK; Gupta, A; Khaira, A; Tandon, N, 2009
)
3.24
"The gatifloxacin eye drop has a good therapeutic effect to the bacterial conjunctivitis. "( [Comparative research of the efficacy of the gatifloxacin and levofloxacin for bacterial conjunctivitis in human eyes].
Gong, L; Qiu, XD; Qu, J; Sun, XH; Xiong, QC; Yuan, ZL; Zhang, YQ, 2010
)
1.18
"Gatifloxacin has been associated with increased risks of hypoglycemic and hyperglycemic side effects. "( Comparative and chemical proteomic approaches reveal gatifloxacin deregulates enzymes involved in glucose metabolism.
Bhosale, SD; Kulkarni, MJ; Suresh, KK; Thulasiram, HV, 2011
)
2.06
"Gatifloxacin has a broad spectrum of antibacterial activity in vitro and good clinical and bacteriological efficacy in patients with indicated infections following once-daily administration by the intravenous or oral routes."( Gatifloxacin: a review of its use in the treatment of bacterial infections in the US.
Croom, KF; Keam, SJ; Keating, GM, 2005
)
2.49
"Gatifloxacin has been associated with both hypoglycemia and hyperglycemia. "( Outpatient gatifloxacin therapy and dysglycemia in older adults.
Dresser, L; Juurlink, DN; Kopp, A; Low, DE; Mamdani, MM; Park-Wyllie, LY; Shah, BR; Stukel, TA; Stumpo, C, 2006
)
2.17
"Gatifloxacin recently has been reported to stimulate insulin secretion by inhibition of ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells."( Gatifloxacin acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis.
Inagaki, N; Kawasaki, Y; Nagashima, K; Seino, Y; Takahashi, A; Ueno, H; Yamada, C; Yamada, Y, 2006
)
2.5
"Gatifloxacin has a large volume of distribution ( approximately 1.8 L/kg), low protein binding ( approximately 20%), and broad tissue distribution and is primarily excreted unchanged in the urine (>80%)."( Clinical pharmacology of gatifloxacin, a new fluoroquinolone.
Grasela, DM, 2000
)
1.33
"Gatifloxacin has a higher probability of achieving target AUC:MIC ratios than levofloxacin. "( The use of Monte Carlo simulation to examine pharmacodynamic variance of drugs: fluoroquinolone pharmacodynamics against Streptococcus pneumoniae.
Ambrose, PG; Grasela, DM, 2000
)
1.75
"Gatifloxacin has a long plasma elimination half-life, thus allowing once-daily administration."( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
2.48
"Gatifloxacin has an extended spectrum of antibacterial activity and provides better coverage of Gram-positive organisms (e.g. "( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
3.2

Actions

Gatifloxacin can cause both hypoglycemia and hyperglycemia in both diabetic and non-diabetic patients. Gatifl Oxacin showed lower resistance levels than moxiflOxacin.

ExcerptReferenceRelevance
"Gatifloxacin could cause multi-system and multi-organ ADRs with wide variety of clinical manifestations. "( [Analysis of adverse drug reaction of gatifloxacin in Hunan province from Aug. 2003 to Jul. 2007].
Deng, S; He, Y; Long, L; Yin, T; Zhang, W, 2009
)
2.07
"Gatifloxacin showed lower resistance levels than moxifloxacin."( [In vitro antibiotic susceptibility to fluoroquinolones].
Galvis, V; Rey, JJ; Tello, A; Villareal, D; Wong, CA, 2012
)
1.1
"Gatifloxacin can cause both hypoglycemia and hyperglycemia in both diabetic and non-diabetic patients. "( Gatifloxacin acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis.
Inagaki, N; Kawasaki, Y; Nagashima, K; Seino, Y; Takahashi, A; Ueno, H; Yamada, C; Yamada, Y, 2006
)
3.22

Treatment

Gatifloxacin-treated eyes demonstrated significantly less inflammation, infection, and culture-positive endophthalmitis (P < 0.05), compared to the control animals. GLUT1 promoter activity was stimulated by 2.8 and 3.8 folds. Glucose uptake was decreased by 41% and 52%, respectively.

ExcerptReferenceRelevance
"The gatifloxacin treatment resulted in significant reductions in the scores on the JPN-NIH CPSI."( Gatifloxacin treatment for chronic prostatitis: a prospective multicenter clinical trial.
Hirose, T; Horita, H; Iwasawa, A; Koroku, M; Kunishima, Y; Matsukawa, M; Nishimura, M; Suzuki, N; Takahashi, S; Takeda, K; Takeyama, K; Tanaka, T; Tanda, H; Tsukamoto, T; Yokoo, A, 2008
)
2.27
"Gatifloxacin-treated eyes did not develop clinical infection and exhibited lower mean inflammation scores (P <.01 compared with the other groups)."( Fluoroquinolone therapy in multiple-drug resistant staphylococcal keratitis after lamellar keratectomy in a rabbit model.
Carpenter, TR; Kaufman, MB; McDonnell, PJ; Sarayba, MA; Sweet, PM; Taban, M; Tungsiripat, T, 2003
)
1.04
"Gatifloxacin-treated eyes demonstrated significantly less inflammation, infection, and culture-positive endophthalmitis (P < 0.05), compared to the control animals. "( Prevention of Staphylococcus aureus endophthalmitis with topical gatifloxacin in a rabbit prophylaxis model.
Bartholomew, LR; de Castro, LE; Sandoval, HP; Solomon, KD; Vroman, DT, 2006
)
2.01
"When treated with gatifloxacin at concentrations of 3.4 mug/ml (8.4 muM) and 17 mug/ml (42 muM), GLUT1 promoter activity was stimulated by 2.8 and 3.8 folds, GLUT1 mRNA expression was decreased by 41% and 31%, and glucose uptake was decreased by 41% and 52%, respectively."( Gatifloxacin affects GLUT1 gene expression and disturbs glucose homeostasis in vitro.
Ge, TF; Ho, YY; Law, PY; Wong, HY, 2007
)
2.11

Toxicity

Gatifloxacin appears to be safe for children, with no evidence of producing arthrotoxicity in 867 children exposed to the antibiotic. The drug is safe and efficacious in adults of any age with community-acquired pneumonia, including the elderly up to 100 years old.

ExcerptReferenceRelevance
" The most frequent treatment-related adverse effects were local intravenous site reactions, which were associated with dose and/or concentration of intravenous solution."( A dose-escalation study of the safety, tolerability, and pharmacokinetics of intravenous gatifloxacin in healthy adult men.
Birkhofer, MJ; Duncan, G; Gajjar, DA; Grasela, DM; Kollia, GD; LaCreta, FP; Uderman, HD, 2000
)
0.53
"Gatifloxacin was safe and well tolerated at intravenous doses of up to 800 mg/day for 14 days."( A dose-escalation study of the safety, tolerability, and pharmacokinetics of intravenous gatifloxacin in healthy adult men.
Birkhofer, MJ; Duncan, G; Gajjar, DA; Grasela, DM; Kollia, GD; LaCreta, FP; Uderman, HD, 2000
)
1.97
" All treatment-emergent adverse events were mild or moderate in intensity and resolved before subjects were discharged from the study."( Safety and pharmacokinetics of a single oral dose of gatifloxacin in patients with moderate to severe hepatic impairment.
Christofalo, B; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP; Manning, JA; Noveck, R, 2000
)
0.56
"Modest increases in Cmax and AUC0-infinity are not anticipated to have a negative effect on the outcome of therapy in hepatically impaired subjects, nor are they anticipated to result in adverse drug reactions."( Safety and pharmacokinetics of a single oral dose of gatifloxacin in patients with moderate to severe hepatic impairment.
Christofalo, B; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP; Manning, JA; Noveck, R, 2000
)
0.56
" The most commonly reported adverse events, nausea (2."( Multicenter evaluation of the efficacy and safety of gatifloxacin in Mexican adult outpatients with respiratory tract infections.
Casillas, JL; Mascareño, A; Rangel-Frausto, S; Rico, G; Rodríguez-Parga, D,
)
0.38
" The incidence of adverse events was low and the most commonly reported events were nausea and dyspepsia."( Effectiveness, safety and tolerability of gatifloxacin, a new 8-methoxyfluoroquinolone, in the treatment of outpatients with community-acquired pneumonia: a Brazilian study.
Carvalho, CR; Franca, SA, 2002
)
0.58
"Gatifloxacin, 400 mg PO once daily for 7 to 14 days, is effective and safe in the treatment of patients with CAP."( Effectiveness, safety and tolerability of gatifloxacin, a new 8-methoxyfluoroquinolone, in the treatment of outpatients with community-acquired pneumonia: a Brazilian study.
Carvalho, CR; Franca, SA, 2002
)
2.02
" Drug-related adverse events were reported by 27% of the patients, diarrhea being the most frequent, occurring in 12% of patients."( An open label, multicenter, non-comparative study of the efficacy and safety of oral gatifloxacin in the treatment of community-acquired pneumonia: a Brazilian study in five centers.
Nicodemo, AC, 2003
)
0.54
" Safety was determined through recording of adverse events."( A randomized, investigator- masked clinical trial comparing the efficacy and safety of gatifloxacin 0.3% administered BID versus QID for the treatment BID versus QID for the treatment of acute bacterial conjunctivitis of acute bacterial conjunctivitis.
Bernstein, P; Jensen, H; Schiffman, R; Tepedino, M; Whitcup, SM; Yee, RW, 2005
)
0.55
"6%) reported adverse events."( A randomized, investigator- masked clinical trial comparing the efficacy and safety of gatifloxacin 0.3% administered BID versus QID for the treatment BID versus QID for the treatment of acute bacterial conjunctivitis of acute bacterial conjunctivitis.
Bernstein, P; Jensen, H; Schiffman, R; Tepedino, M; Whitcup, SM; Yee, RW, 2005
)
0.55
"Gatifloxacin had adverse event rates that were similar overall to those of a comparator antibiotic (amoxicillin-clavulanate), except for increased diarrhea in children <2 years old receiving amoxicillin-clavulanate."( Safety and efficacy of gatifloxacin therapy for children with recurrent acute otitis media (AOM) and/or AOM treatment failure.
Arguedas, A; Dagan, R; Echols, R; Hamed, K; Pichichero, ME; Saez-Llorens, X; Sher, L, 2005
)
2.08
"Gatifloxacin appears to be safe for children, with no evidence of producing arthrotoxicity in 867 children exposed to the antibiotic when used as treatment for ROM and AOMTF."( Safety and efficacy of gatifloxacin therapy for children with recurrent acute otitis media (AOM) and/or AOM treatment failure.
Arguedas, A; Dagan, R; Echols, R; Hamed, K; Pichichero, ME; Saez-Llorens, X; Sher, L, 2005
)
2.08
"7% reported insignificant adverse events."( Efficacy and safety of gatifloxacin for urinary tract infection in nonspecialized Korean urologic practice.
Cho, IR; Cho, YH; Choo, MS; Hwang, TK; Kim, CI; Kim, CS; Kim, ME; Kim, MH; Kim, YG; Lee, KS; Lee, SD; Lee, SJ; Rhew, HY; Ryu, SB; Shim, BS; Sung, LH; Yoon, DK, 2006
)
0.64
" No significant adverse effects were reported."( Efficacy and safety of rabeprazole, amoxicillin, and gatifloxacin after treatment failure of initial Helicobacter pylori eradication.
Abdul-Baki, H; Aoun, E; Araj, GF; Chaar, HF; Kanj, SS; Sharara, AI, 2006
)
0.58
"In vitro cell cultures are useful for evaluating cell response to potentially toxic insults, although cell cultures may lack tissue components that may prevent or ameliorate damage in vivo."( Intrinsic cytotoxic effects of fluoroquinolones on human corneal keratocytes and endothelial cells.
Bezwada, P; Clark, LA; Schneider, S, 2008
)
0.35
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" Four patients did not complete the 1-year treatment because of adverse events."( The clinical efficacy and safety of a fluoroquinolone-containing regimen for pulmonary MAC disease.
Fujita, M; Harada, E; Ikegame, S; Kajiki, A; Matsumoto, T; Miyazaki, M; Nakanishi, Y; Ouchi, H; Tao, Y; Uchino, J; Watanabe, K, 2012
)
0.38
" Safety variables included adverse events (AEs), lisamine green, fluorescein ocular surface stains, and clinical signs of tolerability."( Efficacy and Safety of 0.6% Pazufloxacin Ophthalmic Solution Versus Moxifloxacin 0.5% and Gatifloxacin 0.5% in Subjects with Bacterial Conjunctivitis: A Randomized Clinical Trial.
Baiza-Durán, L; Casillas-Magallanes, M; Gómez-Bastar, PA; González-Lomelí, M; Lizárraga-Corona, A; Mercado-Sesma, AR; Montoya-Sánchez, IM; Mora-González, A; Ochoa-Tabares, JC; Olvera-Montaño, O; Oregon-Miranda, AA; Orozco-Carroll, M; Páez-Garza, JH; Pérez-Balbuena, AL; Sandoval-Delgadillo, LI; Saucedo-Rodríguez, LR; Villanueva-Najera, MA, 2018
)
0.7
" Therefore, we firstly explored the toxic effects and possible mechanism of cardiovascular toxicity induced by gatifloxacin (GTFX) and ciprofloxacin (CPFX) using zebrafish model."( The cardiovascular toxicity induced by high doses of gatifloxacin and ciprofloxacin in zebrafish.
Lan, R; Shen, R; Xia, Z; Yu, R; Yu, Y; Yuan, Z, 2019
)
0.97

Pharmacokinetics

Pharmacokinetics of a single 400-mg dose of gatifloxacin alone were characterized as follows (mean +/- standard deviation): peak concentration (Cmax), 3.

ExcerptReferenceRelevance
" The elimination half-life was 7 to 8 h, independently of the doses."( Single- and multiple-dose pharmacokinetics of AM-1155, a new 6-fluoro-8-methoxy quinolone, in humans.
Ishida, R; Kosuge, K; Kusajima, H; Masuda, Y; Nakashima, M; Ooie, T; Uchida, H; Uematsu, T, 1995
)
0.29
" With each organism, a series of monoexponential pharmacokinetic profiles of GA (half-life [t(1/2)], 7 h) and CI (t(1/2) = 4 h) were simulated to mimic different single doses of GA and two 12-h doses of CI."( Comparative pharmacodynamics of gatifloxacin and ciprofloxacin in an in vitro dynamic model: prediction of equiefficient doses and the breakpoints of the area under the curve/MIC ratio.
Firsov, AA; Kononenko, OV; Lubenko, IY; Vostrov, SN; Zinner, SH, 2000
)
0.59
" Adjustment for creatinine clearance had only a slight effect on Cmax but reduced the estimated effect of age on AUC0-infinity in women from a 32% increase to a 15% increase."( Age and gender effects on the pharmacokinetics of gatifloxacin.
Behr, D; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP, 2000
)
0.56
"The effects of age on gatifloxacin pharmacokinetic values were largely attributed to declining renal function, whereas those of gender were largely attributed to differences in body weight."( Age and gender effects on the pharmacokinetics of gatifloxacin.
Behr, D; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP, 2000
)
0.87
" There were no statistically significant differences in any other pharmacokinetic values except apparent oral clearance (ClT/F)."( Safety and pharmacokinetics of a single oral dose of gatifloxacin in patients with moderate to severe hepatic impairment.
Christofalo, B; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP; Manning, JA; Noveck, R, 2000
)
0.56
"Modest increases in Cmax and AUC0-infinity are not anticipated to have a negative effect on the outcome of therapy in hepatically impaired subjects, nor are they anticipated to result in adverse drug reactions."( Safety and pharmacokinetics of a single oral dose of gatifloxacin in patients with moderate to severe hepatic impairment.
Christofalo, B; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP; Manning, JA; Noveck, R, 2000
)
0.56
" Inter-subject pharmacokinetic and MIC variability may impact the probability of attaining optimal AUC:MIC ratios and hence favorable clinical outcome."( The use of Monte Carlo simulation to examine pharmacodynamic variance of drugs: fluoroquinolone pharmacodynamics against Streptococcus pneumoniae.
Ambrose, PG; Grasela, DM, 2000
)
0.31
"The pharmacodynamic parameters of peak serum drug concentration/MIC (peak/MIC) ratio and the area under the curve (AUC)/MIC ratio have been used to characterize in vivo drug exposure and its relationship to bacterial killing for the fluoroquinolones."( Pharmacodynamic assessment of gatifloxacin against Streptococcus pneumoniae.
Banevicius, M; Li, D; Mattoes, HM; Nicolau, DP; Nightingale, CH; Turley, C; Xuan, D, 2001
)
0.6
"Previous studies have demonstrated that fluoroquinolone area under the curve (AUC)/MIC ratios of 30 to 50 are sufficient to eradicate pneumococci from in vitro pharmacokinetic models (IVPMs)."( Pharmacodynamics of gatifloxacin against Streptococcus pneumoniae in an in vitro pharmacokinetic model: impact of area under the curve/MIC ratios on eradication.
Lister, PD, 2002
)
0.64
"In vitro and in vivo models of infection suggest that the area under the concentration-time curve (AUC): minimum inhibitory concentration (MIC) ratio is the pharmacodynamic parameter that is most predictive of bactericidal activity for the fluoroquinolones."( Pharmacodynamic profiling of levofloxacin and gatifloxacin using Monte Carlo simulation for community-acquired isolates of Streptococcus pneumoniae.
Ambrose, PG; Nicolau, DP, 2001
)
0.57
" We used the neutropenic murine thigh infection model to characterize the time course of antimicrobial activity of gatifloxacin and determine which pharmacokinetic (PK)-pharmacodynamic (PD) parameter best correlated with efficacy."( Pharmacodynamics of the new fluoroquinolone gatifloxacin in murine thigh and lung infection models.
Andes, D; Craig, WA, 2002
)
0.79
" Gatifloxacin was rapidly absorbed and a favourable elimination half-life of 7-8 h was evaluated."( Multiple-dose pharmacokinetics and excretion balance of gatifloxacin, a new fluoroquinolone antibiotic, following oral administration to healthy Caucasian volunteers.
Brault, M; Göhler, K; Gualano, V; Guillaume, M; Mignot, A; Millérioux, L; Stahlberg, HJ, 2002
)
1.47
"The pharmacokinetics of gatifloxacin were assessed in serum and in skin blister fluid (SBF), as was the pharmacodynamic activity in SBF."( Pharmacokinetics and pharmacodynamics of gatifloxacin against Streptococcus pneumoniae and Staphylococcus aureus in a granulocyte-rich exudate.
Laifer, G; Rajacic, Z; Trampuz, A; Wenk, M; Zimmerli, W, 2002
)
0.89
"First, a previously derived population pharmacokinetic model, with patient demographics, was used to estimate gatifloxacin AUC0-24 following a dosage regimen of 400 mg/24 h in 10 index patients with severe hyperglycaemia."( Gatifloxacin and the elderly: pharmacokinetic-pharmacodynamic rationale for a potential age-related dose reduction.
Ambrose, PG; Bhavnani, SM; Cirincione, BB; Grasela, TH; Piedmonte, M, 2003
)
1.97
" The pharmacokinetic profiles also reflected the effectiveness of GFLX."( Pharmacodynamics and bactericidal activity of gatifloxacin in experimental pneumonia caused by penicillin-resistant Streptococcus pneumoniae.
Fukuda, Y; Hirakata, Y; Kadota, J; Kohno, S; Miyazaki, Y; Murata, I; Tashiro, T; Tomono, K; Tsukamoto, K; Yanagihara, K, 2004
)
0.58
" Monte Carlo simulation was used to construct pharmacodynamic models for imipenem, meropenem, ertapenem, levofloxacin, gatifloxacin, and ciprofloxacin."( Pharmacodynamic modeling of carbapenems and fluoroquinolones against bacteria that produce extended-spectrum beta-lactamases.
Burgess, DS; Frei, CR; Moczygemba, LR, 2004
)
0.53
" In the pharmacodynamic models, imipenem and meropenem had an equal likelihood of achieving a free T>MIC > or =40% against bacteria that produced ESBLs (> or =97%) and bacteria that did not produce ESBLs (> or =98%)."( Pharmacodynamic modeling of carbapenems and fluoroquinolones against bacteria that produce extended-spectrum beta-lactamases.
Burgess, DS; Frei, CR; Moczygemba, LR, 2004
)
0.32
" Pharmacodynamic modeling based on local ESBL-producing isolates and pharmacokinetic data from healthy humans indicated that imipenem and meropenem may have a greater likelihood of achieving pharmacodynamic targets against bacteria that produce ESBLs than ertapenem or fluoroquinolones."( Pharmacodynamic modeling of carbapenems and fluoroquinolones against bacteria that produce extended-spectrum beta-lactamases.
Burgess, DS; Frei, CR; Moczygemba, LR, 2004
)
0.32
" The pharmacokinetic parameters (Cmax, AUCo-t, tmax) of this drug have been evaluated to compare the single dose (400mg) bioavailability of gatifloxacin with the reference formulation."( A study to determine the pharmacokinetics of gatifloxacin following a single oral dose.
Banerjee, SN; Chakraborty, M; Chakravarty, M; Chattaraj, TK; Ghosh, A; Jayakumar, M; Mandal, U; Musmade, P; Pal, TK; Rajan, DS; Roy, K, 2004
)
0.79
" Previously described population pharmacokinetic models of gatifloxacin and levofloxacin administration in patients with serious CAP were utilised to simulate gatifloxacin and levofloxacin pharmacokinetics."( Comparison of gatifloxacin and levofloxacin administered at various dosing regimens to hospitalised patients with community-acquired pneumonia: pharmacodynamic target attainment study using North American surveillance data for Streptococcus pneumoniae.
Hoban, DJ; Noreddin, AM; Zhanel, GG, 2005
)
0.93
" Risk analysis software was used to simulate 10,000 patients by integrating published pharmacokinetic parameters, their variability, and minimum inhibitory concentration (MIC) distributions from the TSN database."( Pharmacodynamic analysis of ceftriaxone, gatifloxacin,and levofloxacin against Streptococcus pneumoniae with the use of Monte Carlo simulation.
Burgess, DS; Frei, CR, 2005
)
0.59
"Ceftriaxone maintained high probability of target attainment over a broad range of pharmacodynamic targets regardless of penicillin susceptibility (%T > MIC 0-60%)."( Pharmacodynamic analysis of ceftriaxone, gatifloxacin,and levofloxacin against Streptococcus pneumoniae with the use of Monte Carlo simulation.
Burgess, DS; Frei, CR, 2005
)
0.59
" Plasmatic pharmacokinetic profiles after daily 1-h perfusion of 400 mg for 48 h were accurately simulated."( Activity of gatifloxacin in an in vitro pharmacokinetic-pharmacodynamic model against Staphylococcus aureus strains either susceptible to ciprofloxacin or exhibiting various levels and mechanisms of ciprofloxacin resistance.
Arpin, C; Ba, BB; Chausse, A; Quentin, C; Saux, MC; Vidaillac, C, 2006
)
0.71
" Pharmacokinetic parameters were estimated by fitting appropriate models to the serum concentration-time data using ADAPT II."( Gatifloxacin pharmacokinetics in healthy men and women.
Kays, MB; Overholser, BR; Sowinski, KM; Zhang, X, 2006
)
1.78
" A population pharmacokinetic model was developed to describe the pharmacokinetics of gatifloxacin in children."( Population pharmacokinetic model for gatifloxacin in pediatric patients.
Blumer, JL; Bradley, JS; Capparelli, EV; Cirincione, B; Grasela, DM; Jacobs, RF; Kearns, GL; Reed, M; Rubino, CM, 2007
)
0.84
" In this study, we aimed to develop a novel pharmacokinetic model to describe NQs-metal cation interactions in order to estimate the optimal dosing interval."( Antacid interaction with new quinolones: dose regimen recommendations based on pharmacokinetic modeling of clinical data for ciprofloxacin, gatifloxacin and norfloxacin and metal cations.
Miyata, K; Ohtani, H; Sawada, Y; Tsujimoto, M, 2007
)
0.54
"Plasma concentration-time profiles of NQs after administration without or with metal cations at various dosing intervals were collected from the literature and analyzed with a pharmacokinetic model incorporating the formation ofNQs-metal cations complex."( Antacid interaction with new quinolones: dose regimen recommendations based on pharmacokinetic modeling of clinical data for ciprofloxacin, gatifloxacin and norfloxacin and metal cations.
Miyata, K; Ohtani, H; Sawada, Y; Tsujimoto, M, 2007
)
0.54
"Based on the findings of this study in small numbers of healthy young adult volunteers and patients with chronic bronchitis, BMS appears to be a promising method for measuring drug concentrations and determining the pharmacokinetic profile of gatifloxacin in bronchial ELF."( Pharmacokinetics of gatifloxacin after a single oral dose in healthy young adult subjects and adult patients with chronic bronchitis, with a comparison of drug concentrations obtained by bronchoscopic microsampling and bronchoalveolar lavage.
Ishizaka, A; Kikuchi, E; Kikuchi, J; Nishimura, M; Yamazaki, K, 2007
)
0.84
"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
)
0.56
" 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
" Mean+/-standard deviation gatifloxacin elimination half-life (t(1/2)), systemic clearance and volume of distribution in patients with CrCL>or=40 mL/min were 10."( Evaluation of gatifloxacin pharmacokinetics and pharmacodynamics in severely ill adults in a medical Intensive Care Unit.
Fish, DN, 2007
)
1
" We then used population pharmacokinetic models for gatifloxacin and simulation to identify dosing regimens with high probabilities of attaining exposures likely to be efficacious in adults and children."( Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
Ambrose, PG; Bhavnani, SM; Craig, WA; Drusano, GL; Forrest, A; Heine, HS; Rubino, CM, 2007
)
0.86
"The objective of this study was to determine the population pharmacokinetic parameters of levofloxacin, gatifloxacin, and moxifloxacin following multiple oral doses."( Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
Boom, WH; Dietze, R; Hadad, DJ; Johnson, JL; Molino, LP; Palaci, M; Peloquin, CA, 2008
)
0.82
" 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
" The developed assay method was applied to a pharmacokinetic study in human volunteers following oral administration of 400 mg GFC tablet."( Development and validation of a HPLC method for simultaneous quantitation of gatifloxacin, sparfloxacin and moxifloxacin using levofloxacin as internal standard in human plasma: application to a clinical pharmacokinetic study.
Mullangi, R; Narasu, L; Shankar, BP; Srinivas, N, 2008
)
0.57
" The serum concentration of GFLX was measured for each patient, and population and pharmacokinetic (PPK) analysis was performed, using the Bayesian method, to calculate the AUC and maximum drug concentration (Cmax)."( Evaluation of clinical dosage of gatifloxacin for respiratory tract infections in elderly patients based on pharmacokinetics/pharmacodynamics (PK/PD).
Hara, H; Kamao, T; Kawanishi, M; Kimura, M; Kishimoto, M; Matsushima, T; Miyashita, N; Moriya, O; Nakamura, J; Niki, Y; Oka, M; Okimoto, N; Tanimukai, T; Uno, M; Watanabe, M; Yoneyama, H; Yoshida, K, 2008
)
0.63
" 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
)
0.61
"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
)
0.61
" Pharmacokinetic and pharmacodynamic indices, other than the minimum inhibitory concentration (MIC), were used as therapeutic parameters in ocular tissues."( Comparative Study of Ocular Pharmacokinetics of Gatifloxacin Between Continuous Lavage and Hourly Topical Instillation in Rabbits.
Chen, S; Lu, H; Shen, X; Wang, M; Zhang, X; Zhao, X, 2018
)
0.74

Compound-Compound Interactions

We studied the activities of clarithromycin and fluoroquinolones in combination with other antimycobacterial drugs against extracellular and intramacrophage Mycobacterium avium complex (MAC) The activity of meropenem combined with either polymyxin B or gatifloxacin was evaluated by the checkerboard method against Pseudomonas aeruginosa (10 strains) and Acinetobacter baumannii.

ExcerptReferenceRelevance
"The activity of gatifloxacin against Toxoplasma gondii, either alone or in combination with pyrimethamine or gamma interferon (IFN-gamma), was examined in vitro and in vivo."( Activity of gatifloxacin alone or in combination with pyrimethamine or gamma interferon against Toxoplasma gondii.
Araujo, FG; Khan, AA; Remington, JS; Slifer, TR, 2001
)
1.04
" In the chequerboard method, the quinolones were tested in combination with ten antimicrobial agents (macrolides, aminoglycosides, beta-lactams, vancomycin, rifampicin and chloramphenicol) against five bacterial strains (one strain each of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis and Streptococcus pneumoniae)."( Activity of gatifloxacin and ciprofloxacin in combination with other antimicrobial agents.
Bonner, DP; Fung-Tomc, J; Gradelski, E; Kolek, B; Minassian, B; Valera, L, 2001
)
0.69
"We studied the activities of clarithromycin and fluoroquinolones (gatifloxacin, sitafloxacin, levofloxacin) in combination with other antimycobacterial drugs against extracellular and intramacrophage Mycobacterium avium complex (MAC)."( Antimicrobial activities of clarithromycin, gatifloxacin and sitafloxacin, in combination with various antimycobacterial drugs against extracellular and intramacrophage Mycobacterium avium complex.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.81
"Studies were undertaken in order to assess the anti- Mycobacterium tuberculosis (MTB) activities of newly developed fluoroquinolones in combination with other antituberculous drugs."( Anti-Mycobacterium tuberculosis activities of new fluoroquinolones in combination with other antituberculous drugs.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.31
"A new C-8-methoxyl fluoroquinolone, gatifloxacin (GFLX), and a new C-8-chloro fluoroquinolone, sitafloxacin (STFX), in combination with other drugs were examined for their activities against extracellular growing MTB organisms and those replicating in RAW264."( Anti-Mycobacterium tuberculosis activities of new fluoroquinolones in combination with other antituberculous drugs.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.59
" Both GFLX and STFX exhibited combined activities against intramacrophage MTB, when used in combination with rifampin, rifalazil, isoniazid, pyrazinamide, ethambutol, streptomycin, or clofazimine."( Anti-Mycobacterium tuberculosis activities of new fluoroquinolones in combination with other antituberculous drugs.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.31
" The silicon slides were covered by dense and black stained material in the blank group; the black stained material as mildly less in the group treated with anti-alginate serum, and much less in the group treated with gatifloxacin, and the BF was thin and only slightly stained black in the group treated with anti-alginate combined with gatifloxacin."( Influence of anti-alginate serum combined with gatifloxacin on mucoid pseudomonas aeruginosa biofilm morphology.
Chai, D; Chen, Q; Li, X; Pei, F; Wang, R, 2002
)
0.76
"Anti-alginate serum affects the structure and morphology of the biofilm of mucoid Pseudomonas aeruginosa and destroys the biofilm structure when combined with gatifloxacin."( Influence of anti-alginate serum combined with gatifloxacin on mucoid pseudomonas aeruginosa biofilm morphology.
Chai, D; Chen, Q; Li, X; Pei, F; Wang, R, 2002
)
0.77
"To study the in vitro interaction of gatifloxacin in combination with gentamicin and with the beta-lactams cefepime, meropenem and piperacillin against clinical isolates of Stenotrophomonas maltophilia, Pseudomonas aeruginosa, Burkholderia cepacia, extended-spectrum beta-lactamase (ESBL)-producing Klebsiella pneumoniae, vancomycin-resistant Enterococcus faecium (VRE) and methicillin-resistant Staphylococcus aureus (MRSA)."( In vitro activity of gatifloxacin alone and in combination with cefepime, meropenem, piperacillin and gentamicin against multidrug-resistant organisms.
Dawis, MA; France, KA; Isenberg, HD; Jenkins, SG, 2003
)
0.91
" Several regimens of gatifloxacin in combination with rifampicin were compared with isoniazid plus rifampicin in a mouse tuberculosis model."( Gatifloxacin in combination with rifampicin in a murine tuberculosis model.
Cynamon, M; Shoen, C; Sklaney, MR, 2007
)
2.1
"Gatifloxacin in combination with rifampicin is a promising combination for potential evaluation in human clinical trials."( Gatifloxacin in combination with rifampicin in a murine tuberculosis model.
Cynamon, M; Shoen, C; Sklaney, MR, 2007
)
3.23
" When the three FQs were individually combined with CLR in vitro, mild antagonism was observed for 53 to 57% of the tested isolates."( In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
Fukushima, K; Higashiyama, Y; Hirakata, Y; Kohno, S; Kohno, Y; Miyazaki, Y; Ohno, H; Yanagihara, K, 2007
)
0.34
"The antimicrobial activity of meropenem combined with either polymyxin B or gatifloxacin was evaluated by the checkerboard method against Pseudomonas aeruginosa (10 strains) and Acinetobacter baumannii (10 strains)."( In vitro evaluation of the antimicrobial activity of meropenem in combination with polymyxin B and gatifloxacin against Pseudomonas aeruginosa and Acinetobacter baumannii.
Cardoso, CL; Carrara-Marrone, FE; Gales, AC; Garcia, LB; Guelfi, KC; Tognim, MC, 2008
)
0.79
"In this study, it was aimed to investigate the effects of quinupristin/dalfopristin in combination with vancomycin and gatifloxacin against Staphylococcus aureus and Enterococcus faecium isolates."( [In vitro activities of quinupristin/dalfopristin in combination with vancomycin and gatifloxacin against Staphylococcus aureus and Enterococcus faecium clinical isolates].
Ermertcan, S; Gülden, E, 2009
)
0.79
"3% solutions alone or when treatment was combined with steroids, and to correlate these concentrations with the minimum inhibitory concentrations (MIC) for the most common endophthalmitis-causing organisms."( Aqueous humor concentrations of topical fluoroquinolones alone or in combination with a steroid.
Campos, M; Cruz, AC; Gomes, RLR; Lima, AAS; Melo, LAS; Suenaga, EM; Viana, RG,
)
0.13

Bioavailability

The pharmacokinetic parameters (Cmax, AUCo-t, tmax) of this drug have been evaluated. The oral bioavailability of gatifloxacin was 72·96 ± 1·10 %. After an oral administration in humans, the majority is excreted in the urine as the unchanged form.

ExcerptReferenceRelevance
"The pharmacokinetics of gatifloxacin (400 mg orally) and the influence of the antacid aluminum magnesium hydroxide (20 ml of Maalox 70) on the bioavailability of gatifloxacin in 24 healthy volunteers were assessed."( Pharmacokinetics of gatifloxacin and interaction with an antacid containing aluminum and magnesium.
Koeppe, P; Lober, S; Lode, H; Mignot, A; Rau, M; Schreiber, G; Ziege, S, 1999
)
0.93
" The absolute bioavailability of gatifloxacin after oral administration was 96%, consistent with bioequivalence of the 400-mg intravenous and oral doses."( Interchangeability of 400-mg intravenous and oral gatifloxacin in healthy adults.
Duncan, G; Grasela, DM; Kaul, S; Kollia, GD; LaCreta, FP; Randall, DM, 2000
)
0.84
" The drug has high oral bioavailability (96%), and, therefore, oral and intravenous formulations are bioequivalent and interchangeable."( Clinical pharmacology of gatifloxacin, a new fluoroquinolone.
Grasela, DM, 2000
)
0.61
" Bioavailability is 96%, with a plasma half-life of approximately 8 hours in individuals with normal renal function."( Gatifloxacin, an advanced 8-methoxy fluoroquinolone.
Fish, DN; North, DS, 2001
)
1.75
" Gatifloxacin is absorbed well from the gastrointestinal tract (oral bioavailability is almost 100%)."( Gatifloxacin: a review of its use in the management of bacterial infections.
Hurst, M; Onrust, SV; Ormrod, D; Perry, CM, 2002
)
2.67
" Moreover, the rate of absorption was not affected by food intake."( Oral bioavailability of gatifloxacin in healthy volunteers under fasting and fed conditions.
Göhler, K; Guillaume, M; Mignot, A; Stahlberg, HJ, 2002
)
0.62
"Previous studies have demonstrated a significant reduction in the oral bioavailability of trovafloxacin and ciprofloxacin when administered concomitantly with an intravenous opiate, such as morphine."( Minimal interaction between gatifloxacin and oxycodone.
Grant, EM; Nicolau, DR; Nightingale, C; Quintiliani, R, 2002
)
0.61
" Bioavailability testing indicated that although the 90% confidence intervals (CIs) for the ratio of the geometric means of the calcium-fortified juice and water arms' AUC stayed within the range of 80% to 125%, those for Cmax did not."( Lack of bioequivalence of gatifloxacin when coadministered with calcium-fortified orange juice in healthy volunteers.
Amsden, GW; Victory, JM; Wallace, AW, 2003
)
0.62
"Sequential intravenous-to-oral antimicrobial therapy with highly bioavailable antiinfective agents such as the fluoroquinolones may improve patient safety and decrease cost of infection management."( Bioavailability of gatifloxacin by gastric tube administration with and without concomitant enteral feeding in critically ill patients.
Barletta, JF; Devlin, JW; Kanji, S; Kruse, JA; McKinnon, PS, 2003
)
0.65
" Bioavailability was determined as the ratio of NG/intravenous area under the concentration-time curve (AUC infinity ) measured by the trapezoidal method."( Bioavailability of gatifloxacin by gastric tube administration with and without concomitant enteral feeding in critically ill patients.
Barletta, JF; Devlin, JW; Kanji, S; Kruse, JA; McKinnon, PS, 2003
)
0.65
" More research is needed to identify those patients in whom gatifloxacin bioavailability is reduced and for whom an empirical increase in gatifloxacin dose should be considered."( Bioavailability of gatifloxacin by gastric tube administration with and without concomitant enteral feeding in critically ill patients.
Barletta, JF; Devlin, JW; Kanji, S; Kruse, JA; McKinnon, PS, 2003
)
0.89
" After an oral administration in humans, gatifloxacin is well absorbed and distributed, and the majority is excreted in the urine as the unchanged form."( [Antibacterial property and clinical effect of gatifloxacin, a novel quinolone antibacterial agent].
Hosaka, M, 2003
)
0.84
"Studies have shown that the bioavailability of gatifloxacin is decreased with concurrent administration of antacids containing aluminum or magnesium; dietary supplements containing zinc, magnesium, and iron; multivitamin preparations containing minerals; and sucralfate."( Coadministration of gatifloxacin and multivitamin preparation containing minerals: potential treatment failure in an elderly patient.
Huang, A; Mallet, L, 2005
)
0.91
" At the 10-mg/kg dose, the bioavailability was similar between the suspension and tablet formulation."( Pharmacokinetics of gatifloxacin in infants and children.
Blumer, JL; Bradley, JS; Capparelli, EV; Damle, BD; Grasela, DM; Jacobs, RF; Kearns, GL; Reed, MD, 2005
)
0.65
" The pharmacokinetic parameters (Cmax, AUCo-t, tmax) of this drug have been evaluated to compare the single dose (400mg) bioavailability of gatifloxacin with the reference formulation."( A study to determine the pharmacokinetics of gatifloxacin following a single oral dose.
Banerjee, SN; Chakraborty, M; Chakravarty, M; Chattaraj, TK; Ghosh, A; Jayakumar, M; Mandal, U; Musmade, P; Pal, TK; Rajan, DS; Roy, K, 2004
)
0.79
"To determine the effect of Ensure on the relative oral bioavailability of gatifloxacin in healthy volunteers."( Effect of ensure on the oral bioavailability of gatifloxacin in healthy volunteers.
Goldman, M; Kays, MB; Lagvankar, S; Overholser, BR; Sowinski, KM, 2005
)
0.81
"The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid pre-corneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and then undergo a sol-gel transition in the cul-de-sac."( Study of an alginate/HPMC-based in situ gelling ophthalmic delivery system for gatifloxacin.
Ding, P; Li, J; Liu, H; Liu, Z; Nie, S; Pan, W, 2006
)
0.56
" Intestinal permeation study also revealed the decreased bioavailability of gatifloxacin relatively to the presence of aluminium hydroxide."( Interaction characteristics and thermodynamic behaviour of gatifloxacin by aluminium hydroxide.
De, PK; Ghoshal, G; Mallick, S; Mondal, A; Pattnaik, S; Saha, A; Swain, K, 2007
)
0.81
"The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of gel system."( Study on the ocular pharmacokinetics of ion-activated in situ gelling ophthalmic delivery system for gatifloxacin by microdialysis.
Li, J; Li, X; Liu, Z; Pan, W; Yang, XG, 2007
)
0.56
" In conclusion, gatifloxacin liposomal hydrogel is a suitable delivery system for the improvement of the ocular bioavailability of gatifloxacin."( Optimization of gatifloxacin liposomal hydrogel for enhanced transcorneal permeation.
Hosny, KM, 2010
)
1.05
" These "in combo" PAMPA data were used to predict the human absolute bioavailability of the ampholytes."( The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
Avdeef, A; Sun, N; Tam, KY; Tsinman, O, 2010
)
0.36
"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
" Gatifloxacin showed better bioavailability and sustained action in aqueous humor and corneal tissue from the nanoparticles compared to the commercial eye drops."( Mucoadhesive nanoparticles as carrier systems for prolonged ocular delivery of gatifloxacin/prednisolone bitherapy.
El-Leithy, IS; Ibrahim, HK; Makky, AA, 2010
)
1.5
" Such clarification may lead to the development of strategies to overcome efflux and enhance its bioavailability at target site."( Interaction of gatifloxacin with efflux transporters: a possible mechanism for drug resistance.
Kwatra, D; Mitra, AK; Pal, D; Vadlapatla, RK; Vadlapudi, AD, 2010
)
0.71
"This study aims to improve gatifloxacin bioavailability to the eye using solid-lipid nanoparticles (SLN)."( Part I: Development and optimization of solid-lipid nanoparticles using Box-Behnken statistical design for ocular delivery of gatifloxacin.
Abul Kalam, M; Ali, A; Aljuffali, IA; Alshamsan, A; Aqil, M; Mishra, AK; Sultana, Y, 2013
)
0.89
"The successful ophthalmic delivery system is reliant on the diminution in the precorneal loss of drugs by increasing the corneal contact time and increasing the transcorneal permeability, which may enhance the bioavailability of drug to the eyes."( Delivery of gatifloxacin using microemulsion as vehicle: formulation, evaluation, transcorneal permeation and aqueous humor drug determination.
Aljuffali, IA; Alshamsan, A; Kalam, MA; Mishra, AK; Sultana, Y, 2016
)
0.81
", solubility in an aqueous medium and lipophilic properties, which have an effect on the bioavailability of five selected fluoroquinolones."( Experimental and theoretical studies on the molecular properties of ciprofloxacin, norfloxacin, pefloxacin, sparfloxacin, and gatifloxacin in determining bioavailability.
Betlejewska-Kielak, K; Biernacka, J; Grudzień, M; Kłosińska-Szmurło, E; Mazurek, AP; Pluciński, FA, 2014
)
0.61
"The developed system is a viable alternative to conventional eyedrops of GTN due to its ability to enhance bioavailability through its longer precorneal residence time."( Therapeutic Effectiveness in the Treatment of Experimental Bacterial Keratitis with Ion-activated Mucoadhesive Hydrogel.
Kant, S; Kesavan, K; Pandit, JK, 2016
)
0.43
"The present investigation aimed at improving the ocular bioavailability of gatifloxacin by prolonging its residence time in the eye and reducing problems associated with the drug re-crystallization after application through incorporation into cationic polymeric nanoparticles."( Development of gatifloxacin-loaded cationic polymeric nanoparticles for ocular drug delivery.
Al-Kassas, R; Deo, S; Duxfield, L; Englebretsen, V; Rupenthal, I; Sultana, R; Swift, S; Wang, R, 2016
)
1.02
"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
" Two modified melittin peptides displayed rapid bactericidal properties against antibiotic-resistant strains, low innate resistance development by pathogenic bacteria, remained nonimmunogenic for T lymphocytes, and increased bioavailability in tear fluids."( Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
Agrawal, R; Barathi, VA; Beuerman, RW; Chan, LW; Jie, TY; Koh, SK; Lakshminarayanan, R; Leng, ET; Mayandi, V; Sebastian, TM; Somaraju Chalasani, ML; Ting, DSJ; Urf Turabe Fazil, MH; Varadarajan, J; Verma, NK; Xi, Q; Zhou, L, 2020
)
0.56

Dosage Studied

Gatifloxacin should be avoided in the same patient population, and the recommended dosage of 400 mg/day should not be exceeded. The optimized microemulsion possessed good stability and showed greater adherence to corneal surface.

ExcerptRelevanceReference
" The bactericidal activity of gatifloxacin in CSF was closely related to the AUC/MBC ratio, but maximal activity was achieved only when drug concentrations exceeded the MBC for the entire dosing interval."( Pharmacodynamics of gatifloxacin in cerebrospinal fluid in experimental cephalosporin-resistant pneumococcal meningitis.
Friedland, IR; Ghaffar, F; Jafri, HS; Lutsar, I; McCoig, CC; McCracken, GH; Ng, W; Wubbel, L, 1998
)
0.91
" Based on achievable serum levels with projected gatifloxacin dosing regimens, MIC break points of < or = 2 micrograms/mL (> or = 18 mm) for susceptibility and > or = 8 micrograms/mL (< or = 14 mm) for resistance were selected."( Gatifloxacin (AM-1155, CG 5501) susceptibility testing interpretive criteria and quality control guidelines for dilution and disk (5-microgram) diffusion methods. The Quality Control Study Group.
Beach, ML; Biedenbach, DJ; Erwin, ME; Jones, RN; Kugler, KC; Pfaller, MA, 1999
)
2
" Our data suggest that gatifloxacin dosed at 400 mg od should be adequate to treat systemic infections caused by most bacterial species."( A study to determine the pharmacokinetics and inflammatory fluid penetration of gatifloxacin following a single oral dose.
Andrews, JM; Ashby, JP; Marshall, J; Wise, R, 1999
)
0.84
" pneumoniae, with standard dosing resulting in area under the concentration-time curve/MIC ratios and peak concentration/MIC ratios that resulted in 99."( Activities of trovafloxacin, gatifloxacin, clinafloxacin, sparfloxacin, levofloxacin, and ciprofloxacin against penicillin-resistant Streptococcus pneumoniae in an in vitro infection model.
Hershberger, E; Rybak, MJ, 2000
)
0.6
" Physical examinations, ECGs, spirometry, and clinical laboratory tests, including glucose tolerance test (GTT) and assessment of glucose homeostasis, were performed before treatment and on selected dosing days."( A dose-escalation study of the safety, tolerability, and pharmacokinetics of intravenous gatifloxacin in healthy adult men.
Birkhofer, MJ; Duncan, G; Gajjar, DA; Grasela, DM; Kollia, GD; LaCreta, FP; Uderman, HD, 2000
)
0.53
" Serial blood and urine samples were collected for 96 hours after dosing to determine drug concentrations."( Age and gender effects on the pharmacokinetics of gatifloxacin.
Behr, D; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP, 2000
)
0.56
" These modest age- and gender-related differences do not warrant dosage adjustment."( Age and gender effects on the pharmacokinetics of gatifloxacin.
Behr, D; Duncan, G; Grasela, DM; Kollia, GD; LaCreta, FP, 2000
)
0.56
" Physical examinations, electrocardiograms, spirometry, and clinical laboratory tests were performed before dosing and on selected dosing days."( Effect of multiple-dose gatifloxacin or ciprofloxacin on glucose homeostasis and insulin production in patients with noninsulin-dependent diabetes mellitus maintained with diet and exercise.
Berger, S; Gajjar, DA; Grasela, DM; Kollia, GD; LaCreta, FP; Smith, WB; Stolz, RR; Swingle, M, 2000
)
0.61
" Bactericidal activity of gatifloxacin was correlated with the area under the time-concentration curve-to-MBC ratio; maximal activity was achieved when gatifloxacin concentrations exceeded the MBC for the entire dosing interval."( Pharmacodynamics of gatifloxacin in experimental models of pneumococcal meningitis.
McCracken, GH, 2000
)
0.93
" All quinolones tested selected for resistance; judicious use and proper dosing will be necessary to avoid resistance selection of newer broad-spectrum fluoroquinolones."( Single- and multi-step resistance selection study of gemifloxacin compared with trovafloxacin, ciprofloxacin, gatifloxacin and moxifloxacin in Streptococcus pneumoniae.
Appelbaum, PC; Davies, TA; Dewasse, BE; Jacobs, MR; Nagai, K, 2001
)
0.52
" Gatifloxacin should be avoided in the same patient population, and the recommended dosage of 400 mg/day should not be exceeded."( Rates of torsades de pointes associated with ciprofloxacin, ofloxacin, levofloxacin, gatifloxacin, and moxifloxacin.
Frothingham, R, 2001
)
1.44
" Many of the fluoroquinolone agents have once-daily dosing regimens, enhancing patient adherence."( The expanding role of fluoroquinolones.
Schaeffer, AJ, 2002
)
0.31
" Following multiple oral doses of 400 and 600 mg, the pharmacokinetics of gatifloxacin were similar on days 1 and 15, suggesting no therapeutically relevant time-dependent changes in the pharmacokinetics of gatifloxacin at the doses and duration of dosing studied."( Multiple-dose pharmacokinetics and excretion balance of gatifloxacin, a new fluoroquinolone antibiotic, following oral administration to healthy Caucasian volunteers.
Brault, M; Göhler, K; Gualano, V; Guillaume, M; Mignot, A; Millérioux, L; Stahlberg, HJ, 2002
)
0.79
" Patients received gatifloxacin 400 mg either by the intravenous or NG route followed by the alternative dosage form after a 72-hr washout period."( Bioavailability of gatifloxacin by gastric tube administration with and without concomitant enteral feeding in critically ill patients.
Barletta, JF; Devlin, JW; Kanji, S; Kruse, JA; McKinnon, PS, 2003
)
0.98
" For example, the cost implications of using manufacturers' recommendations for dosing in patients with renal dysfunction may be important, depending on the distribution of various levels of renal function within a patient population."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Also, costs of failing to adjust dosing regimens for decreased renal function were determined."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Costs potentially incurred by failing to adjust dosing for renal function were substantial."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
"Formulary decisions can be facilitated by considering factors such as patient characteristics and related dosing in addition to simple acquisition costs."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
"First, a previously derived population pharmacokinetic model, with patient demographics, was used to estimate gatifloxacin AUC0-24 following a dosage regimen of 400 mg/24 h in 10 index patients with severe hyperglycaemia."( Gatifloxacin and the elderly: pharmacokinetic-pharmacodynamic rationale for a potential age-related dose reduction.
Ambrose, PG; Bhavnani, SM; Cirincione, BB; Grasela, TH; Piedmonte, M, 2003
)
1.97
"The impact of the pharmacokinetic/pharmacodynamic (PK/PD) parameters (the 24h area under the concentration-time curve [AUC24h]/minimum inhibitory concentration [MIC] and maximum concentration in serum [Cmax]/MIC ratio) after single oral dosing of gatifloxacin on its bactericidal activity and resistance selectivity against quinolone-susceptible clinical isolates of Streptococcus pneumoniae J-69 was investigated using an in vitro PK model."( The effect of pharmacokinetic/pharmacodynamic (PK/PD) parameters of gatifloxacin on its bactericidal activity and resistance selectivity against clinical isolates of Streptococcus pneumoniae.
Ebisu, H; Fukuda, H; Kishii, R; Takei, M, 2003
)
0.74
" With both NEK and IEK simulations, significant increases in MIC were observed at those AUC(24)/MICs that correspond to gatifloxacin concentrations within the MSW over most of the dosing interval (>25%)."( Concentration-dependent changes in the susceptibility and killing of Staphylococcus aureus in an in vitro dynamic model that simulates normal and impaired gatifloxacin elimination.
Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2004
)
0.73
"The efficacy and safety of two oral dosing regimens of gatifloxacin were compared to ciprofloxacin in the treatment of complicated urinary tract infection in a randomised, double-blind multi-centre trial."( Gatifloxacin 200 mg or 400 mg once daily is as effective as ciprofloxacin 500 mg twice daily for the treatment of patients with acute pyelonephritis or complicated urinary tract infections.
Ankel-Fuchs, D; Bartnicki, A; Bischoff, W; Hanus, M; Milutinovic, S; Naber, KG; Schönwald, S; van Belle, F; Weitz, P, 2004
)
2.01
"The efficacy and safety of two oral dosing regimens of gatifloxacin compared with ciprofloxacin for the treatment of acute uncomplicated lower urinary tract infection was investigated in a double-blind, randomised study, in adult female patients who received either gatifloxacin (400 mg as a single shot or 3 days of 200 mg once daily) or ciprofloxacin (250 mg given twice daily for 3 days)."( Gatifloxacin 400 mg as a single shot or 200 mg once daily for 3 days is as effective as ciprofloxacin 250 mg twice daily for the treatment of patients with uncomplicated urinary tract infections.
Allin, DM; Ankel-Fuchs, D; Clarysse, L; Haworth, DA; Hopkins, G; James, IG; Naber, KG; Raini, C; Schneider, H; Wall, A; Weitz, P, 2004
)
2.01
"The aqueous penetration of the commercial preparations of the fluoroquinolone antibiotics ofloxacin, ciprofloxacin, levofloxacin, and gatifloxacin were compared following topical dosing in a rabbit model."( Aqueous penetration of gatifloxacin and levofloxacin into the rabbit aqueous humor following topical dosing.
Blanchard, J; Lane, LC; Levine, JM; Noecker, RJ; Rapedius, M; Snyder, RW, 2004
)
0.84
" Eyes were dosed according to a keratitis protocol; ie, every 15 minutes for 4 hours."( Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing.
Herrygers, L; Lane, LC; Levine, JM; Nix, D; Noecker, RJ; Snyder, RW, 2004
)
0.58
"In the keratitis dosing protocol, the mean concentration of moxifloxacin in the aqueous (n=9) was 11."( Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing.
Herrygers, L; Lane, LC; Levine, JM; Nix, D; Noecker, RJ; Snyder, RW, 2004
)
0.58
" There was no statistically significant difference between the 2 drugs in the cataract prophylaxis dosing model."( Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing.
Herrygers, L; Lane, LC; Levine, JM; Nix, D; Noecker, RJ; Snyder, RW, 2004
)
0.58
"To compare the effects of the commercial formulations of moxifloxacin and gatifloxacin on rabbit corneal epithelium using two dosing protocols: high-frequency dosing for bacterial keratitis and cataract surgery prophylaxis."( Comparison of corneal surface effects of gatifloxacin and moxifloxacin using intensive and prolonged dosing protocols.
Herrygers, LA; Lane, LC; Levine, JM; Noecker, RJ, 2005
)
0.83
"Despite differences in formulations, with short-term dosing neither gatifloxacin nor moxifloxacin appears to be toxic to the corneal epithelium in this rabbit model."( Comparison of corneal surface effects of gatifloxacin and moxifloxacin using intensive and prolonged dosing protocols.
Herrygers, LA; Lane, LC; Levine, JM; Noecker, RJ, 2005
)
0.83
"3% dosing varied among 4 groups with frequencies of 16-48 doses/day (days 1-2), 3-16 doses/day (days 3-7), and maintenance dosing of 3-4 doses/day (days 8-22)."( Comparison of ophthalmic gatifloxacin 0.3% and ciprofloxacin 0.3% in healing of corneal ulcers associated with Pseudomonas aeruginosa-induced ulcerative keratitis in rabbits.
Carrier, M; Jensen, H; Short, B; Zerouala, C, 2005
)
0.63
"To report a case of severe hyperglycemia in a nondiabetic patient receiving gatifloxacin that was properly dosed based on renal function."( Severe hyperglycemia during renally adjusted gatifloxacin therapy.
Blommel, AL; Lutes, RA,
)
0.62
" Dosing regimens for gatifloxacin were 400 mg once daily (qd) administered to younger patients (<65 years) and gatifloxacin 200 mg qd to elderly patients (> or =65 years)."( Comparison of gatifloxacin and levofloxacin administered at various dosing regimens to hospitalised patients with community-acquired pneumonia: pharmacodynamic target attainment study using North American surveillance data for Streptococcus pneumoniae.
Hoban, DJ; Noreddin, AM; Zhanel, GG, 2005
)
1.01
" The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation <2%), while being simple, cheap and less time consuming and can be suitably applied for the estimation of gatifloxacin in different dosage forms and dissolution studies."( New, simple and validated UV-spectrophotometric methods for the estimation of gatifloxacin in bulk and formulations.
Saha, RN; Venugopal, K,
)
0.54
" The method was applied to the determination of LFX, SFX and GFX in dilute urine samples and dosage forms, and compared with the HPLC method."( Electrochemical adsorptive behavior of some fluoroquinolones at carbon paste electrode.
Abdel Ghani, NT; El Ries, MA; El-Shall, MA; Wassel, AA, 2005
)
0.33
"5% ophthalmic solutions are toxic to the corneal epithelium when used with 1 of 2 dosing regimens in healthy human eyes."( Effect of gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions on human corneal epithelium following 2 dosing regimens.
Maclellan, D; Price, FW; Price, MO, 2005
)
0.73
"5% did not result in clinically significant epithelial toxicity in healthy human corneas after dosing regimens of 4 times a day for 7 days or hourly for 10 hours dosing regimens."( Effect of gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions on human corneal epithelium following 2 dosing regimens.
Maclellan, D; Price, FW; Price, MO, 2005
)
0.73
"3% solution in the aqueous humor (AH) in humans after topical application with published levels of other available fluoroquinolones under similar dosing conditions."( Fourth-generation fluoroquinolone penetration into the aqueous humor in humans.
Aronowicz, JD; Caudle, D; McCulley, JP; Shine, WE, 2006
)
0.33
" This regimen simulated a realistic postoperative dosing schedule."( Fourth-generation fluoroquinolone penetration into the aqueous humor in humans.
Aronowicz, JD; Caudle, D; McCulley, JP; Shine, WE, 2006
)
0.33
"Aqueous humor antibiotic concentrations achieved at the time of cataract surgery after topical application can serve as an effective surrogate for what can be achieved with typical postoperative topical dosing (e."( Fourth-generation fluoroquinolone penetration into the aqueous humor in humans.
Aronowicz, JD; Caudle, D; McCulley, JP; Shine, WE, 2006
)
0.33
"A simple and sensitive high-performance thin-layer chromatography (HPTLC) method has been developed for the quantitative estimation of gatifloxacin and ornidazole in its combined dosage forms."( Determination of gatifloxacin and ornidazole in tablet dosage forms by high-performance thin-layer chromatography.
Marolia, BP; Patel, HM; Rathod, IS; Shah, DR; Shah, SA; Suhagia, BN, 2006
)
0.88
"5 points above the INR before fluoroquinolone use; major or minor bleeding events; requirement for vitamin K administration; warfarin dosage reduction or withholding doses; and warfarin-related hospital, emergency, or urgent care admissions or visits."( Anticoagulation-related outcomes in patients receiving warfarin after starting levofloxacin or gatifloxacin.
Cole, J; Mathews, S; Ryono, RA, 2006
)
0.55
" The value of dosing of antimicrobial agents based on MPC thresholds results in a rapid reduction in viable cells--even at higher inocula which are more reflective of organism burden in pneumonia."( Application of two methods to determine killing of Streptococcus pneumoniae by various fluoroquinolones.
Blondeau, JM; Blondeau, LD; Borsos, S; Hesje, C, 2006
)
0.33
"Simple, rapid, and extractive spectrophotometric methods were developed for the determination of gatifloxacin (GT) in bulk and pharmaceutical dosage form."( Spectrophotometric determination of gatifloxacin in pure form and in pharmaceutical formulation.
Amin, AS; El-Fetouh Gouda, AA; El-Sheikh, R; Zahran, F, 2007
)
0.83
"The broad spectrum of antimicrobial activity, oral bioavailability, extensive tissue distribution, and once-daily intravenous or oral dosing of gatifloxacin, an expanded-spectrum 8-methoxy fluoroquinolone, make it a potentially useful agent for the treatment of pediatric infections."( Population pharmacokinetic model for gatifloxacin in pediatric patients.
Blumer, JL; Bradley, JS; Capparelli, EV; Cirincione, B; Grasela, DM; Jacobs, RF; Kearns, GL; Reed, M; Rubino, CM, 2007
)
0.81
" In this study, we aimed to develop a novel pharmacokinetic model to describe NQs-metal cation interactions in order to estimate the optimal dosing interval."( Antacid interaction with new quinolones: dose regimen recommendations based on pharmacokinetic modeling of clinical data for ciprofloxacin, gatifloxacin and norfloxacin and metal cations.
Miyata, K; Ohtani, H; Sawada, Y; Tsujimoto, M, 2007
)
0.54
"Plasma concentration-time profiles of NQs after administration without or with metal cations at various dosing intervals were collected from the literature and analyzed with a pharmacokinetic model incorporating the formation ofNQs-metal cations complex."( Antacid interaction with new quinolones: dose regimen recommendations based on pharmacokinetic modeling of clinical data for ciprofloxacin, gatifloxacin and norfloxacin and metal cations.
Miyata, K; Ohtani, H; Sawada, Y; Tsujimoto, M, 2007
)
0.54
"The developed model can adequately describe the extent of interaction between NQs and metal cations, and should be clinically useful to design dosage regimens to circumvent the interaction."( Antacid interaction with new quinolones: dose regimen recommendations based on pharmacokinetic modeling of clinical data for ciprofloxacin, gatifloxacin and norfloxacin and metal cations.
Miyata, K; Ohtani, H; Sawada, Y; Tsujimoto, M, 2007
)
0.54
" 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
" Pharmacodynamic evaluation by Monte Carlo simulation indicated that approved gatifloxacin dosage regimens appear to be adequate for most pathogens (minimum inhibitory concentration (MIC) ( Evaluation of gatifloxacin pharmacokinetics and pharmacodynamics in severely ill adults in a medical Intensive Care Unit.
Fish, DN, 2007
)
0.93
" The method is successfully used for the estimation of gatifloxacin in a variety of dosage forms, and the results are in good agreement with the label claims."( Development and validation of an ion-pairing RP-HPLC method for the estimation of gatifloxacin in bulk and formulations.
Bende, G; Saha, R; Snehalatha, M; Venugopal, K, 2007
)
0.81
" We then used population pharmacokinetic models for gatifloxacin and simulation to identify dosing regimens with high probabilities of attaining exposures likely to be efficacious in adults and children."( Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
Ambrose, PG; Bhavnani, SM; Craig, WA; Drusano, GL; Forrest, A; Heine, HS; Rubino, CM, 2007
)
0.86
" Improper dosage adjustment based on renal function was not associated with higher rates of hypoglycemia and hyperglycemia for either drug."( Effects of gatifloxacin and levofloxacin on rates of hypoglycemia and hyperglycemia among elderly hospitalized patients.
Graves, J; Lodise, T; Lomaestro, B; Miller, C; Mohr, JF; Smith, RP, 2007
)
0.73
" Rabbits were subsequently dosed with 1 drop, 3 times per day for 4 days with either moxifloxacin, gatifloxacin, or a commercially available irrigating solution."( Corneal wound healing in New Zealand White Rabbits following anterior keratectomy and treatment with moxifloxacin ophthalmic solution 0.5% or gatifloxacin ophthalmic solution 0.3%.
Hiddemen, JW; McCartney, MD; Rice, RL; Shepard, AR; Wax, MB; Williams, KK, 2007
)
0.76
" Multivariate analysis demonstrated that lack of downward dosage adjustment based on creatinine clearance (odds ratio [OR] 10."( Prevalence of and risk factors for dysglycemia in patients receiving gatifloxacin and levofloxacin in an outpatient setting.
LaPlante, KL; Mersfelder, TL; Quilliam, BJ; Ward, KE, 2008
)
0.58
" Lack of downward fluoroquinolone dosage adjustment for renal function, presence of diabetes, and treatment with insulin or sulfonylureas each independently increased the risk of dysglycemia."( Prevalence of and risk factors for dysglycemia in patients receiving gatifloxacin and levofloxacin in an outpatient setting.
LaPlante, KL; Mersfelder, TL; Quilliam, BJ; Ward, KE, 2008
)
0.58
" The proposed methods were successfully applied to the determination of gatifloxacin in pharmaceutical dosage forms without interference from common additives encountered."( Utility of some pi-acceptors for spectrophotometric determination of gatifloxacin in pure form and in pharmaceutical preparations.
Amin, AS; El-Sheikh, R; Gouda, AA, 2008
)
0.81
"To evaluate the ocular surface and aqueous antimicrobial effects of gatifloxacin and moxifloxacin administered in two dosing regimens to patients undergoing phacoemulsification."( Antimicrobial efficacy of prophylactic gatifloxacin 0.3% and moxifloxacin 0.5% in patients undergoing phacoemulsification surgery.
Amico, LM; Bucci, FA; Evans, RE, 2008
)
0.85
"3% at twice-daily dosing of GFLX 100 mg, 97."( [The proper use of quinolones to the elderly patient with community-acquired pneumonia examined by Monte Carlo simulation].
Fukushima, K; Hirakata, Y; Izumikawa, K; Kakeya, H; Kohno, S; Kurihara, S; Miyazaki, Y; Morinaga, Y; Nakamura, S; Seki, M; Tashiro, T; Yamamoto, Y; Yanagihara, K, 2007
)
0.34
" Gatifloxacin tissue penetration was investigated after intravenous dosing of 6 mg/kg to Wistar rats."( Evaluation of gatifloxacin penetration into skeletal muscle and lung by microdialysis in rats.
Bettoni, CC; Dalla Costa, T; Oliveira, LK; Tasso, L, 2008
)
1.62
" Although a 1-hour pretreatment is associated with a reduction in bacterial growth, the combination of 1-day and 1-hour preoperative gatifloxacin dosing results in an even lower overall bacterial load, suggesting that the latter might be the preferred preoperative regimen for eyes undergoing anterior segment surgery."( Comparison of one-day versus one-hour application of topical gatifloxacin in eliminating conjunctival bacterial flora.
Egbert, PR; Kaspar, HM; Liu, YI; Montague, A; Moss, JM; Nguyen, D; Singh, K; Ta, CN, 2008
)
0.79
"A reversed-phase high performance liquid chromatography (HPLC) method was developed, validated, and used for the quantitative determination of gatifloxacin (GA) and ambroxol hydrochloride (AM), from its tablet dosage form."( Simultaneous determination of gatifloxacin and ambroxol hydrochloride from tablet dosage form using reversed-phase high performance liquid chromatography.
Dehghan, MH; Feroz, S; Nanda, R; Nasreen, H; Shahed, M, 2008
)
0.84
"Fluoroquinolone antimicrobials do not affect growth velocity in the ovine model when administered along a dosing regimen that closely models that seen in pediatric medicine."( The effect of fluoroquinolone antibiotics on growing cartilage in the lamb model.
Conway, J; Hutson, P; Leiferman, EM; Noonan, KJ; Sansone, JM; Wilsman, NJ, 2009
)
0.35
" These data suggest that expanded studies in lambs and other species, including humans, with differences in dosing and duration are justified to ultimately demonstrate clinical safety."( The effect of fluoroquinolone antibiotics on growing cartilage in the lamb model.
Conway, J; Hutson, P; Leiferman, EM; Noonan, KJ; Sansone, JM; Wilsman, NJ, 2009
)
0.35
"Improved dosing regimens have been proposed for various antimicrobial agents by application of pharmacokinetic/pharmacodynamic (PK/PD) principles."( Effect of dosing interval on the efficacy of topical ophthalmic gatifloxacin against Enterococcus faecalis in an in vitro pharmacokinetic model simulating the local eye compartment.
Kida, T; Kozai, S; Ohtori, A; Sakaki, H; Tajika, T; Wada, T, 2009
)
0.59
"A selective and simple kinetic spectrophotometric has been developed, for the first time, for the determination of gatifloxacin (GAT) in its dosage forms."( Selective kinetic spectrophotometric method for determination of gatifloxacin based on formation of its N-vinyl chlorobenzoquinone derivative.
Al-Arfaj, HA; Darwish, IA; Sultan, MA, 2010
)
0.81
"3% ophthalmic solution after topical dosing in human eyes."( [Human aqueous humor levels of levofloxacin 0.5%, gatifloxacin 0.3% and levofloxacin 0.3% ophthalmic solution after topical dosing].
Chen, WJ; Huang, XD; Yao, K; Yuan, JQ; Zhang, Z, 2009
)
0.61
" The proposed procedure was applied successfully for the detection of the investigated drugs in their pharmaceutical dosage forms, in spiked plasma, spiked urine, and urine samples, with good precision and accuracy."( Determination of ofloxacin and gatifloxacin by mixed micelle-mediated cloud point extraction-fluorimetry combined methodology.
Du, LM; Wu, H; Zhao, GY, 2010
)
0.65
"3% eye drops administered in two different dosing regimens during phacoemulsification surgery."( Aqueous humour penetration of moxifloxocin and gatifloxacin eye drops in different dosing regimens before phacoemulsification surgery.
Akova, YA; Babaoğlu, MÖ; Bozkurt, A; Çetinkaya, A; Çolak, M; Güngör, SG; Yasar, Ü, 2011
)
0.63
" The penetration of both antibiotics increased significantly when the dosage of the agent was doubled."( Aqueous humour penetration of moxifloxocin and gatifloxacin eye drops in different dosing regimens before phacoemulsification surgery.
Akova, YA; Babaoğlu, MÖ; Bozkurt, A; Çetinkaya, A; Çolak, M; Güngör, SG; Yasar, Ü, 2011
)
0.63
" An in vitro infection model was used to simulate free pulmonary fluctuating concentrations expected after multiple dosing regimens of both drugs in humans or constant multiples of the minimum inhibitory concentration."( Pharmacokinetic/pharmacodynamic modelling of the bactericidal activity of free lung concentrations of levofloxacin and gatifloxacin against Streptococcus pneumoniae.
Dalla Costa, T; de Andrade, C; Tasso, L, 2011
)
0.58
" The optimized microemulsion possessed good stability, showed greater adherence to corneal surface and good permeation of gatifloxacin in the anterior chamber of the eye, resulting in a twofold increase in gatifloxacin concentration than the conventional dosage form."( Delivery of gatifloxacin using microemulsion as vehicle: formulation, evaluation, transcorneal permeation and aqueous humor drug determination.
Aljuffali, IA; Alshamsan, A; Kalam, MA; Mishra, AK; Sultana, Y, 2016
)
1.02
" A pharmacokinetic profile was observed where there is a double peak pattern; a sharp initial increase in the concentration soon after dosing followed by a steady decline until another increase in concentration after a longer period post dosing in all three biological samples was observed."( MALDI MSI and LC-MS/MS: Towards preclinical determination of the neurotoxic potential of fluoroquinolones.
Baijnath, S; Bester, LA; Bratkowska, D; Govender, T; Kruger, HG; Naicker, T; Naiker, S; Shobo, A; Singh, SD; Somboro, AM, 2016
)
0.43
" In contrast, hyperglycemia without QT/QTc prolongations was noted 24 h after dosing in one animal."( Usefulness of simultaneous and sequential monitoring of glucose level and electrocardiogram in monkeys treated with gatifloxacin under conscious and nonrestricted conditions.
Chiba, K; Ishizaka, T; Mori, K; Yoshimatsu, Y, 2018
)
0.69
"A simplified dosing regimen was selected to follow the development of ophthalmic pazufloxacin based on its efficacy and safety profile."( Efficacy and Safety of 0.6% Pazufloxacin Ophthalmic Solution Versus Moxifloxacin 0.5% and Gatifloxacin 0.5% in Subjects with Bacterial Conjunctivitis: A Randomized Clinical Trial.
Baiza-Durán, L; Casillas-Magallanes, M; Gómez-Bastar, PA; González-Lomelí, M; Lizárraga-Corona, A; Mercado-Sesma, AR; Montoya-Sánchez, IM; Mora-González, A; Ochoa-Tabares, JC; Olvera-Montaño, O; Oregon-Miranda, AA; Orozco-Carroll, M; Páez-Garza, JH; Pérez-Balbuena, AL; Sandoval-Delgadillo, LI; Saucedo-Rodríguez, LR; Villanueva-Najera, MA, 2018
)
0.7
" However, based on their pharmacokinetics (PK) and pharmacodynamics (PD), these drugs are also promising for TB meningitis and might perhaps have the potential to shorten pulmonary TB treatment if dosing could be optimized."( The Role of Fluoroquinolones in the Treatment of Tuberculosis in 2019.
Alffenaar, JWC; Kosterink, JGW; Pranger, AD; van der Werf, TS, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antiinfective agentA substance used in the prophylaxis or therapy of infectious diseases.
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitorA topoisomerase inhibitor that inhibits DNA topoisomerase (ATP-hydrolysing), EC 5.99.1.3 (also known as topoisomerase II and as DNA gyrase), which catalyses ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands.
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
[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 (5)

ClassDescription
quinolinemonocarboxylic acidAny aromatic carboxylic acid that contains a quinoline moiety that is substituted by one carboxy substituent.
N-arylpiperazine
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
quinolone
quinolone antibioticAn organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.
[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 (35)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency31.62280.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency64.09190.004023.8416100.0000AID485290; AID489007
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
Chain A, CruzipainTrypanosoma cruziPotency25.11890.002014.677939.8107AID1476
endonuclease IVEscherichia coliPotency1.25890.707912.432431.6228AID2565
thioredoxin reductaseRattus norvegicus (Norway rat)Potency56.23410.100020.879379.4328AID588456
15-lipoxygenase, partialHomo sapiens (human)Potency19.95260.012610.691788.5700AID887
RAR-related orphan receptor gammaMus musculus (house mouse)Potency26.60320.006038.004119,952.5996AID1159521
TDP1 proteinHomo sapiens (human)Potency18.84670.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency9.43920.000714.592883.7951AID1259369
AR proteinHomo sapiens (human)Potency26.83250.000221.22318,912.5098AID743035; AID743063
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency9.43920.003041.611522,387.1992AID1159552
farnesoid X nuclear receptorHomo sapiens (human)Potency29.84700.375827.485161.6524AID743220
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.60320.000229.305416,493.5996AID743079
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.18380.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.81070.354828.065989.1251AID504847
flap endonuclease 1Homo sapiens (human)Potency39.81070.133725.412989.1251AID588795
Cellular tumor antigen p53Homo sapiens (human)Potency0.10590.002319.595674.0614AID651631
[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
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
DNA gyrase subunit AEscherichia coli K-12IC50 (µMol)0.50000.02390.56295.2300AID262137; AID271586
DNA gyrase subunit BEscherichia coli K-12IC50 (µMol)0.50000.00500.43985.2300AID262137; AID271586
DNA topoisomerase 4 subunit AStaphylococcus aureusIC50 (µMol)1.20000.30003.55799.1600AID262138
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50 (µMol)27.13330.01503.477310.0000AID532977; AID532978; AID532979
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)129.11870.00091.901410.0000AID161281; AID243151; AID243188; AID408340; AID420668; AID51930; AID576612; AID755684
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[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)0.66800.06008.9128130.5170AID1902
[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)
DNA gyrase subunit BStaphylococcus aureusCC500.70000.70002.85005.0000AID1626596
DNA topoisomerase 4 subunit BStaphylococcus aureusCC500.20000.20000.30000.4000AID1626595
DNA topoisomerase 4 subunit AStaphylococcus aureusCC500.20000.20000.30000.4000AID1626595
DNA gyrase subunit AStaphylococcus aureusCC5012.23330.70002.85005.0000AID1626596; AID1626598; AID530629
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (201)

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)
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)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
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
hematopoietic progenitor cell differentiationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-alphaHomo sapiens (human)
DNA ligationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA damage responseDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome segregationDNA topoisomerase 2-alphaHomo sapiens (human)
female meiotic nuclear divisionDNA topoisomerase 2-alphaHomo sapiens (human)
apoptotic chromosome condensationDNA topoisomerase 2-alphaHomo sapiens (human)
embryonic cleavageDNA topoisomerase 2-alphaHomo sapiens (human)
regulation of circadian rhythmDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of apoptotic processDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIDNA topoisomerase 2-alphaHomo sapiens (human)
rhythmic processDNA topoisomerase 2-alphaHomo sapiens (human)
negative regulation of DNA duplex unwindingDNA topoisomerase 2-alphaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-alphaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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 (75)

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)
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)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
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
magnesium ion bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
RNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-alphaHomo sapiens (human)
protein kinase C bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP-dependent activity, acting on DNADNA topoisomerase 2-alphaHomo sapiens (human)
DNA binding, bendingDNA topoisomerase 2-alphaHomo sapiens (human)
protein homodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
ubiquitin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein heterodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo 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 (46)

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)
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)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
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
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
nuclear chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
centrioleDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome, centromeric regionDNA topoisomerase 2-alphaHomo sapiens (human)
condensed chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
male germ cell nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
cytoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA topoisomerase 2-alphaHomo sapiens (human)
protein-containing complexDNA topoisomerase 2-alphaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo 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 (1609)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347167Vero cells viability 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.
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.
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.
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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
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.
AID1347168HepG2 cells viability 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.
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.
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.
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.
AID1347149Furin counterscreen 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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347161Confirmatory 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.
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.
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.
AID1508628Confirmatory 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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
AID1347153Confirmatory 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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
AID1347152Confirmatory screen NINDS 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.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID342246Increase in toxin level in epidemic Clostridium difficile BI6-8-17 infected CF1 mouse at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID279293Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID559055Antibacterial activity against Lancefield Streptococcus sp. 'group C' by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID286112Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 67 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID64580Minimum inhibitory concentration against Escherichia coli, strain ES1422003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
AID271587Antibacterial activity against Escherichia coli EC1-102006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID530626Activity at Staphylococcus aureus wild-type DNA topoisomerase 4 subunit ParC2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID285739Antibacterial activity against beta-lactamase positive Moraxella catarrhalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID562828Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0930 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558902Antimicrobial activity against Clostridium difficile CD5b harboring GyrB Ser416Ala mutant gene selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1237407Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
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).
AID342079Effect on growth of epidemic Clostridium difficile BI6-8-17 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID559065Antibacterial activity against Streptococcus mitis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID442254Antimalarial activity against Plasmodium falciparum 3D72009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.
AID342063Antimicrobial activity against nonepidemic Clostridium difficile J29 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1237406Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID559511Antibacterial activity against Lancefield Streptococcus sp. group F assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID580998Renal excretion in healthy human at 400 mg/kg, po administered as single dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID286048Peak free concentration at 200 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID324754Antibacterial activity in Mycobacterium leprae infected mouse foot-pad model assessed as parasite killing after 9 months2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID613792Antibacterial activity against Enterococcus faecalis 08-12 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID542508Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87 and parC R80, V84 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID286115Bactericidal activity against Staphylococcus aureus BSP-2443 with parC S52G, N91D mutation at fAUC/MIC of 51 after 72 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID278253Antimicrobial activity against Salmonella enterica serovar Typhimurium CS3 gyrA+ with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID1391313Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate CCARM 3167 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID425337Antibacterial activity against penicillin-resistant Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1626597Inhibition of FQ-resistant Staphylococcus aureus topoisomerase 4 ParC S80F mutant assessed as compound concentration causing 50% induction of cleavage of covalently closed DNA substrate2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID428986Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 107 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID264952Inhibition of Mycobacterium tuberculosis DNA gyrase2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
Gatifloxacin derivatives: synthesis, antimycobacterial activities, and inhibition of Mycobacterium tuberculosis DNA gyrase.
AID530345Antimicrobial activity against Escherichia coli BicA expressing blaTEM-1, blaCTX-M-15 and qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID244996Minimum inhibitory concentration against Streptococcus pneumoniae ATCC 496192005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID559535Antibacterial activity against Legionella pneumophila assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID563024Antimycobacterial activity against Mycobacterium tuberculosis 08-0745 harboring gyrA Asp89Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID244972Minimum inhibitory concentration against Streptococcus pyogenes ATCC 196152005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1600108Bactericidal activity against Pseudomonas aeruginosa ATCC 9027 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID532978Inhibition of DNA supercoiling activitysof Mycobacterium tuberculosis DNA gyrase subunit A A90V mutant2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID559489Antibacterial activity against Prevotella sp. by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID429010Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT48 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID264951Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
Gatifloxacin derivatives: synthesis, antimycobacterial activities, and inhibition of Mycobacterium tuberculosis DNA gyrase.
AID278268Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS38 with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID429037Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT76 harboring wild type DNA gyrase A assessed as decrease in bacterial population at 4 times MIC after 30 mins by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1240503Antibacterial activity against Pseudomonas aeruginosa DR4877 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID518797Antimycobacterial activity against quinolone-resistant multidrug-resistant Mycobacterium tuberculosis after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID558915Antimicrobial activity against Clostridium difficile CD5i harboring GyrA Ala92Glu and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID613797Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID286045Peak free concentration at 100 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285761Antibacterial activity against Pseudomonas aeruginosa2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID351295Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID278062Suppression of TNF alpha-stimulated IL8 D-170 mutant promoter activity in human PC3 cells at 16 ug/ml dual luciferase reporter assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID285780Antibacterial activity against Prevotella oralis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID518798Antimycobacterial activity against Mycobacterium kansasii after 7 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1330192Antibacterial activity against Pseudomonas aeruginosa 2742 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID244995Minimum inhibitory concentration against Streptococcus agalactiae ATCC 138132005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
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).
AID425545Antibacterial activity against Streptococcus pneumoniae HMC 2527 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID394149Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in spleen at 50 mg/kg, ip administered 10 days postinfection for 10 days measured after 35 days of infection2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids.
AID430966Antibacterial activity against Escherichia coli SKM9 containing gyrA L83, Y87 and parC L80 mutants assessed as increase in MIC by Etest relative to MIC for Escherichia coli 1596 containing gyrA L83 and parC I80 mutants2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID68675In vitro antibacterial activity was tested for Escherichia coli H5601995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID559494Antibacterial activity against Peptostreptococcus sp. assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1626612Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID518801Antimycobacterial activity against Mycobacterium avium serovar 8 after 14 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID342257Effect on growth of fluoroquinolone-susceptible epidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content dosed sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID310323Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
An atom efficient, solvent-free, green synthesis and antimycobacterial evaluation of 2-amino-6-methyl-4-aryl-8-[(E)-arylmethylidene]-5,6,7,8-tetrahydro-4H-pyrano[3,2-c]pyridine-3-carbonitriles.
AID425356Antibacterial activity against Streptococcus pneumoniae HMC 1059 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460N mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559068Antibacterial activity against Streptococcus sanguinis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID271605Antibacterial activity against vancomycin-resistant Enterococcus faecium EF4-34892006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID373141Antimycobacterial activity against Mycobacterium avium complex N084 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID278237Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-2 gyrA+ with ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID285723Antibacterial activity against Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID425576Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 harboring S79Y mutation in quinolone-resistant determining regions of ParC gene after 34 passages with gemifloxacin measured afte2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID530636Antimicrobial activity against Staphylococcus aureus CB370 harboring rifampin-resistant rpoB H481Y mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID559046Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus aureus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID531857Tmax in tuberculosis patient at 400 mg/day, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID425335Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1888648Antibacterial activity against rifampicin resistant Staphylococcus aureus harboring RpoBH481Y mutant assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID456050Inhibition of Staphylococcus aureus wild type DNA gyrase2009Bioorganic & 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.
AID1600104Bactericidal activity against Bacillus subtilis ATCC 6633 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID558907Antimicrobial activity against Clostridium difficile CD5d harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID519204Antibacterial activity against Streptococcus pneumoniae assessed as resistant isolates by microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
In vitro activity of AR-709 against Streptococcus pneumoniae.
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.
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]
AID450458Antibacterial activity against Bacillus subtilis after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID425354Antibacterial activity against Streptococcus pneumoniae HMC 5041 harboring S81F and S79F mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425547Antibacterial activity against Streptococcus pneumoniae HMC 4026 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559204Antibacterial activity against Streptococcus pneumoniae D001 harboring parC Ser79Phe and gyrA Gly85Lys mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID563226Antimycobacterial activity against Mycobacterium tuberculosis 08-0781 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1391317Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID430964Antibacterial activity against Escherichia coli 1596 containing gyrA L83 and parC I80, G84 mutants assessed as increase in MIC by Etest relative to MIC for Escherichia coli 1608 containing gyrA mutant2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID556012Antibacterial activity against Helicobacter pylori harboring gyrA mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID559242Antibacterial activity against Streptococcus pneumoniae S003 harboring wild-type parC and gyrA Ser81Phe mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1237427Bactericidal activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1664938Antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity.
AID759324Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID542518Antimicrobial activity against Escherichia coli ATCC 25922 by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Relationships among ciprofloxacin, gatifloxacin, levofloxacin, and norfloxacin MICs for fluoroquinolone-resistant Escherichia coli clinical isolates.
AID1382069Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID559396Antimicrobial activity against Clostridium difficile 630C selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID318921Antimycobacterial activity against Mycobacterium smegmatis MC2 by agar dilution method2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid.
AID558613Antimicrobial activity against Streptococcus pneumoniae isolate 2686 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1237408Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID563046Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0757 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559537Antibacterial activity against Morganella morganii assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
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).
AID559143Antimicrobial activity against Clostridium difficile A422g harboring GyrA Asp81Asn mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID285738Antibacterial activity against beta-lactamase negative Moraxella catarrhalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID286080fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 200 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID558604Antimicrobial activity against Streptococcus pneumoniae isolate 1055 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID428983Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate CT61 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID285747Antibacterial activity against Klebsiella pneumoniae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID428987Antimicrobial activity against Salmonella enterica Serovar Typhi isolate nar 108 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID405818Antimicrobial activity against Acinetobacter sp. 5248 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID342075Effect on growth of epidemic Clostridium difficile BI6-8-17 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID285783Antibacterial activity against Neisseria meningitidis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID565314Antibacterial activity against Mycoplasma genitalium TW10-6G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID388877Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 10 mg/kg, iv administered as single dose 2 days before bacterial challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID559501Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus aureus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID303468Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected CD1 mouse assessed as lung bacterial count at 50 mg/kg, ip after 35 days post infection2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid.
AID285776Antibacterial activity against Prevotella bivia2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID278047Suppression of PMA-stimulated IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID559049Antibacterial activity against Staphylococcus haemolyticus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559045Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus aureus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558921Antimicrobial activity against Clostridium difficile CD5i harboring GyrA Ala118Ser, Thr82Ala and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID388878Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 10 mg/kg, iv administered as single dose 1 hr before bacterial challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID558630Antimicrobial activity against Streptococcus pneumoniae isolate 4747 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID285338Antimicrobial activity against streptomycin-resistant Escherichia coli J53 transconjugant with qnrA1 producing urinary specimen isolate 13.52 by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
First report of plasmid-mediated qnrA1 in a ciprofloxacin-resistant Escherichia coli strain in Latin America.
AID279286Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79F and gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID559157Antimicrobial activity against Clostridium difficile 630f selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID286047Peak free concentration at 175 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID278252Antimicrobial activity against Salmonella enterica serovar Typhimurium CS3 with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID265977Cytotoxicity against Vero cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID1199292Antimicrobial activity against Staphylococcus aureus ATCC 29213 by broth macrodilution method2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Amino acid modified xanthone derivatives: novel, highly promising membrane-active antimicrobials for multidrug-resistant Gram-positive bacterial infections.
AID324747Antibacterial activity against Mycobacterium leprae at 5 ug/mL after 11 to 18 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID542511Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83,N87,gyrB V456, parC I80 and parE A458 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID542499Antimicrobial activity against Escherichia coli K-12 harboring gyrA A83 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID285766Antibacterial activity against Bacteroides thetaiotaomicron2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID279262Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3665 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID425733Apparent total clearance in mouse at 10 to 100 mg/kg, ip2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID428998Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT144 harboring DNA gyrase A D87G mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID286078fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 150 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID559378Antimicrobial activity against Clostridium difficile A422C selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID698997Antimycobacterial activity against Mycobacterium tuberculosis infected in human assessed as log reduction of bacterial count at 400 mg, qd measured up to 2 days2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID342078Effect on growth of epidemic Clostridium difficile BI9 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID425552Antibacterial activity against penicillin-, macrolide-susceptible and quinolone-resistant Streptococcus pneumoniae HMC 1074 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutat2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID558891Antimicrobial activity against Clostridium difficile C253f selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559060Antibacterial activity against Streptococcus pyogenes by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425543Antibacterial activity against Streptococcus pneumoniae HMC 1156 harboring S81F and S79F mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively showing efflux to ciprofloxacin, gemifloxacin by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID429017Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG7 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559191Antimicrobial activity against Clostridium difficile CD5A harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559066Antibacterial activity against Streptococcus oralis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1488561Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID571172Antimicrobial activity against Clostridium difficile harboring ribotype 027 by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Clostridium difficile infections in a Canadian tertiary care hospital before and during a regional epidemic associated with the BI/NAP1/027 strain.
AID559377Antimicrobial activity against Clostridium difficile A422B selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425349Antibacterial activity against Streptococcus pneumoniae HMC 1076 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559515Antibacterial activity against Streptococcus pyogenes assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558612Antimicrobial activity against Streptococcus pneumoniae isolate 2617 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID279272Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 37 with GyrA S81Y, GyrB E474K and ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID559167Antimicrobial activity against Clostridium difficile BI2a harboring GyrB Arg447Lys mutant gene selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID528514Bactericidal activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus at 8 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID285737Antibacterial activity against Legionella pneumophila2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID286107Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 60 after 24 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285757Antibacterial activity against Shigella sonnei2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID69639Minimum inhibitory concentration against Escherichia coli2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Artificial neural network applied to prediction of fluorquinolone antibacterial activity by topological methods.
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.
AID558913Antimicrobial activity against Clostridium difficile CD5 1-g harboring GyrA Ala92Glu and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID285721Antibacterial activity against penicillin-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID285759Antibacterial activity against Acinetobacter sp.2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
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.
AID518799Antimycobacterial activity against Mycobacterium fortuitum after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID394146Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids.
AID456031Antibacterial activity against Enterococcus faecalis ATCC 19433 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.
AID159910In vitro inhibitory activity against hepatic stages of Plasmodium yoelii yoelii 265 BY; No data2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
AID425770Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA after 46 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID425342Antibacterial activity against Streptococcus pneumoniae HMC 1149 harboring S81F and S79Y mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively showing efflux to ciprofloxacin, gemifloxacin by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID699004Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID285735Antibacterial activity against beta-lactamase negative Haemophilus influenzae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID430963Antibacterial activity against Escherichia coli 1608 containing gyrA L83, L87 mutants assessed as increase in MIC by Etest relative to MIC for wild type Escherichia coli 16092007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID601703Antibacterial activity against 10'4 CFU Staphylococcus aureus ATCC 25923 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1601848Antibacterial activity against Escherichia coli CMCC 44568 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID425725Apparent total clearance in human2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID558629Antimicrobial activity against Streptococcus pneumoniae isolate 3791 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID285771Antibacterial activity against Fusobacterium sp.2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID278244Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-4 with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID279269Antibacterial activity against levofloxacin resistance selected Streptococcus pneumoniae 19 with GyrA S81Y and ParC D83Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID563016Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0810 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID565315Antibacterial activity against Mycoplasma genitalium TW48-5G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID565326Antibacterial activity against Mycoplasma genitalium M6090 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID429009Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT47 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559145Antimicrobial activity against Clostridium difficile A422i harboring GyrA Asp81Asn mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1600099Antibacterial activity against Staphylococcus epidermidis ATCC 14990 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID565327Antibacterial activity against Mycoplasma genitalium M6151 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID429002Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT3 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID433404Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID601791Antibacterial activity against 10'4 CFU Pseudomonas aeruginosa ATCC 27853 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1626615Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y and gyrA S84L mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID285718Antibacterial activity against Streptococcus sanguis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID342255Effect on growth of fluoroquinolone-resistant epidemic Clostridium difficile NAP1 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID286110Bactericidal activity against Staphylococcus aureus ATCC 49619 with S79Y Parc mutation and S81F gyrA mutation at fAUC/MIC of 60 after 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID278264Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS18 with GyrA S38F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID559047Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus epidermidis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID530629Activity at Staphylococcus aureus wild-type GyrA S84L mutant2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID528513Bactericidal activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus at 8 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1600111Antibacterial activity against methicillin resistant Staphylococcus aureus 6347 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID262133Antimicrobial activity against Escherichia coli ATCC 259222006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID293152Antibacterial activity against Streptococcus pneumoniae by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID425553Antibacterial activity against penicillin- and quinolone-susceptible Streptococcus pneumoniae HMC 5055 expressing mefA by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID558884Antimicrobial activity against Clostridium difficile C253b selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1491401Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 7 days by rapid direct susceptibility test
AID759327Antibacterial activity against Staphylococcus aureus KCTC 209 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID325857Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in lungs at 50 mg/kg, ip after 10 days2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
AID425578Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I4602008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID563216Antimycobacterial activity against Mycobacterium tuberculosis 08-0815 harboring gyrA Thr80Ala and Ala90Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID519205Antibacterial activity against Streptococcus pneumoniae by microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
In vitro activity of AR-709 against Streptococcus pneumoniae.
AID559202Antibacterial activity against Streptococcus pneumoniae S003 harboring wild-type parC and gyrA Ser81Phe mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1664939Antimalarial activity against CQ-resistant Plasmodium falciparum NF54-R assessed as inhibition of parasite growth2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity.
AID1264464Antimycobacterial activity against non-replicating streptomycin starved Mycobacterium tuberculosis 18b after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID285732Antibacterial activity against Listeria monocytogenes2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1551290Antibacterial activity against Staphylococcus aureus RN4220 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID559503Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus epidermidis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID456052Selectivity ratio of IC50 for Staphylococcus aureus DNA gyrase Ser84Leu mutant to IC50 for Staphylococcus aureus wild type DNA gyrase2009Bioorganic & 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.
AID425344Antibacterial activity against Streptococcus pneumoniae HMC 1058 harboring S79F, K137N mutation in quinolone-resistant determining regions of ParC gene and 460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID278060Suppression of TNF alpha-stimulated IL8 D-240 mutant promoter activity in human PC3 cells at 16 ug/ml dual luciferase reporter assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID425347Antibacterial activity against Streptococcus pneumoniae HMC 1070 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID69933Antibacterial activity was determined against Escherichia coli NIHJ strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID285734Antibacterial activity against Corynebacterium sp.2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
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).
AID425549Antibacterial activity against Streptococcus pneumoniae HMC 1068 harboring E85K mutation in quinolone-resistant determining regions of GyrA gene, S79Y, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to ciproflox2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID428982Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate CT29 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1067073Antimicrobial activity against Candida albicans 7535 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID559073Antibacterial activity against Citrobacter koseri by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425730Apparent peripheral volume of distribution in mouse at 10 to 100 mg/kg, ip2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID559056Antibacterial activity against Lancefield Streptococcus sp. group F by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID563020Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-0319 harboring gyrA Asp94Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID429015Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG5 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID528510Bactericidal activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus at 4 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID394147Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in lungs at 50 mg/kg, ip administered 10 days postinfection for 10 days measured after 35 days of infection2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids.
AID530347Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M carrying blaCTX-M-15 and pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID601790Antibacterial activity against 10'4 CFU Klebsiella pneumoniae 09-23 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
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.
AID563034Antimycobacterial activity against Mycobacterium tuberculosis 08-0764 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285711Antibacterial activity against Staphylococcus haemolyticus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558890Antimicrobial activity against Clostridium difficile C253e selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1600113Antibacterial activity against methicillin resistant Staphylococcus epidermidis ATCC 13199 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1382075Antibacterial activity against Escherichia coli NCDC 134 after overnight incubation by single disc method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID278246Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-4 acrAB::Kan with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID565308Antibacterial activity against Mycoplasma genitalium by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID279257Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3009 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID285746Antibacterial activity against Klebsiella oxytoca2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1524622Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID601780Antibacterial activity against 10'4 CFU methicillin-sensitive Staphylococcus epidermidis 09-6 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID558587Antimicrobial activity against Streptococcus pneumoniae 19A by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1626618Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y and parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID556015Antibacterial activity against Helicobacter pylori infected in human assessed as bacterial eradication rate at 20 mg, po BID for 7 days2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID1557287Antibacterial activity against Enterococcus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID562824Antimycobacterial activity against Mycobacterium tuberculosis 00-0715 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558614Antimicrobial activity against Streptococcus pneumoniae isolate 2688 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559061Antibacterial activity against Streptococcus anginosus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID405817Antimicrobial activity against Pseudomonas putida 12346 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID698999Tmax in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID342094Increase in toxin level in epidemic Clostridium difficile BI9 infected CF1 mouse at 2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID558581Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID563208Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-0319 harboring gyrA Asp94Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID293153Antibacterial activity against Moraxella catarrhalis by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID285754Antibacterial activity against Salmonella enterica serovar Typhi2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID342254Effect on growth of fluoroquinolone-resistant epidemic Clostridium difficile NAP1 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID559199Antimicrobial activity against Clostridium difficile CD5F harboring GyrB Ser416Ala mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID209612In vitro antibacterial activity was tested for Streptococcus pyogenes C2031995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID425566Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559062Antibacterial activity against Streptococcus bovis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285756Antibacterial activity against Shigella flexneri2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID559198Antimicrobial activity against Clostridium difficile CD5E harboring GyrB Ser416Ala mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID286106Bactericidal activity against Staphylococcus aureus ATCC 49619 with Parc S79Y mutation and gyrA S81F mutation at fAUC/MIC of 35 after 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID298871Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 700802 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID563048Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0790 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558611Antimicrobial activity against Streptococcus pneumoniae isolate 1564 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558625Antimicrobial activity against Streptococcus pneumoniae isolate 3458 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID528496Antimicrobial activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus JCSC 6765 expressing gyrA Ser84Leu, norA T389C and grlA Ser80Phe/Glu84Lys mutants by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID293156Antibacterial activity against Escherichia coli with AcrAB efflux system by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID285728Antibacterial activity against VanA-resistant Enterococcus faecium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1382076Antibacterial activity against Pseudomonas aeruginosa NCDC105 after overnight incubation by single disc method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID433582Selectivity index, ratio of IC50 for Mycobacterium leprae DNA gyrase subunit A A91V mutant to IC50 for Mycobacterium leprae wild type DNA gyrase A2B22008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1237429Bactericidal activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID279202Antibacterial activity against Streptococcus pneumoniae 3009 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID565317Antibacterial activity against Mycoplasma genitalium M2282 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1557280Antibacterial activity against Pseudomonas aeruginosa by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID278261Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS14 gyrA+ with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID565325Antibacterial activity against Mycoplasma genitalium M6328 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID244953Minimum inhibitory concentration against Staphylococcus aureus ATCC 259232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID528507Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 8 times MIC after 120 mins by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1626609Antimicrobial activity against Staphylococcus aureus isogenic forms expressing gyrA S84L and parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID559512Antibacterial activity against Lancefield Streptococcus sp. 'group G' assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425361Antibacterial activity against Streptococcus pneumoniae HMC 1078 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID285765Antibacterial activity against Bacteroides ovatus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558596Antimicrobial activity against Streptococcus pneumoniae 8 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1264492Antimicrobial activity against nonreplicating Mycobacterium tuberculosis 18b by resazurin microtiter assay2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents.
AID528515Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 16 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID530627Activity at Staphylococcus aureus DNA topoisomerase 4 subunit ParC S80F mutant2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1524628Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID565291Antimicrobial activity against Mycoplasma hominis by agar dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activity of a new quinoline derivative, ER-2, against clinical isolates of Mycoplasma pneumoniae and Mycoplasma hominis.
AID528501Antimicrobial activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus JCSC 6770 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID559054Antibacterial activity against Streptococcus agalactiae by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285714Antibacterial activity against Alloiococcus otitidis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID563227Antimycobacterial activity against Mycobacterium tuberculosis 08-0782 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559500Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus aureus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1254067Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID278258Antimicrobial activity against Salmonella enterica serovar Typhimurium CS9 acrAB::Kan with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID558607Antimicrobial activity against Streptococcus pneumoniae isolate 1384 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559197Antimicrobial activity against Clostridium difficile CD5D harboring GyrB Ser416Ala mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID563035Antimycobacterial activity against Mycobacterium tuberculosis 08-0774 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID580860Oral bioavailability in healthy human at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID542515Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, Y87, parC I80 and parE A458 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID601704Antibacterial activity against 10'4 CFU methicillin-sensitive Staphylococcus aureus 08-1 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID279261Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3665 with GyrA S81Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID518803Antimycobacterial activity against Mycobacterium chelonae after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID425069Antimicrobial activity against multidrug-resistant Klebsiella pneumoniae M7943 bearing qnrB10 gene with aac(6)-Ib-cr-blaOXA-30 catB3-arr-3 integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID428977Antimicrobial activity against Salmonella enterica Serovar Typhi isolate D43 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1254079Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID271597Antibacterial activity against Staphylococcus aureus UC-76 SA-12006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID1524624Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID429042Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT144 harboring DNA gyrase A D87G mutation assessed as complete cell killing at 4 times MIC after 6 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID563007Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0785 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285719Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID372992Antimycobacterial activity against Mycobacterium intracellular JATA52-01 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last do2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID372981Antimycobacterial activity against Mycobacterium avium complex N018 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID285748Antibacterial activity against beta-lactamase positive Klebsiella pneumoniae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1551296Antifungal activity against Candida albicans 7535 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1600118Bactericidal activity against Serratia marcescens ATCC 12795 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID559390Antimicrobial activity against Clostridium difficile A422I harboring GyrA Thr82Ile and GyrB Leu451Phe mutant genes selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID285769Antibacterial activity against Fusobacterium nucleatum2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1600116Bactericidal activity against Streptococcus pneumoniae cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID559395Antimicrobial activity against Clostridium difficile 630B selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID278064Decrease in IL8 secretion in human prostatic myofibroblast cells at 16 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID563056Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0810 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1524629Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID429004Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT15 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559401Antimicrobial activity against Clostridium difficile 630E harboring GyrA Ala118Val mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID285778Antibacterial activity against Prevotella corporis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1600101Antibacterial activity against Enterococcus hirae ATCC 1052 cultured in BHI medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID368422Antimicrobial activity against Escherichia coli KAM32 pSTVqepA containing qepA gene ligated to pSTV28 plasmid by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID559490Antibacterial activity against Propionibacterium acnes by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1254073Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1888652Antibacterial activity against Escherichia coli assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID278265Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS18 gyrA+ with GyrA S38F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID298866Antibacterial activity against Staphylococcus aureus ATCC 29213 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID563021Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0172 harboring gyrA Asp94Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID279266Antibacterial activity against azithromycin resistance selected Streptococcus pneumoniae 3243 with L22 insertion 93SFRPRA94 mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID558606Antimicrobial activity against Streptococcus pneumoniae isolate 1147 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1330194Antibacterial activity against methicillin-resistant Staphylococcus aureus 3167 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID530594Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr6 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID1254074Antibacterial activity against Pseudomonas aeruginosa 2004 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID278242Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-3 acrAB::Kan with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID285717Antibacterial activity against Streptococcus bovis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558600Antimicrobial activity against Streptococcus pneumoniae 12 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID530589Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr1 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID563027Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0794 harboring gyrA Thr80Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1601846Antibacterial activity against Bacillus subtilis CMCC 63501 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID559486Antibacterial activity against Clostridium perfringens by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID342077Effect on growth of nonepidemic Clostridium difficile J29 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID613785Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 09-3 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID285716Antibacterial activity against Streptococcus agalactiae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID279236Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 3009 after 14 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID559051Antibacterial activity against Staphylococcus lugdunensis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID342076Effect on growth of nonepidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1330185Antibacterial activity against Staphylococcus aureus 503 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID528502Antimicrobial activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus JCSC 6822 harboring mutation in norA gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1551292Antibacterial activity against Staphylococcus aureus KCTC503 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1237409Antibacterial activity against Pseudomonas aeruginosa 2004 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1600110Bactericidal activity against Proteus vulgaris NCTC 4635 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID558933Antimicrobial activity against Clostridium difficile A422f selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1601853Antibacterial activity against multidrug-resistant Escherichia coli ATCC BAA-196 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID428993Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 51 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1510745Antibacterial activity against methicillin-sensitive Staphylococcus aureus by two fold dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Nitroimidazole-containing compounds and their antibacterial and antitubercular activities.
AID1551295Antibacterial activity against Pseudomonas aeruginosa 2742 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID563039Antimycobacterial activity against Mycobacterium tuberculosis 08-0782 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID372983Antimycobacterial activity against Mycobacterium avium complex after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID207831Minimum inhibitory concentration against Staphylococcus aureus - methicillin resistant Ciprofloxacin sensitive strain MI3002003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
AID559244Antibacterial activity against Streptococcus pneumoniae D001 harboring parC Ser79Phe and gyrA Gly85Lys mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID405457Antibacterial activity against Escherichia coli C600Rif in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID559078Antibacterial activity against Klebsiella oxytoca by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID563030Antimycobacterial activity against Mycobacterium tuberculosis 08-0769 harboring gyrA putative promoter mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID372982Antimycobacterial activity against Mycobacterium avium complex N084 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID558601Antimicrobial activity against Streptococcus pneumoniae isolate 24 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID342062Antimicrobial activity against nonepidemic Clostridium difficile ATCC 9689 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID245029Minimum inhibitory concentration against Staphylococcus haemolyticus ATCC 299702005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1600097Antibacterial activity against methicillin resistant Staphylococcus aureus N315 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID565290Antimicrobial activity against Mycoplasma pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activity of a new quinoline derivative, ER-2, against clinical isolates of Mycoplasma pneumoniae and Mycoplasma hominis.
AID601789Antibacterial activity against 10'4 CFU Klebsiella pneumoniae 09-22 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID372980Antimycobacterial activity against Mycobacterium avium complex N016 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1557279Antibacterial activity against Escherichia coli by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1237411Antifungal activity against Candida albicans 7535 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID542512Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, Y87 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID558602Antimicrobial activity against Streptococcus pneumoniae isolate 33 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1600136Resistance index, ratio of MIC for Proteus vulgaris NCTC 4635 measured after 5 dilution steps to MIC for Proteus vulgaris NCTC 4635 measured after 48 hrs incubation by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID405454Antibacterial activity against Escherichia coli C600Rif by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID580865Plasma protein binding in healthy human at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID285729Antibacterial activity against VanB-resistant Enterococcus faecium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID456033Antibacterial activity against Klebsiella pneumoniae type 2 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.
AID559414Antimicrobial activity against Clostridium difficile BI2F harboring GyrB Glu466Lys mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID279254Antibacterial activity against levofloxacin resistance selected Streptococcus pneumoniae 3009 with GyrA S81Y and ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID563218Antimycobacterial activity against Mycobacterium tuberculosis 08-0769 harboring gyrA putative promoter mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID699001Bioavailability in human2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1237422Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1600109Antibacterial activity against Proteus vulgaris NCTC 4635 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID279280Antimicrobial activity against Streptococcus pneumoniae R6 transformants with gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID528506Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 4 times MIC after 120 mins by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1240502Antibacterial activity against Pseudomonas aeruginosa DR5790 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID372985Antimycobacterial activity against Mycobacterium avium JATA51-01 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID207483Antibacterial activity was determined against Staphylococcus aureus FDA 209-P strain after incubation at 37 degrees C for 18 h2003Journal 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.
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.
AID322982Antimicrobial activity against macrolide-susceptible Mycoplasma pneumoniae FH2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
AID559238Antibacterial activity against Streptococcus pneumoniae W001 harboring wild-type parC and gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID613791Antibacterial activity against Enterococcus faecalis 08-10 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID405459Antibacterial activity against Escherichia coli C600Rif containing pIP1206 plasmid in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1483976Ratio of MIC for Staphylococcus aureus ATCC 29213 after and before 15 serial passages2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Symmetrically Substituted Xanthone Amphiphiles Combat Gram-Positive Bacterial Resistance with Enhanced Membrane Selectivity.
AID456047Inhibition of Staphylococcus aureus wild type DNA topoisomerase 42009Bioorganic & 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.
AID278269Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS38 gyrA+ with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID1491403Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID394145Antibacterial activity against Mycobacterium smegmatis ATCC 14468 by agar dilution method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids.
AID429008Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT42 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID285770Antibacterial activity against Fusobacterium necrophorum2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID285727Antibacterial activity against Enterococcus faecium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID429014Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG3 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID278271Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS38 tolC::Kan with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID1240498Antibacterial activity against Pseudomonas aeruginosa DM4150R after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID1626599Inhibition of human DNA topoisomerase 2-alpha assessed as compound concentration causing 50% induction of cleavage of covalently closed DNA substrate2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID559510Antibacterial activity against Lancefield Streptococcus sp. 'group C' assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID530628Activity at Staphylococcus aureus wild-type GyrA2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID559487Antibacterial activity against Fusobacterium sp. by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558901Antimicrobial activity against Clostridium difficile CD5a harboring GyrB Ser416Ala mutant gene selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID433402Inhibition of Mycobacterium leprae DNA gyrase subunit A A91V mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID558619Antimicrobial activity against Streptococcus pneumoniae isolate 3275 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID285740Antibacterial activity against Neisseria gonorrhoeae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558903Antimicrobial activity against Clostridium difficile CD5c harboring GyrB Ser416Ala mutant gene selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1601854Antibacterial activity against multidrug-resistant Pseudomonas aeruginosa ATCC BAA-2111 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID213599Clonogenic cytotoxicity against Chinese hamster V-79 cells1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID1557288Antibacterial activity against Clostridium perfringens by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID613800Antibacterial activity against Pseudomonas aeruginosa 09-34 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID1626604Antimicrobial activity against wild type Staphylococcus aureus2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID559520Antibacterial activity against Streptococcus mitis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID584113Ratio of LD99 for Escherichia coli K-12 DM4100 to MIC for Escherichia coli K-12 DM41002010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID278249Antimicrobial activity against Salmonella enterica serovar Typhimurium CS1 gyrA+ with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID571174Antimicrobial activity against Clostridium difficile harboring other ribotypes by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Clostridium difficile infections in a Canadian tertiary care hospital before and during a regional epidemic associated with the BI/NAP1/027 strain.
AID558582Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID429022Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG152 harboring DNA gyrase A S83F and D87G mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
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.
AID286044Susceptibility of Streptococcus pneumoniae BSP-2443 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285733Antibacterial activity against Corynebacterium jeikeium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
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.
AID559509Antibacterial activity against Streptococcus agalactiae assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1524627Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID411949Antitubercular activity against Mycobacterium tuberculosis H37Rv after 14 days by turbidimetric assay2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Peptide deformylase inhibitors of Mycobacterium tuberculosis: synthesis, structural investigations, and biological results.
AID558595Antimicrobial activity against Streptococcus pneumoniae 7 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID342074Effect on growth of epidemic Clostridium difficile BI9 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID265986Activity against Mycobacterium tuberculosis H37Rv infected in CD1 mouse assessed as decrease in bacterial load relative to control in spleen at 50 mg/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID244988Minimum inhibitory concentration against Streptococcus pneumoniae ATCC 63032005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID285720Antibacterial activity against penicillin-intermediate resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID559536Antibacterial activity against Moraxella catarrhalis assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID613799Antibacterial activity against Pseudomonas aeruginosa 09-33 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID278041Cytotoxicity against human PC3 cells at 16 ug/ml relative to control2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1524626Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID425341Antibacterial activity against quinolone-resistant Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425546Antibacterial activity against Streptococcus pneumoniae HMC 2536 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID520108Antimicrobial activity against Mycobacterium tuberculosis H37Rv at assessed as growth inhibition at 10 mg/kg following 24 days oxygen depletion by Wayne method relative to control2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID1551299Antibacterial activity against Quinolone-resistant Staphylococcus aureus CCARM 3505 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID405819Antimicrobial activity against Acinetobacter sp. 5227 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID518796Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID565319Antibacterial activity against Mycoplasma genitalium M2321 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1382077Antibacterial activity against Paenibacillus polymyxa NCDC 64 after overnight incubation by single disc method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID1557304AUC in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID698998AUC in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1601845Antibacterial activity against Enterococcus faecalis CMCC 29212 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID559050Antibacterial activity against Staphylococcus hominis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID279285Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79F and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID559063Antibacterial activity against Streptococcus constellatus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1915654Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 72 hrs by two-fold dilution method2021European journal of medicinal chemistry, Jan-15, Volume: 210An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
AID160372In vitro antibacterial activity was tested for Propion acnes PA5-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID278045Reduction of peptidoglycan-stimulated IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID520615Antimicrobial activity against Nocardia brasiliensis HUJEG-1 infected in BALB/c mouse assessed as decrease in number of lesions on foot-pad at 100 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.
AID286079fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 175 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID534771Antimicrobial activity against Acinetobacter baumannii-calcoaceticus obtained from war-wounded patient assessed as susceptible isolates2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
AID390113Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 20 mg/kg, iv administered as single dose 2 days before bacterial challenge2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.
AID428990Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 45 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559064Antibacterial activity against Streptococcus intermedius by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1237410Antibacterial activity against Salmonella typhimurium 2421 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID286062Half life at 200 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285785Antibacterial activity against Streptococcus mitis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558583Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID528503Bactericidal activity against methicillin-resistant Staphylococcus aureus at 4 times MIC upto 60 mins by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID563009Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0791 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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).
AID559506Antibacterial activity against Staphylococcus lugdunensis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425551Antibacterial activity against penicillin-, macrolide- and quinolone-susceptible Streptococcus pneumoniae HMC 63 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID318925Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in spleen at 50 mg/kg, ip after 10 days2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid.
AID558617Antimicrobial activity against Streptococcus pneumoniae isolate 3260 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID563209Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0172 harboring gyrA Asp94Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID279264Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3676 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID430967Antibacterial activity against Escherichia coli SKM18 containing gyrA L83, Y87 and parC L80, G84 mutants assessed as increase in MIC by Etest relative to MIC for Escherichia coli SKM9 containing gyrA L83, Y87 and parC L80 mutants2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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.
AID613796Antibacterial activity against Klebsiella pneumoniae 09-22 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID558592Antimicrobial activity against Streptococcus pneumoniae 4 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID601784Antibacterial activity against 10'4 CFU Enterococcus faecalis 08-12 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1551297Antibacterial activity against Methicillin-resistant Staphylococcus aureus CCARM 3167 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID559048Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus epidermidis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID518802Antimycobacterial activity against Mycobacterium intracellular serovar 16 after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID278059Suppression of TNF alpha-stimulated IL8 D-145 mutant promoter activity in human PC3 cells at 16 ug/ml by dual luciferase reporter assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID699000Half life in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID558597Antimicrobial activity against Streptococcus pneumoniae 9 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1600095Antibacterial activity against Staphylococcus aureus ATCC 6538 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1240499Antibacterial activity against Pseudomonas aeruginosa DM23257 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID559205Antibacterial activity against Streptococcus pneumoniae D002 harboring parC Ser79Phe and gyrA Ser81Phe mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID556010Antibacterial activity against Helicobacter pylori harboring gyrA mutant gene2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID1916429Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 in C57BL/6 mouse model of bacterial keratitis assessed as log reduction in viable bacterial count in infected cornea at 0.3 % pre-infected with bacteria for 24 hrs followed by topical adminis
AID1488559Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by two fold dilution method
AID565318Antibacterial activity against Mycoplasma genitalium M2300 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID559485Antibacterial activity against Bacteroides fragilis by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285749Antibacterial activity against Morganella morganii2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558931Antimicrobial activity against Clostridium difficile A422d selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID563222Antimycobacterial activity against Mycobacterium tuberculosis 08-0764 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID318924Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in lung at 50 mg/kg, ip after 10 days2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid.
AID428980Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate A102 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID285750Antibacterial activity against Proteus mirabilis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID342243Increase in toxin level in nonepidemic Clostridium difficile ATCC 9689 infected in CF1 mouse at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID429001Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT2 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1557283Antibacterial activity against Haemophilus influenzae with horse blood by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID530588Antimicrobial activity against Escherichia coli TOP10 by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID298861Antibacterial activity against Enterococcus faecalis ATCC 29212 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID563028Antimycobacterial activity against Mycobacterium tuberculosis 08-0815 harboring gyrA Thr80Ala and Ala90Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID528505Bactericidal activity against methicillin-resistant Staphylococcus aureus at 16 times MIC upto 60 mins by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID565329Antibacterial activity against Mycoplasma genitalium M6283 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1264494Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis by resazurin microtiter assay2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents.
AID285743Antibacterial activity against Enterobacter aerogenes2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID293154Antibacterial activity against Haemophilus influenzae by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID285768Antibacterial activity against Clostridium perfringens2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID373140Antimycobacterial activity against Mycobacterium avium complex N084 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID157244In vitro antibacterial activity was tested for Pepto asac PA 3-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID41263In vitro antibacterial activity against Bacteroides fragilis BFA1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID532979Inhibition of DNA supercoiling activity of Mycobacterium tuberculosis DNA gyrase subunit A D94G mutant2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
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).
AID278245Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-4 gyrA+ with ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID285755Antibacterial activity against Shigella dysenteriae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1557285Antibacterial activity against Streptococcus pneumoniae by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1626607Antimicrobial activity against Staphylococcus aureus isogenic forms expressing parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID405298Antimicrobial activity against Leptospira interrogans serovar Portlandvere infected golden Syrian hamster model of acute lethal leptospirosis assessed as survival at 25 mg/kg/day, ip once daily for 5 days administered 2 day after infection2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of fluoroquinolones against Leptospira interrogans in a hamster model.
AID528497Antimicrobial activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus JCSC 6766 expressing gyrA Glu84Lys and grlA Ser80Phe mutants by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID278057Inhibition of TNF alpha-stimulated IL8 mRNA expression in human PC3 cells at 16 ug/ml after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID303466Antimycobacterial activity against multi-drug-resistant Mycobacterium tuberculosis by agar dilution method2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid.
AID613798Antibacterial activity against Pseudomonas aeruginosa 09-32 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID286077fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 100 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
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.
AID278267Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS18 tolC::Kan with GyrA S38F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID298863Antibacterial activity against Klebsiella pneumoniae ATCC 10031 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID559156Antimicrobial activity against Clostridium difficile 630e selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
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]
AID279267Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3243 with 23S rRNA A2059T mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID559239Antibacterial activity against Streptococcus pneumoniae W002 harboring wild-type parC and gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID310322Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
An atom efficient, solvent-free, green synthesis and antimycobacterial evaluation of 2-amino-6-methyl-4-aryl-8-[(E)-arylmethylidene]-5,6,7,8-tetrahydro-4H-pyrano[3,2-c]pyridine-3-carbonitriles.
AID1067080Antimicrobial activity against Streptococcus mutans 3065 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID341089Antimicrobial activity against Clostridium difficile clinical isolates by agar dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro activities of 15 antimicrobial agents against 110 toxigenic clostridium difficile clinical isolates collected from 1983 to 2004.
AID351292Antibacterial activity against Bacillus subtilis ATCC 6051 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID271589Antibacterial activity against Klebsiella pneumonia ESBL KP37292006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID425340Antibacterial activity against quinolone-susceptible Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID298869Antibacterial activity against linezolid-resistant Staphylococcus aureus NRS 119 by microbroth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID559052Antibacterial activity against Staphylococcus saprophyticus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558618Antimicrobial activity against Streptococcus pneumoniae isolate 3263 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID699003Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID558919Antimicrobial activity against Clostridium difficile CD5 2-g harboring GyrA Ala118Ser, Thr82Ala and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559081Antibacterial activity against Moraxella catarrhalis by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID601782Antibacterial activity against 10'4 CFU Streptococcus pneumoniae 08-4 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID542519Antimicrobial activity against fluoroquinolone-sensitive Escherichia coli clinical isolate by Etest2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Relationships among ciprofloxacin, gatifloxacin, levofloxacin, and norfloxacin MICs for fluoroquinolone-resistant Escherichia coli clinical isolates.
AID1888649Antibacterial activity against wild type Staphylococcus aureus assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID559382Antimicrobial activity against Clostridium difficile A422D harboring GyrB Leu451Phe mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID245697Mutant prevention concentration aganist methicillin resistant Staphylococcus aureus-5023 done for 48 hr at 37 degree C with compound2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID584111Bacteriostatic activity against Escherichia coli K-12 DM41002010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID613822Antibacterial activity against Klebsiella pneumoniae 09-23 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID165206In vitro antibacterial activity was tested for Pseudomonas aeruginosa UI-181995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID429026Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG182 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID498191Antibacterial activity against Stenotrophomonas maltophilia MBS101 containing plasmid encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID279265Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3243 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
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).
AID425579Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I462008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID68676In vitro antibacterial activity was tested for Escherichia coli Vogel1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID285782Antibacterial activity against Propionibacterium acnes2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID559067Antibacterial activity against Streptococcus salivarius by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285764Antibacterial activity against Bacteroides fragilis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID559168Antimicrobial activity against Clostridium difficile BI2b harboring GyrB Arg447Lys mutant gene selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID556011Antibacterial activity against Helicobacter pylori harboring gyrA mutant gene assessed as resistant isolates2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID425336Antibacterial activity against penicillin-intermediate Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1557286Antibacterial activity against Streptococcus pyogenes by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID285730Antibacterial activity against Enterococcus casseliflavus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID528516Bactericidal activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus at 16 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1254075Antibacterial activity against Salmonella typhimurium 2421 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID303467Antimicrobial activity against Mycobacterium smegmatis by agar dilution method2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid.
AID293151Antibacterial activity against Enterococcus faecalis by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID318920Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid.
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).
AID425575Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene after 22 passages with moxifloxacin measured afte2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID285760Antibacterial activity against Burkholderia cepacia2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID285741Antibacterial activity against Citrobacter diversus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID285722Antibacterial activity against levofloxacin-resistant Streptococcus pneumoniae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID559080Antibacterial activity against Legionella pneumophila by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID450459Antibacterial activity against Serratia marcescens after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID342067Antimicrobial activity against fluoroquinolone-susceptible nonepidemic Clostridium difficile strain6 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID563217Antimycobacterial activity against Mycobacterium tuberculosis 08-0773 harboring gyrA Pro8Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558932Antimicrobial activity against Clostridium difficile A422e selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559161Antimicrobial activity against Clostridium difficile 630g harboring GyrB Asp26Val mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID558889Antimicrobial activity against Clostridium difficile C253d selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1557281Antibacterial activity against Klebsiella by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID285706Antibacterial activity against oxacillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID368419Antimicrobial activity against Escherichia coli KAM32 expressing deltaacrB ydhE hsd gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID429038Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate HTD 798 harboring DNA gyrase A S83F mutation assessed as decrease in bacterial population at 4 times MIC after 30 mins by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID285744Antibacterial activity against Enterobacter cloacae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID563044Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-1647 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1330188Antibacterial activity against Streptococcus mutans 3065 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID285337Antimicrobial activity against Escherichia coli qnrA1 producing urinary specimen isolate 13.52 by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
First report of plasmid-mediated qnrA1 in a ciprofloxacin-resistant Escherichia coli strain in Latin America.
AID425577Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I4602008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1888651Antibacterial activity against Staphylococcus aureus harboring RpoBH481Y/ParCS80F/GyrAS84L triple mutant assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID278238Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-2 acrAB::Kan with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID558920Antimicrobial activity against Clostridium difficile CD5h harboring GyrA Ala118Ser, Thr82Ala and GyrB Ser416Ala mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425070Antimicrobial activity against multidrug-resistant Escherichia coli M7943-TC2 bearing qnrB10 gene with aac(6)-Ib-cr-blaOXA-30 catB3-arr-3 integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID285762Antibacterial activity against Stenotrophomonas maltophilia2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID279268Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 19 with GyrA S81F mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID405466Antibacterial activity against Escherichia coli TOP10 containing pIP1206 plasmid in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1254077Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
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.
AID561399Antibacterial activity against quinolone-susceptible Bordetella pertussis BP117 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID445446Oral bioavailability in human2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
AID285777Antibacterial activity against Prevotella buccae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1237403Antibacterial activity against Staphylococcus aureus KCTC 209 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID285745Antibacterial activity against Escherichia coli2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID456051Inhibition of Staphylococcus aureus DNA gyrase Ser84Leu mutant2009Bioorganic & 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.
AID559203Antibacterial activity against Streptococcus pneumoniae S004 harboring wild-type parC and gyrA Gly85Asn mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID429030Antimicrobial activity against Salmonella enterica Serovar Typhi isolate BL 21801 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID298858Antibacterial activity against Bacillus subtilis ATCC 6633 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID208294Minimum inhibitory concentration against Streptococcus pneumoniae - penicillin sensitive, strain STP642003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
AID285736Antibacterial activity against beta-lactamase positive Haemophilus influenzae2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID528509Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 4 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID279282Antimicrobial activity against Streptococcus pneumoniae R6 transformants with gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID342242Increase in toxin level in epidemic Clostridium difficile BI6-8-17 infected CF1 mouse at 1.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID278039Cytotoxicity against human PC3 cells at 2 ug/ml relative to control2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID425358Antibacterial activity against Streptococcus pneumoniae HMC 1072 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID278247Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-4 tolC::Kan with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID318919Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid.
AID542506Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87, parC I80 and parE A548 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID450461Antibacterial activity against Escherichia coli after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID558610Antimicrobial activity against Streptococcus pneumoniae isolate 1424 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID565309Antibacterial activity against Mycoplasma genitalium by quantitative TaqMan PCR method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID342066Antimicrobial activity against fluoroquinolone-resistant epidemic Clostridium difficile NAP1 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID563023Antimycobacterial activity against Mycobacterium tuberculosis 08-0787 harboring gyrA Asp94His mutant gene and deletion of codons 678 and 679 in gyrB mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID278236Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-2 with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID556014Antibacterial activity against Helicobacter pylori infected in human assessed as bacterial eradication rate at 1 g, po BID for 7 days2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID565311Antibacterial activity against Mycoplasma genitalium M30 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID561388Antibacterial activity against quinolone-susceptible Bordetella pertussis CCUG 30837 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
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.
AID322984Antimicrobial activity against macrolide-susceptible Mycoplasma pneumoniae M1292007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
AID342096Increase in toxin level in nonepidemic Clostridium difficile ATCC 9689 infected in CF1 mouse at 1.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID262137Inhibitory activity against wild type Escherichia coli gyrase2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID518804Antimycobacterial activity against Mycobacterium abscessus after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1237425Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID565331Antibacterial activity against Mycoplasma genitalium M6287 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1551300Antibacterial activity against Quinolone-resistant Staphylococcus aureus CCARM 3519 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID558896Antimicrobial activity against Clostridium difficile C253h harboring GyrA Ala118Ser mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559519Antibacterial activity against Streptococcus intermedius assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559384Antimicrobial activity against Clostridium difficile A422F harboring GyrB Leu451Phe mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559174Antimicrobial activity against Clostridium difficile BI2e harboring GyrB Arg447Lys and Asp426Asn mutant gene selected after 32 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID613793Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID278051Suppression IL8 secretion in human PC3 cells at 16 ug/ml added simultaneously with TNF alpha2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID559187Antimicrobial activity against Clostridium difficile C253F selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
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.
AID271593Antibacterial activity against Escherichia coli EC25492006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID530633Antimicrobial activity against Staphylococcus aureus CB811 harboring quinolone-resistant gyrA S84L mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID733004Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB G89C mutant-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID279292Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N and gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID405460Antibacterial activity against Escherichia coli C600Rif containing pIP1206 plasmid in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID542510Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87, parC I80, K84 and parE D460 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID285800Antimicrobial activity against Bacteroides distasonis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID559517Antibacterial activity against Streptococcus bovis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285731Antibacterial activity against Enterococcus gallinarum2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID563008Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0790 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID584112Bactericidal activity against Escherichia coli K-12 DM4100 after 2 hrs in presence of protein synthesis inhibitor chloramphenicol treated 10 mins before compound challenge2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID428996Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate CT118 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1601842Antibacterial activity against Staphylococcus aureus CMCC 25923 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID559400Antimicrobial activity against Clostridium difficile 630D harboring GyrA Ala118Val mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425581Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring I460V mutation in QRDR of ParE gene after 41 passages with gemifloxacin measured after 10 daily antibiotic-free s2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID368423Antimicrobial activity against Escherichia coli KAM32 pSTVdeltaqepA containing disrupted qepA gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID1600102Bactericidal activity against Enterococcus hirae ATCC 1052 cultured in BHI medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1626602Antimicrobial activity against Staphylococcus aureus isogenic forms expressing gyrA S84L mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID556017Antibacterial activity against Helicobacter pylori harboring gyrA mutant gene infected in human assessed as bacterial eradication rate after 7 days2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID1570241Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID429016Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG6 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID601785Antibacterial activity against 10'4 CFU Enterococcus faecium 08-2 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID278256Antimicrobial activity against Salmonella enterica serovar Typhimurium CS9 with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID559155Antimicrobial activity against Clostridium difficile 630d selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID249970Ratio of MPC to MIC against methicillin resistant Staphylococcus aureus-50232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID528519Bactericidal activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus at 2048 ug/ml after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID561397Antibacterial activity against quinolone-susceptible Bordetella pertussis BP58 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID425350Antibacterial activity against Streptococcus pneumoniae HMC 1146 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, and D435N mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID428988Antimicrobial activity against Salmonella enterica Serovar Typhi isolate ipt 2 harboring DNA gyrase A D87G mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1585704Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis after 3 to 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID563026Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2834 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID571173Antimicrobial activity against Clostridium difficile harboring ribotype 001 by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Clostridium difficile infections in a Canadian tertiary care hospital before and during a regional epidemic associated with the BI/NAP1/027 strain.
AID542502Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID279263Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3676 with GyrA E85G, GyrB S478I and ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID563019Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2399 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558622Antimicrobial activity against Streptococcus pneumoniae isolate 3374 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID249968Ratio of MPC to MIC aganist methicillin resistant Staphylococcus aureus-322005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
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.
AID368424Ratio of MIC for Escherichia coli KAM32 pSTVqepA mutant to MIC for Escherichia coli KAM32 pSTV28 mutant2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID325858Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse assessed as bacterial load in spleen at 50 mg/kg, ip after 10 days2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
AID285715Antibacterial activity against Streptococcus pyogenes2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID318922Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Antimycobacterial activities of novel 2-(sub)-3-fluoro/nitro-5,12-dihydro-5-oxobenzothiazolo[3,2-a]quinoline-6-carboxylic acid.
AID428985Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 104 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID278233Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-1 gyrA+2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID285752Antibacterial activity against Salmonella enterica serovar Paratyphi2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID580863Tmax in patients with pulmonary tuberculosis at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID425559Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559057Antibacterial activity against Lancefield Streptococcus sp. 'group G' by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1240500Antibacterial activity against Pseudomonas aeruginosa DM23376 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID298865Antibacterial activity against Staphylococcus aureus ATCC 25923 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID237457Partition coefficient (logD2.0)2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID613787Antibacterial activity against Streptococcus pneumoniae 08-2 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID368418Antimicrobial activity against multidrug-resistant Escherichia coli C316 pHPA containing mutated GyrA gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
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.
AID1237405Antibacterial activity against Streptococcus mutans 3065 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID559408Antimicrobial activity against Clostridium difficile BI2C selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID210029Antibacterial activity was determined against Streptococcus pneumoniae J-24 strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID342256Effect on growth of fluoroquinolone-resistant epidemic Clostridium difficile NAP1 in CF1 mouse assessed as increase in bacterial density in cecal content at 2.0 mg/day, sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1524623Antibacterial activity against Streptococcus mutans 3289 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1626596Inhibition of wild type Staphylococcus aureus gyrase assessed as compound concentration causing 50% induction of cleavage of covalently closed DNA substrate2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID286060Half life at 100 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1557305Half life in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID285786Antibacterial activity against Streptococcus viridans2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID405465Antibacterial activity against Escherichia coli TOP10 containing pIP1206 plasmid in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1600096Bactericidal activity against Staphylococcus aureus ATCC 6538 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID278259Antimicrobial activity against Salmonella enterica serovar Typhimurium CS9 tolC::Kan with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID286049Peak free concentration at 400 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID498192Antibacterial activity against Stenotrophomonas maltophilia MBS100 deficient in Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID209232In vitro antibacterial activity was tested for Streptococcus faecalis MGH-21995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID278234Antimicrobial activity against Salmonella enterica serovar Typhimurium GyrA S21-1 acrAB::Kan with GyrA S83F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID438298Inhibition of penicillin-resistant Streptococcus pneumoniae 5204 PBP2X preincubated for 4 hrs before addition of substrate (R)-[2-(benzoylamino)propionylsulfanyl]acetic acid2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening.
AID278043Decrease in IL8 secretion in human PC3 cells at 4 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID558926Antimicrobial activity against Clostridium difficile A422b selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1605844Antibacterial activity against vancomycin-resistant Enterococcus faecalis 1010 assessed as reduction in bacterial growth measured after 24 hrs by broth microdilution method2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
AID1254071Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1601841Antibacterial activity against Staphylococcus aureus CMCC(B) 26003 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID293148Antibacterial activity against quinoline-susceptible methicillin-resistant Staphylococcus aureus by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID563214Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2834 by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425564Antibacterial activity against quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 5048 expressing mefA after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID285712Antibacterial activity against Staphylococcus saprophyticus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID286081fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 400 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID206764In vitro antibacterial activity was tested for Staphylococcus aureus H2281995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID1254078Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID456032Antibacterial activity against Escherichia coli NIHJ 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.
AID561402Antibacterial activity against quinolone-susceptible Bordetella pertussis BP122 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID278257Antimicrobial activity against Salmonella enterica serovar Typhimurium CS9 gyrA+ with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
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.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
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).
AID285725Antibacterial activity against VanB-resistant Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID389912Antibacterial activity against Staphylococcus aureus ATCC 13709 after 24 hrs by microdilution method2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.
AID558605Antimicrobial activity against Streptococcus pneumoniae isolate 1146 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
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.
AID542509Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87, gyrB T471 and parC I80, G84 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID1557303Cmax in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID559528Antibacterial activity against Citrobacter koseri assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID521103Antimicrobial activity against Streptococcus sp. 'group B' isolate 1 harboring gyrA Glu85Lys mutant, parC Ser79Tyr mutant and parE Ileu495Leu mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
AID1605840Ratio of MIC for vancomycin-resistant Enterococcus faecalis 1010 to MIC for Mel-5-resistant vancomycin-resistant Enterococcus faecalis 1010 incubated for 24 hrs by broth microdilution method2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
AID271598Antibacterial activity against Staphylococcus aureus SA25522006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID271595Antibacterial activity against Moraxella catarrhalis BC-35312006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID1240497Antibacterial activity against Pseudomonas aeruginosa DR18531 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID209591Antibacterial activity was determined against Streptococcus mitis IID685 strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID562826Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2934 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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.
AID303464Cytotoxicity against Vero cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid.
AID278270Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS38 acrAB::Kan with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID286108Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 60 after 48 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID561398Antibacterial activity against quinolone-susceptible Bordetella pertussis BP99 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID351293Antibacterial activity against Enterococcus faecalis NCTC 6013 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID372996Antimycobacterial activity against Mycobacterium avium complex N016 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID559082Antibacterial activity against Morganella morganii by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID528508Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 16 times MIC after 120 mins by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID565316Antibacterial activity against Mycoplasma genitalium UTMB-10G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID425339Antibacterial activity against azithromycin-resistant Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID565328Antibacterial activity against Mycoplasma genitalium M6282 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID559185Antimicrobial activity against Clostridium difficile C253D selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1510743Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis by two fold dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Nitroimidazole-containing compounds and their antibacterial and antitubercular activities.
AID425352Antibacterial activity against Streptococcus pneumoniae HMC 1150 harboring S81C mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1237414Bactericidal activity against Staphylococcus aureus KCTC 503 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID561391Antibacterial activity against quinolone-susceptible Bordetella pertussis BP109 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID563036Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0777 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1330187Antibacterial activity against Staphylococcus aureus 209 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID565324Antibacterial activity against Mycoplasma genitalium M6286 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID298862Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID429025Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG176 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID425338Antibacterial activity against azithromycin-susceptible Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID733006Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose gel electro2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID286105Bactericidal activity against Staphylococcus aureus ATCC 49619 with Parc S79Y mutation and gyrA S81F mutation at fAUC/MIC of 35 after 72 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID563057Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0821 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425072Antimicrobial activity against Escherichia coli DH10B expressing pCRQB10 in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID433583Selectivity index, ratio of CC25 for Mycobacterium leprae DNA gyrase subunit A A91V mutant to CC25 for Mycobacterium leprae wild type DNA gyrase A2B2 by DNA cleavage assay2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID425351Antibacterial activity against Streptococcus pneumoniae HMC 1147 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to gemifloxacin by 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID565312Antibacterial activity against Mycoplasma genitalium R32 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID286161Effect on efflux-mediatated resistance of Staphylococcus aureus ATCC 49619 mutant2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID279255Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 3009 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID530595Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr7 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID244721Frequency of resistance emergence for methicillin resistant Staphylococcus aureus-332005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID264956Activity against Mycobacterium tuberculosis ATCC 35801 in CD1 mouse at 50 mg/kg assessed as decrease in bacterial load in spleen relative to control2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
Gatifloxacin derivatives: synthesis, antimycobacterial activities, and inhibition of Mycobacterium tuberculosis DNA gyrase.
AID558590Antimicrobial activity against Streptococcus pneumoniae 2 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID405456Antibacterial activity against Escherichia coli C600Rif in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID563211Antimycobacterial activity against Mycobacterium tuberculosis 08-0787 harboring gyrA Asp94His mutant gene assessed as microbial susceptibility and deletion of codons 678 and 679 in gyrB mutant gene assessed as microbial susceptibility by agar proportion m2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID565323Antibacterial activity against Mycoplasma genitalium M6285 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID279283Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79Y and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1382067Antibacterial activity against Staphylococcus epidermidis ATCC 12228 by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID530590Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr2 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID1237426Bactericidal activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID405467Antibacterial activity against Escherichia coli TOP10 containing pAT851 plasmid by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1237402Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1254072Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1391316Antibacterial activity against Escherichia coli 1924 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID532977Inhibition of DNA supercoiling activity of wild type Mycobacterium tuberculosis DNA gyrase A2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID244968Minimum inhibitory concentration against Pseudomonas aeruginosa ATCC 278532005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant 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
AID528500Antimicrobial activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus JCSC 6769 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID271596Antibacterial activity against Staphylococcus aureus SA14172006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID559053Antibacterial activity against Staphylococcus warneri by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1605834In vivo antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL/6 mouse assessed as reduction in bacterial burden by measuring log10 CFU/cornea at 0.3% administered topically as two times on day 1, four times on day 2 and two tim2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
AID1600098Bactericidal activity against methicillin resistant Staphylococcus aureus N315 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID342081Effect on growth of nonepidemic Clostridium difficile J29 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID285705Antibacterial activity against oxacillin-susceptible Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
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.
AID433400Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID425731Antimicrobial activity against Bacillus anthracis Ames after 18 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
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.
AID237034Dissociation constant (pKa) was determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID425732Apparent volume of distribution with respect to the bioavailability in mouse at 10 to 100 mg/kg, ip2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID518800Antimycobacterial activity against Mycobacterium avium serovar 4 after 14 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID559179Antimicrobial activity against Clostridium difficile C253A selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1600112Bactericidal activity against methicillin resistant Staphylococcus aureus 6347 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium 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.
AID285758Antibacterial activity against Serratia marcescens2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID563012Antimycobacterial activity against Mycobacterium tuberculosis 02-1975 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID429040Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT76 harboring wild type DNA gyrase A assessed as complete cell killing at 4 times MIC after 6 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID563050Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0797 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID428899Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT18 harboring DNA gyrase A S83F and D87G mutation assessed as decrease in viable count at 16 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1393792Antibacterial activity against multidrug resistant Mycobacterium tuberculosis ATTC 27294 by Alamar Blue assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID351442Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID613782Antibacterial activity against methicillin-resistant Staphylococcus aureus 08-1 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID96407In vitro antibacterial activity was tested for Klebsiella pneumoniae MGH-21995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID278262Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS14 acrAB::Kan with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID286111Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 66 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID456029Antibacterial activity against Streptococcus pyogenes G-36 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.
AID1391315Antifungal activity against Candida albicans 7535 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID1570240Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID342065Antimicrobial activity against epidemic Clostridium difficile BI6-8-17 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID278232Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-1 GyrA S83F mutant2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1067077Antimicrobial activity against Pseudomonas aeruginosa 2742 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID285753Antibacterial activity against Salmonella enterica serovar Typhimurium2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID429027Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG258 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1601849Antibacterial activity against Pseudomonas aeruginosa CMCC 27853 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID278241Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-3 gyrA+ with ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID285781Antibacterial activity against Prevotella sp.2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1067072Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolate 3167 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID342064Antimicrobial activity against epidemic Clostridium difficile BI9 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID425348Antibacterial activity against Streptococcus pneumoniae HMC 1073 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID285339Antimicrobial activity against streptomycin-resistant Escherichia coli J53 by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
First report of plasmid-mediated qnrA1 in a ciprofloxacin-resistant Escherichia coli strain in Latin America.
AID163740In vitro antibacterial activity was tested for Providencia rettgeri H17711995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID322985Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae with 23S rRNA A2063G mutant isolate 12007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
AID278240Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-3 with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
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.
AID285774Antibacterial activity against Peptostreptococcus magnus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
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.
AID563215Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0794 harboring gyrA Thr80Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID342245Increase in toxin level in epidemic Clostridium difficile BI9 infected CF1 mouse at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID405825Antimicrobial activity against Acinetobacter baumannii 694 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID425775Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB after 28 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1601844Antibacterial activity against Streptococcus pneumoniae CMCC 31968 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID428997Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT142 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID67078Antibacterial activity was determined against Enterococcus faecalis ATCC 19433 strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID559200Antibacterial activity against Streptococcus pneumoniae S001 harboring parC Asp83Asn mutant and wild-type gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559507Antibacterial activity against Staphylococcus saprophyticus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID298873Antibacterial activity against penicillin-resistant Streptococcus pneumoniae ATCC 700904 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID265984Activity against Mycobacterium tuberculosis H37Rv infected in CD1 mouse assessed as decrease in bacterial load relative to control in lung at 50 mg/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
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.
AID561400Antibacterial activity against quinolone-susceptible Bordetella pertussis BP118 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID558925Antimicrobial activity against Clostridium difficile A422a selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425357Antibacterial activity against Streptococcus pneumoniae HMC 1071 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene and S79F, K137N mutation in QRDR of ParC gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1330196Antibacterial activity against quinolone-resistant Staphylococcus aureus 3505 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID563031Antimycobacterial activity against Mycobacterium tuberculosis 08-0771 harboring gyrA putative promoter mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558621Antimicrobial activity against Streptococcus pneumoniae isolate 3346 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID565313Antibacterial activity against Mycoplasma genitalium TW10-5G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1237417Fungicidal activity against Candida albicans 7535 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID237037Dissociation constant (pKa) was determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID265978Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID279273Antibacterial activity against Streptococcus pneumoniae assessed as period of suppression of bacterial growth2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID558877Antimicrobial activity against Clostridium difficile A422 expressing tcdA and tcdB gene by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559245Antibacterial activity against Streptococcus pneumoniae D002 harboring parC Ser79Phe and gyrA Ser81Phe mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1067083Antimicrobial activity against Staphylococcus aureus RN4220 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID405299Antimicrobial activity against Leptospira interrogans serovar Portlandvere infected golden Syrian hamster model of acute lethal leptospirosis assessed as survival at 5 mg/kg/day, ip once daily for 5 days administered 2 day after infection2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of fluoroquinolones against Leptospira interrogans in a hamster model.
AID1237415Bactericidal activity against Streptococcus mutans 3065 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1067071Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolate 3506 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID425073Antimicrobial activity against Escherichia coli DH10B expressing pCR2.1 in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID456034Antibacterial activity against Pseudomonas aeruginosa PAO1 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.
AID520613Cmax in BALB/c mouse serum at 100 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.
AID530634Antimicrobial activity against Staphylococcus aureus CB808 harboring quinolone-resistant parC S80F mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID559175Antimicrobial activity against Clostridium difficile BI2f harboring GyrB Arg447Lys and Asp426Asn mutant gene selected after 32 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID428978Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate B111 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID436988Inhibition of human HeLa cell proliferation2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
7-((4-Substituted)piperazin-1-yl) derivatives of ciprofloxacin: synthesis and in vitro biological evaluation as potential antitumor agents.
AID530632Antimicrobial activity against Staphylococcus aureus CB190 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID558908Antimicrobial activity against Clostridium difficile CD5e harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID405824Antimicrobial activity against Acinetobacter baumannii 696 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID425542Antibacterial activity against Streptococcus pneumoniae HMC 1139 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID298867Antibacterial activity against Staphylococcus aureus ATCC 33592 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID279277Antimicrobial activity agaisnt Streptococcus pneumoniae R6 transformants with parC S79Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID278040Cytotoxicity against human PC3 cells at 4 ug/ml relative to control2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1264463Antimycobacterial activity against rifamypicin-resistant Mycobacterium tuberculosis after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID429019Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG15 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID528517Bactericidal activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus at 16 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID530350Antimicrobial activity against Escherichia coli TOP10 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID559505Antibacterial activity against Staphylococcus hominis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285772Antibacterial activity against Peptostreptococcus anaerobius2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID279203Antibacterial activity against Streptococcus pneumoniae 1076 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID559488Antibacterial activity against Peptostreptococcus sp. by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID542501Antimicrobial activity against Escherichia coli K-12 harboring parE A458 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID565320Antibacterial activity against Mycoplasma genitalium M2341 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID563038Antimycobacterial activity against Mycobacterium tuberculosis 08-0781 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425074Antimicrobial activity against Escherichia coli DH10B in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID278050Suppression of 1 ng/ml LPS-stimulated IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID563058Antimycobacterial activity against Mycobacterium tuberculosis 04-0649 harboring gyrA Asp94Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559495Antibacterial activity against Prevotella sp. assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID271600Antibacterial activity against Staphylococcus aureus SA25582006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID559240Antibacterial activity against Streptococcus pneumoniae S001 harboring parC Asp83Asn mutant and wild-type gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID498188Antibacterial activity against Stenotrophomonas maltophilia MBS108 containing both chromosomally and plasmid encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID262134Antimicrobial activity against Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID530593Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr5 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID425556Antibacterial activity against quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 441 expressing ermB by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1382078Antibacterial activity against Staphylococcus aureus NCDC 110 after overnight incubation by single disc method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID563212Antimycobacterial activity against Mycobacterium tuberculosis 08-0745 harboring gyrA Asp89Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285763Antibacterial activity against Actinomyces sp.2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID325852Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
AID278046Reduction of Mycoplasma hominis-stimulated IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID558598Antimicrobial activity against Streptococcus pneumoniae 10 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID368421Antimicrobial activity against Escherichia coli KAM32 pSTV28 containing chloramphenicol-resistant vector by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID565330Antibacterial activity against Mycoplasma genitalium M6284 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1237404Antibacterial activity against Staphylococcus aureus KCTC 503 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1067075Antimicrobial activity against Salmonella typhimurium 2421 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1067070Antimicrobial activity against quinolone-resistant Staphylococcus aureus clinical isolate 3505 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID342093Increase in toxin level in nonepidemic Clostridium difficile J29 infected CF1 mouse at 2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID285779Antibacterial activity against Prevotella melaninogenica2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID286117Bactericidal activity against Staphylococcus aureus BSP-2443 at fAUC/MIC of 62 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1551291Antibacterial activity against Staphylococcus aureus KCTC209 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID425736Ratio of AUC (0 to 24 hrs) for Staphylococcus aureus infected ICR/Swiss mouse model to MIC for Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID558627Antimicrobial activity against Streptococcus pneumoniae isolate 3587 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID542503Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87 and parC K84 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID559496Antibacterial activity against Propionibacterium acnes assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558909Antimicrobial activity against Clostridium difficile CD5f harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1240504Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID428995Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate ipt 33 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID279211Antibacterial activity against Streptococcus pneumoniae 37 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID286113Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 144 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID558875Antimicrobial activity against Clostridium difficile C253 expressing tcdA and tcdB gene by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1626595Inhibition of wild type Staphylococcus aureus topoisomerase 4 assessed as compound concentration causing 50% induction of cleavage of covalently closed DNA substrate2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID429041Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate HTD 798 harboring DNA gyrase A S83F mutation assessed as complete cell killing at 4 times MIC after 6 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID425729Tlag in mouse at 10 to 100 mg/kg, ip2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID271592Antibacterial activity against Escherichia coli EC20262006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID558589Antimicrobial activity against Streptococcus pneumoniae 1 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559150Antimicrobial activity against Clostridium difficile 630b selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1330191Antibacterial activity against Salmonella typhimurium 1926 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID562829Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0757 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID563051Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 99-1914 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID373002Antimycobacterial activity against Mycobacterium avium complex N018 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID50848In vitro antibacterial activity was tested for Clostridium diff CD1-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID531858Tmax in tuberculosis patient at 4.59 ug/ml, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID558608Antimicrobial activity against Streptococcus pneumoniae isolate 1394 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID325854Antimycobacterial activity against Mycobacterium smegmatis MC2 by agar dilution method2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
AID279256Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3009 with GyrA S81F and ParC D83N mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID342092Increase in toxin level in nonepidemic Clostridium difficile ATCC 9689 infected in CF1 mouse at 2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1330193Antifungal activity against Candida albicans 7535 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID530639Antimicrobial activity against Staphylococcus aureus CB812 harboring rpoB H481Y, gyrA S84L and gyrA S80F mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1601850Antibacterial activity against Pseudomonas aeruginosa CMCC 10104 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID278250Antimicrobial activity against Salmonella enterica serovar Typhimurium CS1 acrAB::Kan with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID1254069Antibacterial activity against Staphylococcus aureus 503 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID558616Antimicrobial activity against Streptococcus pneumoniae isolate 2880 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID613788Antibacterial activity against Streptococcus pneumoniae 08-4 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID429018Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG8 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID528520Bactericidal activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus at 2048 ug/ml after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID559523Antibacterial activity against Streptococcus sanguinis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558883Antimicrobial activity against Clostridium difficile C253a selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1557306Protein binding in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID425570Antibacterial activity against penicillin-susceptible, quinolone-resistant Streptococcus pneumoniae HMC 1072 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I460V 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID530637Antimicrobial activity against Staphylococcus aureus CB812 harboring rpo B H481Y and gyrA S84L mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID285707Antibacterial activity against oxacillin and levofloxacin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID542521Antimicrobial activity against fluoroquinolone-resistant Escherichia coli clinical isolate by Etest2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Relationships among ciprofloxacin, gatifloxacin, levofloxacin, and norfloxacin MICs for fluoroquinolone-resistant Escherichia coli clinical isolates.
AID429039Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT144 harboring DNA gyrase A D87G mutation assessed as decrease in bacterial population at 4 times MIC after 30 mins by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID405461Antibacterial activity against Escherichia coli TOP10 by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID563013Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2614 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1330197Antibacterial activity against quinolone-resistant Staphylococcus aureus 3519 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID1600106Bactericidal activity against Escherichia coli ATCC 8739 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1067078Antimicrobial activity against Escherichia coli CCARM 1356 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
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.
AID1890606Antibacterial activity against beta-lactams, macrolide and fluoroquinolone resistant Streptococcus pneumoniae 718 infected in po dosed Swiss mouse septicemia model assessed as protective dose administered on 1 and 5 hrs post infection and measured on day 2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID425726Half life in human2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID563053Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2614 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1330195Antibacterial activity against methicillin-resistant Staphylococcus aureus 3506 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID563052Antimycobacterial activity against Mycobacterium tuberculosis 02-1975 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1585702Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID519203Antibacterial activity against Streptococcus pneumoniae assessed as susceptible isolates by microdilution method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
In vitro activity of AR-709 against Streptococcus pneumoniae.
AID1557282Antibacterial activity against Bacteroides fragilis by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID310321Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
An atom efficient, solvent-free, green synthesis and antimycobacterial evaluation of 2-amino-6-methyl-4-aryl-8-[(E)-arylmethylidene]-5,6,7,8-tetrahydro-4H-pyrano[3,2-c]pyridine-3-carbonitriles.
AID530591Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr3 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID425548Antibacterial activity against Streptococcus pneumoniae HMC 1062 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID309398Antitubercular activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Synthesis and antitubercular activity of lipophilic moxifloxacin and gatifloxacin derivatives.
AID563025Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-1234 harboring gyrA Asn533Thr gyrB mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1382068Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID425071Antimicrobial activity against Escherichia coli J53-AzR in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID565310Antibacterial activity against Mycoplasma genitalium G37 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID428994Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate ipt 32 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1600100Bactericidal activity against Staphylococcus epidermidis ATCC 14990 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID530599Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr11 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
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.
AID245040Minimum inhibitory concentration against Staphylococcus saprophyticus ATCC 153052005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID558897Antimicrobial activity against Clostridium difficile C253i harboring GyrA Ala118Ser mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID531859Antimicrobial activity against Mycobacterium tuberculosis infected in patient at 400 mg/day, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID530592Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr4 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID245695Mutant prevention concentration against methicillin resistant Staphylococcus aureus-32 done for 48 h at 37 degree C with compound2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1600103Antibacterial activity against Bacillus subtilis ATCC 6633 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID433579Inhibition of Mycobacterium leprae wild type DNA gyrase subunit A A91V mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID244935Minimum inhibitory concentration against Klebsiella pneumoniae ATCC 100312005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
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.
AID209273Antibacterial activity was determined against Streptococcus pyogenes G-36 strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID351441Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID561393Antibacterial activity against quinolone-susceptible Bordetella pertussis BP112 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID405297Antimicrobial activity against Leptospira interrogans serovar Portlandvere infected golden Syrian hamster model of acute lethal leptospirosis assessed as survival at 50 mg/kg/day, ip once daily for 5 days administered 2 day after infection2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of fluoroquinolones against Leptospira interrogans in a hamster model.
AID1445729Ratio of MIC for Staphylococcus aureus ATCC 29213 after 15 passages to MIC for Staphylococcus aureus ATCC 292132017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1601852Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID563223Antimycobacterial activity against Mycobacterium tuberculosis 08-0774 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID429023Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG168 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID271608Antibacterial activity against Streptococcus pyogenes C203 SP1-12006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID563040Antimycobacterial activity against Mycobacterium tuberculosis 08-0789 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425762Antibacterial activity against penicillin-, macrolide-susceptible and quinolone-resistant Streptococcus pneumoniae HMC 1074 harboring S81F, E85K mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID279291Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID278251Antimicrobial activity against Salmonella enterica serovar Typhimurium CS1 tolC::Kan with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID1254068Antibacterial activity against Staphylococcus aureus 209 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID164393Antibacterial activity was determined against Pseudomonas aeruginosa PAO1 strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID425734Ratio of AUC (0 to 24 hrs) for Staphylococcus infected patient to MIC for Staphylococcus2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID279270Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 24 with GyrA S81Y, GyrB P413S and ParC S79F mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID286114Bactericidal activity against Staphylococcus aureus BSP-2443 at fAUC/MIC of 51 after 24 to 48 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID298859Antibacterial activity against Staphylococcus epidermidis ATCC 12228 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID425567Antibacterial activity against Streptococcus pneumoniae HMC 3041 after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID562825Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 03-0738 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID613790Antibacterial activity against Enterococcus faecium 08-7 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID563045Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0930 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1601847Antibacterial activity against Escherichia coli CMCC 25922 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID279290Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID563228Antimycobacterial activity against Mycobacterium tuberculosis 08-0789 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID262138Inhibitory activity against wild type Staphylococcus aureus topoisomerase 42006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID278248Antimicrobial activity against Salmonella enterica serovar Typhimurium CS1 with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID324746Effect on Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as enhancement of supercoiled pBR322 DNA cleavage2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID279259Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 1076 with ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID351296Antibacterial activity against Salmonella typhi ATCC 19430 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID563022Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 04-0519 harboring gyrA Ala90Val and Asp94Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID278263Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS14 tolC::Kan with GyrA D87G mutant2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID285767Antibacterial activity against Clostridium difficile2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID1600117Antibacterial activity against Serratia marcescens ATCC 12795 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID105998In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
AID559376Antimicrobial activity against Clostridium difficile A422A selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID278243Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-3 tolC::Kan with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID293149Antibacterial activity against quinoline-intermediate methicillin-resistant Staphylococcus aureus by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID559407Antimicrobial activity against Clostridium difficile BI2B selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID278266Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS18 acrAB::Kan with GyrA S38F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID278054Inhibition of peptidoglycan-induced NF kappaB activation in human PC3 cells at 16 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID429029Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate HTD 798 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID699002Cmax in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
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]
AID1600114Bactericidal activity against methicillin resistant Staphylococcus epidermidis ATCC 13199 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID530597Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr9 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID759326Antibacterial activity against Staphylococcus aureus KCTC 503 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID285799Antibacterial activity against Salmonella enterica serovar Enteritidis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID342253Drug level in Clostridium difficile infected CF1 mouse stool at 0.2 mg/day for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1254080Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID249969Ratio of MPC to MIC against methicillin resistant Staphylococcus aureus-332005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID351290Antibacterial activity against Staphylococcus epidermidis ATCC 4940 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID1237424Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID530596Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr8 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID563224Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0777 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID322983Antimicrobial activity against macrolide-susceptible Mycoplasma pneumoniae Mac2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
AID1600105Antibacterial activity against Escherichia coli ATCC 8739 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID558878Antimicrobial activity against Clostridium difficile 630 expressing tcdA and tcdB gene by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID563032Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0746 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563210Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 04-0519 harboring gyrA Ala90Val and Asp94Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID286075Half life at 175 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID264950Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
Gatifloxacin derivatives: synthesis, antimycobacterial activities, and inhibition of Mycobacterium tuberculosis DNA gyrase.
AID1254076Antifungal activity against Candida albicans 7535 by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1626621Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y/gyrA S84L/parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID428898Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT18 harboring DNA gyrase A S83F and D87G mutation assessed as decrease in viable count at 8 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID429020Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG16 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID425562Antibacterial activity against penicillin- and quinolone-susceptible Streptococcus pneumoniae HMC 5055 expressing mefA after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID342073Effect on growth of nonepidemic Clostridium difficile J29 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID428979Antimicrobial activity against Salmonella enterica Serovar Typhi isolate E86 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1491402Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis after 3 to 7 days by rapid direct susceptibility test
AID237458Partition coefficient (logD7.4)2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID285726Antibacterial activity against beta-lactamase positive Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID425560Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID558876Antimicrobial activity against Clostridium difficile CD25 expressing tcdA, tcdB gene and GyrB Ser416Ala mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID733009Antimicrobial activity against Mycobacterium tuberculosis H37Rv assessed as drug concentration causing =<1% reduction in bacterial growth incubated for 21 to 30 days by proportion method2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID1237416Bactericidal activity against Escherichia coli KCTC 1924 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID528499Antimicrobial activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus JCSC 6768 expressing gyrA Glu84Lys and grlA Ser80Phe mutants by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID285724Antibacterial activity against VanA-resistant Enterococcus faecalis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID558609Antimicrobial activity against Streptococcus pneumoniae isolate 1397 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID285742Antibacterial activity against Citrobacter freundii2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID429013Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT60 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID429031Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate BL 21095 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1382072Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID558623Antimicrobial activity against Streptococcus pneumoniae isolate 3412 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID429028Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG259 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1330190Antibacterial activity against Escherichia coli 1356 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID1382066Antibacterial activity against Escherichia coli ATCC 700603 by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID278230Antimicrobial activity against Salmonella enterica serovar Typhimurium S21 acrAB::Kan2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID559169Antimicrobial activity against Clostridium difficile BI2c harboring GyrB Arg447Lys mutant gene selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
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.
AID559508Antibacterial activity against Staphylococcus warneri assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID561390Antibacterial activity against quinolone-susceptible Bordetella pertussis BP106 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID561395Antibacterial activity against quinolone-susceptible Bordetella pertussis BP115 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID244934Minimum inhibitory concentration against Enterococcus faecalis ATCC 292122005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID559389Antimicrobial activity against Clostridium difficile A422H harboring GyrA Thr82Ile and GyrB Leu451Phe mutant genes selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID558927Antimicrobial activity against Clostridium difficile A422c selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1067069Antimicrobial activity against quinolone-resistant Staphylococcus aureus clinical isolate 3519 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1570244Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID498189Antibacterial activity against Stenotrophomonas maltophilia MBS109 containing chromosomally encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID542505Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87, parC I80 and parE M464 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID559005Antibacterial activity against Streptococcus pneumoniae W002 harboring wild-type parC and gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID429007Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT40 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID208121In vitro antibacterial activity was tested for Streptococcus pneumoniae SV-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID1551293Antibacterial activity against Streptococcus mutans KCTC3289 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1510744Antibacterial activity against methicillin-resistant Staphylococcus aureus by two fold dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Nitroimidazole-containing compounds and their antibacterial and antitubercular activities.
AID285713Antibacterial activity against Staphylococcus warneri2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID351291Antibacterial activity against Streptococcus pneumoniae ATCC 1240 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID271603Antibacterial activity against Enterococcus faecalis MGH2 EF1-12006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID563042Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 03-0738 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563043Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2934 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID542520Antimicrobial activity against fluoroquinolone-resistant Escherichia coli clinical isolate by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Relationships among ciprofloxacin, gatifloxacin, levofloxacin, and norfloxacin MICs for fluoroquinolone-resistant Escherichia coli clinical isolates.
AID298868Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID285709Antibacterial activity against oxacillin-susceptible Staphylococcus epidermidis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
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.
AID278239Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-2 tolC::Kan with GyrA S83F, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID559493Antibacterial activity against Fusobacterium sp. assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1570245Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 1 incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
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.
AID1570246Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 2 incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID425558Antibacterial activity against penicillin-, quinolone-resistant and macrolide-susceptible Streptococcus pneumoniae HMC 1058 harboring S79F, K137N mutation in quinolone-resistant determining regions of ParC gene and 460V mutation in QRDR of ParE gene by br2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID542500Antimicrobial activity against Escherichia coli K-12 harboring by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID278260Antimicrobial activity against Salmonella enterica serovar Typhimurium CHS14 with GyrA D87G mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID425343Antibacterial activity against Streptococcus pneumoniae HMC 1151 harboring D83N, K137N mutation in quinolone-resistant determining regions of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to ciprofloxacin, gemifloxacin by agar dilution 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1237412Bactericidal activity against Staphylococcus aureus RN4220 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID456027Antibacterial activity against Staphylococcus epidermidis 56500 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.
AID388870Antibacterial activity against Staphylococcus aureus ATCC 13709 after 24 hrs by microdilution method2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID558624Antimicrobial activity against Streptococcus pneumoniae isolate 3455 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID298864Antibacterial activity against Escherichia coli ATCC 25922 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID425554Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID429021Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG17 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
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).
AID563220Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0746 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563049Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0791 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559243Antibacterial activity against Streptococcus pneumoniae S004 harboring wild-type parC and gyrA Gly85Asn mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1330189Antibacterial activity against Escherichia coli 1924 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID425765Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I4602008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID429006Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT37 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID563015Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0744 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425359Antibacterial activity against Streptococcus pneumoniae HMC 1074 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID293155Antibacterial activity against Escherichia coli without AcrAB efflux system by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID244926Minimum inhibitory concentration against Bacteroides vulgatus ATCC 293272005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID563029Antimycobacterial activity against Mycobacterium tuberculosis 08-0773 harboring gyrA Pro8Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1067082Antimicrobial activity against Staphylococcus aureus 209 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID286093fAUC/MIC ratio of Staphylococcus aureus BSP-2443 at 235 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285751Antibacterial activity against Proteus vulgaris2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID613789Antibacterial activity against Enterococcus faecium 08-2 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID559521Antibacterial activity against Streptococcus oralis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
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.
AID298872Antibacterial activity against vancomycin-resistant Enterococcus faecium ATCC 700221 by microbroth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID559163Antimicrobial activity against Clostridium difficile 630i harboring GyrB Asp26Val mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID561396Antibacterial activity against quinolone-susceptible Bordetella pertussis BP128 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID271607Antibacterial activity against quinolone-resistant Streptococcus pneumonia SP37632006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID279275Antimicrobial activity against Streptococcus pneumoniae R62007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID278229Antimicrobial activity against Salmonella enterica serovar Typhimurium S21 gyrA+2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID372990Antimycobacterial activity against Mycobacterium intracellular JATA52-01 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID563221Antimycobacterial activity against Mycobacterium tuberculosis 08-0762 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID342083Effect on growth of epidemic Clostridium difficile BI6-8-17 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID558879Antimicrobial activity against Clostridium difficile BI2 by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID285710Antibacterial activity against oxacillin-resistant Staphylococcus epidermidis2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID562827Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-1647 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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).
AID1237413Bactericidal activity against Staphylococcus aureus KCTC 209 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID425544Antibacterial activity against Streptococcus pneumoniae HMC 1541 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID279284Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79Y and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1237423Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1067074Antimicrobial activity against Salmonella typhimurium 1926 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1330186Antibacterial activity against Staphylococcus aureus 4220 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID1601843Antibacterial activity against Streptococcus pyogenes CMCC 32067 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID1916143Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 in C57BL/6 mouse model of bacterial keratitis assessed as log reduction in number of viable bacterial colonies in infected cornea at 3 mg/ml, TOP administered 4 times a day for 3 consecutive
AID286063Half life at 400 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID450457Antibacterial activity against Staphylococcus aureus after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID1402093Antibacterial activity against Staphylococcus aureus2018European journal of medicinal chemistry, Jan-01, Volume: 1434-Quinolone derivatives and their activities against Gram positive pathogens.
AID558885Antimicrobial activity against Clostridium difficile C253c selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1237428Bactericidal activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID425355Antibacterial activity against Streptococcus pneumoniae HMC 1055 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID561389Antibacterial activity against quinolone-susceptible Bordetella pertussis BP101 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
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.
AID428992Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 50 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID428991Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 46 harboring DNA gyrase A D87G mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID433578Inhibition of Mycobacterium leprae wild type DNA gyrase subunit A G89A mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID429005Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT18 harboring DNA gyrase A S83F and D87G mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID601783Antibacterial activity against 10'4 CFU Enterococcus faecalis 08-10 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID528512Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 8 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID429024Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG169 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID542514Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, Y87 and parC I80 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID368420Antimicrobial activity against Escherichia coli KAM32 pHPA containing mutated GyrA gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID271594Antibacterial activity against Haemophilus influenzae HI35422006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID433580Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID559186Antimicrobial activity against Clostridium difficile C253E selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1600094Lipophilicity, log k of the compound at 100 ug/ml by micellar electrokinetic chromatography2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID351289Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID450460Antibacterial activity against Pseudomonas aeruginosa after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID528518Bactericidal activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus at 2048 ug/ml after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID559491Antibacterial activity against Bacteroides fragilis assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID405464Antibacterial activity against Escherichia coli TOP10 containing pIP1206 plasmid by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID563055Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0744 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285775Antibacterial activity against Peptostreptococcus prevotii2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID759323Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
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).
AID556013Antibacterial activity against Helicobacter pylori infected in human assessed as bacterial eradication rate at 400 mg, po QD for 7 days2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID528504Bactericidal activity against methicillin-resistant Staphylococcus aureus at 8 times MIC upto 60 mins by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID1888650Antibacterial activity against ciprofloxacin resistant Staphylococcus aureus harboring ParCS80F and GyrAS84L double mutant assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID271586Inhibition of Escherichia coli gyrase2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID206765In vitro antibacterial activity was tested for Staphylococcus aureus UC-761995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID445445Permeability at pH 6.5 by PAMPA method2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
AID1570242Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID405462Antibacterial activity against Escherichia coli TOP10 in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID601779Antibacterial activity against 10'4 CFU methicillin-resistant Staphylococcus aureus 08-1 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID279281Antimicrobial activity against Streptococcus pneumoniae R6 transformants with gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID285784Antibacterial activity against Streptococcus salivarius2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID428984Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 102 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID425572Antibacterial activity against penicillin-, macrolide- and quinolone-susceptible Streptococcus pneumoniae HMC 63 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83Y mutation in QRDR of ParC gene and I460V mutation in QRDR2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID351299Antibacterial activity against Serratia marcescens PTCC 1111 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID279258Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 1076 with ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID425550Antibacterial activity against penicillin-susceptible, quinolone-resistant Streptococcus pneumoniae 1072 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I460V muta2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID372984Antimycobacterial activity against Mycobacterium avium JATA51-01 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID530348Antimicrobial activity against azide-resistant Escherichia coli J53 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID456030Antibacterial activity against Streptococcus mitis IID685 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.
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.
AID563225Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0779 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558914Antimicrobial activity against Clostridium difficile CD5h harboring GyrA Ala92Glu and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID429011Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT49 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559492Antibacterial activity against Clostridium perfringens assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425557Antibacterial activity against quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 5048 expressing mefA by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID563018Antimycobacterial activity against Mycobacterium tuberculosis 04-0649 harboring gyrA Asp94Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID405823Antimicrobial activity against Acinetobacter baumannii 9043 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID1240505Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID563011Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 99-1914 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID433403Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1570243Inhibition of Mycobacterium tuberculosis DNA gyrase2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID342095Increase in toxin level in epidemic Clostridium difficile BI6-8-17 infected CF1 mouse at 2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID759321Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID1067076Antimicrobial activity against Pseudomonas aeruginosa 2004 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID456048Inhibition of Staphylococcus aureus DNA topoisomerase 4 Ser80Phe mutant2009Bioorganic & 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.
AID428981Antimicrobial activity against Salmonella enterica Serovar Typhi isolate C152 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559406Antimicrobial activity against Clostridium difficile BI2A selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID558591Antimicrobial activity against Streptococcus pneumoniae 3 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID271590Antibacterial activity against Providencia rettgeri PR92006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID394143Antibacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids.
AID1626598Inhibition of FQ-resistant Staphylococcus aureus GyrA S84L mutant assessed as compound concentration causing 50% induction of cleavage of covalently closed DNA substrate2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID372986Antimycobacterial activity against Mycobacterium avium JATA51-01 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1254070Antibacterial activity against Streptococcus mutans 3065 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID528495Antimicrobial activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus JCSC 6764 expressing gyrA Ser84Leu, gyrB Asp437Glu norA T389C and grlA Ser80Phe/Glu84Lys mutants by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID531851Clearance in tuberculosis patient at 400 mg/day, po administered for 7 days measured after 24 hrs by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID278052Suppression of TNF alpha-stimulated IL8 secretion in human PC3 cells at 16 ug/ml added 30 mins after stimulation2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID601793Cytotoxicity against MDCK cells after 48 hrs by CPE assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID372998Antimycobacterial activity against Mycobacterium avium complex N016 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID425360Antibacterial activity against Streptococcus pneumoniae HMC 1077 harboring S81Y and S79F mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID285773Antibacterial activity against Peptostreptococcus asaccharolyticus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID286092fAUC/MIC ratio of Staphylococcus aureus BSP-2443 at 198 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID405463Antibacterial activity against Escherichia coli TOP10 in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID559413Antimicrobial activity against Clostridium difficile BI2E harboring GyrB Glu466Lys mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID298860Antibacterial activity against Staphylococcus aureus ATCC 33591 by micro-broth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID372978Antimycobacterial activity against Mycobacterium avium JATA51-01 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID563047Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0785 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID531860Ratio of fAUC in patient with tuberculosis at 400 mg/day, po administered for 7 days to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID759322Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID1391312Antibacterial activity against quinolone-resistant Staphylococcus aureus isolate CCARM 3505 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID278042Decrease in IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1484396Antitubercular activity against Mycobacterium tuberculosis H37Rv2017European journal of medicinal chemistry, Jun-16, Volume: 133Isoniazid derivatives and their anti-tubercular activity.
AID158681In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum NF54-R in blood2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
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.
AID286104Bactericidal activity against Staphylococcus aureus ATCC 49619 with Parc S79Y mutation and gyrA S81F mutation at fAUC/MIC of 35 after 48 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID559412Antimicrobial activity against Clostridium difficile BI2D harboring GyrB Glu466Lys mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559516Antibacterial activity against Streptococcus anginosus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID278235Antimicrobial activity against Salmonella enterica serovar Typhimurium S21-1 tolC::Kan with GyrA S83F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID563059Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2399 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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.
AID286103Bactericidal activity against Staphylococcus aureus ATCC 49619 with Parc S79Y mutation at fAUC/MIC of 35 after 24 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID405300Toxicity against Leptospira interrogans serovar Portlandvere infected golden Syrian hamster model of acute lethal leptospirosis assessed as induction of diarrhea at 50 mg/kg/day, ip once daily for 5 days administered 2 day after infection2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of fluoroquinolones against Leptospira interrogans in a hamster model.
AID325855Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
AID425565Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 99 after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID342098Increase in toxin level in epidemic Clostridium difficile BI9 infected CF1 mouse at 1.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID286116Bactericidal activity against Staphylococcus aureus BSP-2443 with parC S52G, N91D mutation and gyrA S114G mutation at fAUC/MIC of 51 after 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID390106Binding affinity to bone assessed as drug level bound to cattle bone meal powder by fluorescence assay2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.
AID580862Cmax in patients with pulmonary tuberculosis at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID279240Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 1076 with ParC S79Y mutation after 20 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID542517Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, Y87, parC I80, G84 and parE A458 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID51930K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID68339In vitro antibacterial activity was tested for Enterobacter cloacae HA26461995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID601781Antibacterial activity against 10'4 CFU methicillin-resistant Staphylococcus epidermidis 09-2 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID433401Inhibition of Mycobacterium leprae DNA gyrase subunit A G89C mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1391311Antibacterial activity against Staphylococcus aureus 4220 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID530638Antimicrobial activity against Staphylococcus aureus CB812 harboring rpoB H481Y and gyrA S80F mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID278061Suppression of TNF alpha-stimulated IL8 D-188 mutant promoter activity in human PC3 cells at 16 ug/ml dual luciferase reporter assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1601851Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID559522Antibacterial activity against Streptococcus salivarius assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID245696Mutant prevention concentration aganist methicillin resistant Staphylococcus aureus-33 done for 48 hr at 37 degree C with compound2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID303465Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid.
AID271602Antibacterial activity against ciprofolxacin-resistant Staphylococcus aureus SA20172006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1557284Antibacterial activity against Staphylococcus aureus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID558615Antimicrobial activity against Streptococcus pneumoniae isolate 2874 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID521102Antimicrobial activity against Streptococcus sp. 'group B' isolate 9 harboring gyrA Ser81Leu mutant, parC Ser79Tyr mutant and parE Ileu495Leu mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
AID425766Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I462008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID530635Antimicrobial activity against Staphylococcus aureus CB814 harboring fluoroquinolone-resistant gyrA S84L and parC S80F mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID425353Antibacterial activity against Streptococcus pneumoniae HMC 2538 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to ciproflox2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID271601Antibacterial activity against methicillin-resistant Staphylococcus aureus SA14172006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID1488560Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis 09710 by two fold dilution method
AID559388Antimicrobial activity against Clostridium difficile A422G harboring GyrA Thr82Ile and GyrB Leu451Phe mutant genes selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID286043Susceptibility of Streptococcus pneumoniae ATCC 49619 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID521101Antimicrobial activity against Streptococcus sp. 'group B' isolate 16 harboring gyrA Ser81Leu mutant, parC Ser79Tyr mutant and parE Ileu495Leu mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
AID373004Antimycobacterial activity against Mycobacterium avium complex N018 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID442255Antimalarial activity against Plasmodium falciparum NF542009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.
AID278053Suppression of TNF alpha-stimulated IL8 secretion in human PC3 cells at 16 ug/ml added 60 mins after stimulation2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1067081Antimicrobial activity against Staphylococcus aureus 503 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
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).
AID278228Antimicrobial activity against Salmonella enterica serovar Typhimurium S212007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID372979Antimycobacterial activity against Mycobacterium intracellular JATA52-01 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID429003Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT9 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559402Antimicrobial activity against Clostridium difficile 630F harboring GyrA Ala118Val mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID286109Bactericidal activity against Staphylococcus aureus ATCC 49619 with parC S79Y mutation at fAUC/MIC of 60 after 72 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID278049Suppression of 0.1 ng/ml LPS-stimulated IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID342080Effect on growth of nonepidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID425727Half life in mouse at 10 to 100 mg/kg, ip2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID559144Antimicrobial activity against Clostridium difficile A422h harboring GyrA Asp81Asn mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559173Antimicrobial activity against Clostridium difficile BI2d harboring GyrB Arg447Lys and Asp426Asn mutant gene selected after 32 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID293157Antibacterial activity against Pseudomonas aeruginosa by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID456049Selectivity ratio of IC50 for Staphylococcus aureus DNA topoisomerase 4 Ser80Phe mutant to IC50 for Staphylococcus aureus wild type DNA topoisomerase 42009Bioorganic & 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.
AID498187Antibacterial activity against Stenotrophomonas maltophilia D457 containing chromosomally encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID563010Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0797 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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]
AID438297Inhibition of penicillin-sensitive Streptococcus pneumoniae R6 PBP2X preincubated for 1 hr before addition of substrate (R)-[2-(benzoylamino)propionylsulfanyl]acetic acid2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Discovery of new inhibitors of resistant Streptococcus pneumoniae penicillin binding protein (PBP) 2x by structure-based virtual screening.
AID558593Antimicrobial activity against Streptococcus pneumoniae 5 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID759325Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID1382071Antibacterial activity against methicillin-sensitive Staphylococcus aureus by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID755684Inhibition of human ERG current by patch clamp assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.
AID322988Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae with 23S rRNA A2064G mutant isolate 42007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
AID278254Antimicrobial activity against Salmonella enterica serovar Typhimurium CS3 acrAB::Kan with GyrA S83F, D87N, ParC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID530349Antimicrobial activity against Escherichia coli TOP10 harboring pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID324745Inhibition of Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as inhibition of pBR322 DNA supercoiling2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID279288Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1067079Antimicrobial activity against Escherichia coli KCTC 1924 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID530346Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M plasmid carrying blaCTX-M-15 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID405469Antibacterial activity against Escherichia coli TOP10 containing pAT851 in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID530630Ratio of CC50 for wild-type Staphylococcus aureus GyrA to CC50 for wild-type Staphylococcus aureus ParC2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1391314Antibacterial activity against Streptococcus mutans 3289 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID558631Antimicrobial activity against Streptococcus pneumoniae isolate 4755 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID262135Antimicrobial activity against methicillin-resistant Staphylococcus aureus 7006992006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID559193Antimicrobial activity against Clostridium difficile CD5C harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID580856Antimicrobial activity against rifampicin-resistant Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID733005Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB A91V mutant-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID286046Peak free concentration at 150 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID559504Antibacterial activity against Staphylococcus haemolyticus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID279278Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID559383Antimicrobial activity against Clostridium difficile A422E harboring GyrB Leu451Phe mutant gene selected after 8 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID561394Antibacterial activity against quinolone-susceptible Bordetella pertussis BP113 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID601786Antibacterial activity against 10'4 CFU Enterococcus faecium 06-7 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID528511Bactericidal activity against levofloxacin-sensitive and methicillin-resistant Staphylococcus aureus at 4 times MIC after 24 hrs by time-kill assay2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID425345Antibacterial activity against Streptococcus pneumoniae HMC 1060 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID565322Antibacterial activity against Mycoplasma genitalium M6280 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID262136Cytotoxicity against human Hep2 laryngeal carcinoma cell line2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID351294Antibacterial activity against Micrococcus luteus ATCC 1110 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID271591Antibacterial activity against Pseudomonas aeruginosa PA72006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID279279Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID601788Antibacterial activity against 10'4 CFU Escherichia coli 08-21 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID559394Antimicrobial activity against Clostridium difficile 630A selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1600107Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID279253Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 37 with GyrA S81Y, GyrB E474K and ParC S79Y mutation after 14 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID405820Antimicrobial activity against Acinetobacter baumannii 501 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID244722Frequency of resistance emergence for methicillin resistant Staphylococcus aureus-50232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID601792Antibacterial activity against 10'4 CFU Pseudomonas aeruginosa 09-32 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID759328Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID558599Antimicrobial activity against Streptococcus pneumoniae 11 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID279271Antibacterial activity against azithromycin resistance selected Streptococcus pneumoniae 2527 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID342072Effect on growth of nonepidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
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).
AID265979Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID559533Antibacterial activity against Klebsiella oxytoca assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1240501Antibacterial activity against Pseudomonas aeruginosa DU14476 after 24 hrs by broth microdilution method2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
N-Lipidated Peptide Dimers: Effective Antibacterial Agents against Gram-Negative Pathogens through Lipopolysaccharide Permeabilization.
AID1382073Antibacterial activity against Klebsiella pneumoniae ATCC 25922 by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID279260Antibacterial activity against azithromycin resistance selected Streptococcus pneumoniae 1077 with 23S rRNA A2058G mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID433581Selectivity index, ratio of IC50 for Mycobacterium leprae DNA gyrase subunit A G89C mutant to IC50 for Mycobacterium leprae wild type DNA gyrase A2B22008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID325853Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis by agar dilution method2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids.
AID456028Antibacterial activity against Streptococcus pneumoniae J-24 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.
AID206214Antibacterial activity was determined against Staphylococcus epidermis 56500 strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID373003Antimycobacterial activity against Mycobacterium avium complex N018 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID405468Antibacterial activity against Escherichia coli TOP10 containing pAT851 in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID558620Antimicrobial activity against Streptococcus pneumoniae isolate 3282 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID542507Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87 and parC I80, G84 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID558628Antimicrobial activity against Streptococcus pneumoniae isolate 3681 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID278063Decrease in IL8 secretion in human prostatic myofibroblast cells at 4 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID733007Inhibition of Mycobacterium leprae DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 2 hrs at 30 degC by ethidium bromide based gel electrophoresis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID278056Inhibition of TNF alpha-induced NF kappaB activation in human PC3 cells at 16 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1510742Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by two fold dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Nitroimidazole-containing compounds and their antibacterial and antitubercular activities.
AID425561Antibacterial activity against penicillin-, quinolone-resistant Streptococcus pneumoniae HMC 1541 harboring mutation in L4 protein by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID405458Antibacterial activity against Escherichia coli C600Rif containing pIP1206 plasmid by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID244720Frequency of resistance emergence for methicillin resistant Staphylococcus aureus-322005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1551294Antibacterial activity against Escherichia coli 1924 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID542504Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, N87 and parC I80 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID559004Antibacterial activity against Streptococcus pneumoniae W001 harboring wild-type parC and gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID96072Antibacterial activity was determined against Klebsiella pneumoniae type II strain after incubation at 37 degrees C for 18 h2003Journal 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.
AID425574Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 harboring S81Y and S79Y mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively after 42 passages2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559151Antimicrobial activity against Clostridium difficile 630c selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID563033Antimycobacterial activity against Mycobacterium tuberculosis 08-0762 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558895Antimicrobial activity against Clostridium difficile C253g harboring GyrA Ala118Ser mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID558594Antimicrobial activity against Streptococcus pneumoniae 6 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID322987Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae with 23S rRNA A2064G mutant isolate 22007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
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.
AID1382070Antibacterial activity against Staphylococcus aureus ATCC 29213 by CLSI agar dilution method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
AID428989Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 28 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID278058Suppression of TNF alpha-stimulated IL8 promoter activity in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID286061Half life at 150 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID563041Antimycobacterial activity against Mycobacterium tuberculosis 00-0715 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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]
AID279287Antimicrobial activity agaisnt Streptococcus pneumoniae R6 transformants with parC S79F and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID613794Antibacterial activity against Escherichia coli 08-21 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID372991Antimycobacterial activity against Mycobacterium intracellular JATA52-01 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dos2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID322986Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae with 23S rRNA A2063G mutant isolate 62007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
AID342244Increase in toxin level in nonepidemic Clostridium difficile J29 infected CF1 mouse at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID293150Antibacterial activity against quinoline-resistant methicillin-resistant Staphylococcus aureus by agar dilution method2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.
AID425573Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 99 harboring S81Y and S79Y mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively after 41 passages 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1264465Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID1600115Antibacterial activity against Streptococcus pneumoniae cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID207830Minimum inhibitory concentration against Staphylococcus aureus - methicillin resistant Ciprofloxacin resistant, strain MI3392003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
AID565321Antibacterial activity against Mycoplasma genitalium M6257 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID285708Antibacterial activity against vancomycin-intermediate Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.
AID530598Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr10 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID425728Apparent distribution clearance in mouse at 10 to 100 mg/kg, ip2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID542513Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, Y87 and parC K84 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID271606Antibacterial activity against Streptococcus pneumonia SVI SP32006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID264955Activity against Mycobacterium tuberculosis ATCC 35801 in CD1 mouse at 50 mg/kg assessed as decrease in bacterial load in lung relative to control2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
Gatifloxacin derivatives: synthesis, antimycobacterial activities, and inhibition of Mycobacterium tuberculosis DNA gyrase.
AID733008Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 1 hr at 37 degC by ethidium bromide based gel electrophoresis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID580864Half life in patients with pulmonary tuberculosis at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID424879Antimicrobial activity against multidrug-resistant Enterobacter cloacae E705 bearing qnrB10 gene with aac(6)-IId-aadA1a integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID559162Antimicrobial activity against Clostridium difficile 630h harboring GyrB Asp26Val mutant gene selected after 8 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425346Antibacterial activity against Streptococcus pneumoniae HMC 1066 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID429032Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate BL 3769 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID271604Antibacterial activity against Enterococcus faecalis EF1-35242006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID563017Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0821 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID162936Minimum inhibitory concentration against Pseudomonas aeruginosa, strain PS962003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Discovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.
AID429012Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT54 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID613795Antibacterial activity against Escherichia coli 08-22 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID559518Antibacterial activity against Streptococcus constellatus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID278044Decrease in IL8 secretion in human PC3 cells at 16 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID1199294Antimicrobial activity against Staphylococcus aureus ATCC 29213 at 0.5 times MIC measured after 17 passages by multistep passage drug resistance selection study relative to wild type Staphylococcus aureus ATCC 29213 before passage2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Amino acid modified xanthone derivatives: novel, highly promising membrane-active antimicrobials for multidrug-resistant Gram-positive bacterial infections.
AID1382074Antibacterial activity against Bacillus subtilis NCDC 71 after overnight incubation by single disc method2018European journal of medicinal chemistry, Feb-25, Volume: 146Ciprofloxacin derivatives and their antibacterial activities.
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.
AID559181Antimicrobial activity against Clostridium difficile C253C selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID50999In vitro antibacterial activity against Clostridium perfringens CP 3-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID1488565Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 27294
AID559201Antibacterial activity against Streptococcus pneumoniae S002 harboring parC Ser79Phe mutant and wild-type gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559192Antimicrobial activity against Clostridium difficile CD5B harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID298870Antibacterial activity against Enterococcus faecalis ATCC 14506 by microbroth dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
AID559502Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus epidermidis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID542516Antimicrobial activity against Escherichia coli K-12 harboring gyrA L83, Y87 and parC I80, G84 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Mechanisms accounting for fluoroquinolone resistance in Escherichia coli clinical isolates.
AID279289Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y and gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1551298Antibacterial activity against Methicillin-resistant Staphylococcus aureus CCARM 3506 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID456026Antibacterial activity against Staphylococcus aureus FDA 209-P 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.
AID351297Antibacterial activity against Shigella flexneri NCTC 8516 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID425555Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 99 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425580Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene and I460V, D435N mutation in QRDR of ParE g2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425563Antibacterial activity against penicillin-, macrolide- and quinolone-susceptible Streptococcus pneumoniae HMC 63 after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID558626Antimicrobial activity against Streptococcus pneumoniae isolate 3481 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID563014Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2230 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1524625Antifungal activity against Candida albicans 7535 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1199313Antimicrobial activity against Staphylococcus aureus ATCC 29213 infected in mouse cornea infection model assessed as reduction in viable bacterial count at 0.3% solution applied topically 5 times/day dosed 1 day after infection relative to control2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Amino acid modified xanthone derivatives: novel, highly promising membrane-active antimicrobials for multidrug-resistant Gram-positive bacterial infections.
AID613781Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID271588Antibacterial activity against Klebsiella pneumonia KP22006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID279276Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1605818Antibacterial activity against Mel-5-resistant vancomycin-resistant Enterococcus faecalis 1010 assessed as reduction in bacterial growth measured after 24 hrs by broth microdilution method2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
AID563037Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0779 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID278231Antimicrobial activity against Salmonella enterica serovar Typhimurium S21 tolC::Kan2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID303470Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected CD1 mouse assessed as spleen bacterial count at 50 mg/kg, ip after 35 days post infection2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Antimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid.
AID613784Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 09-4 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID351298Antibacterial activity against Klebsiella pneumoniae ATCC 10031 after 18 hrs by conventional agar dilution method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
AID244957Minimum inhibitory concentration against Streptococcus sanguis ATCC 105562005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID373008Antimycobacterial activity against Mycobacterium avium complex N084 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID563219Antimycobacterial activity against Mycobacterium tuberculosis 08-0771 harboring gyrA putative promoter mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID561401Antibacterial activity against quinolone-susceptible Bordetella pertussis BP121 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID559180Antimicrobial activity against Clostridium difficile C253B selected after 4 ug/ml of levofloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID271599Antibacterial activity against Staphylococcus aureus SA25542006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
AID425735Ratio of AUC (0 to 24 hrs) for Enterococcus infected patient to MIC for Enterococcus2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pharmacokinetics-pharmacodynamics of gatifloxacin in a lethal murine Bacillus anthracis inhalation infection model.
AID342097Increase in toxin level in nonepidemic Clostridium difficile J29 infected CF1 mouse at 1.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID530631Ratio of CC50 for Staphylococcus aureus ParC S80F mutant to CC50 for wild-type Staphylococcus aureus ParC2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID563054Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2230 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID601787Antibacterial activity against 10'4 CFU Escherichia coli ATCC 25922 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
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.
AID425571Antibacterial activity against penicillin-, macrolide-susceptible and quinolone-resistant Streptococcus pneumoniae HMC 1074 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutat2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID428999Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT145 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID498190Antibacterial activity against Stenotrophomonas maltophilia MBS82 deficient in Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID278055Inhibition of Mycoplasma hominis-induced NF kappaB activation in human PC3 cells at 16 ug/ml2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID528498Antimicrobial activity against low level levofloxacin and methicillin-resistant Staphylococcus aureus JCSC 6767 expressing gyrA Glu84Lys and grlA Ser80Phe mutants by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID372997Antimycobacterial activity against Mycobacterium avium complex N016 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID244891Minimum inhibitory concentration against Escherichia coli ATCC 259222005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID613783Antibacterial activity against methicillin-sensitive Staphylococcus aureus 08-1 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID559241Antibacterial activity against Streptococcus pneumoniae S002 harboring parC Ser79Phe mutant and wild-type gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID563213Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-1234 harboring gyrA Asn533Thr gyrB mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559149Antimicrobial activity against Clostridium difficile 630a selected after 2 ug/ml of moxifloxacin by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID561392Antibacterial activity against quinolone-susceptible Bordetella pertussis BP111 by Etest method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Emergence of quinolone-resistant Bordetella pertussis in Japan.
AID613786Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 09-6 after 18 to 24 hrs by NCCLS M100-S11 two fold serial dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and in vitro antibacterial activity of a series of novel gatifloxacin derivatives.
AID558603Antimicrobial activity against Streptococcus pneumoniae isolate 37 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID278048Suppression of TNF alpha-stimulated IL8 secretion in human PC3 cells2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
The 6-fluoro-8-methoxy quinolone gatifloxacin down-regulates interleukin-8 production in prostate cell line PC-3.
AID342082Effect on growth of epidemic Clostridium difficile BI9 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID531856Cmax in tuberculosis patient at 400 mg/day, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID528494Antimicrobial activity against high level levofloxacin and methicillin-resistant Staphylococcus aureus JCSC 6763 expressing gyrA Ser84Leu/Ser85Pro and grlA Ser80Phe/Glu84Lys mutants by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcu
AID278255Antimicrobial activity against Salmonella enterica serovar Typhimurium CS3 tolC::Kan with GyrA S83F, D87N, parC S80I mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Contribution of target gene mutations and efflux to decreased susceptibility of Salmonella enterica serovar typhimurium to fluoroquinolones and other antimicrobials.
AID405821Antimicrobial activity against Acinetobacter baumannii 695 isolate harboring bla IMP-1 carrying integron In86 containing aminoglycoside resistance gene aac(6')-32007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Characterization of an integron carrying blaIMP-1 and a new aminoglycoside resistance gene, aac(6')-31, and its dissemination among genetically unrelated clinical isolates in a Brazilian hospital.
AID394144Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and antimycobacterial activities of novel 6-nitroquinolone-3-carboxylic acids.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
AID493040Navigating the Kinome2011Nature chemical biology, Apr, Volume: 7, Issue:4
Navigating the kinome.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,001)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's45 (4.50)18.2507
2000's629 (62.84)29.6817
2010's279 (27.87)24.3611
2020's48 (4.80)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 75.73

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 Index75.73 (24.57)
Research Supply Index7.07 (2.92)
Research Growth Index5.32 (4.65)
Search Engine Demand Index133.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (75.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials131 (12.51%)5.53%
Reviews56 (5.35%)6.00%
Case Studies83 (7.93%)4.05%
Observational4 (0.38%)0.25%
Other773 (73.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (31)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Randomized Controlled Research of the Application of Triple Antibiotic Paste in Primary Teeth With [NCT02196740]100 participants (Anticipated)Interventional2013-06-30Active, not recruiting
Clinical Study of the Efficacy of the Ophthalmic Solution of Pazufloxacin 0.6% (PRO-157) for the Treatment of Acute Bacterial Conjunctivitis, Compared to the Ophthalmic Solution of Gatifloxacin 0.3%. [NCT03696342]Phase 346 participants (Actual)Interventional2018-10-01Terminated(stopped due to Sponsor's convenience)
Double-Masked, Randomized, Parallel Group Study for Evaluation of Non-Inferiority of 0.3%Gatifloxacin/1.0% Prednisolone Association Compared With Their Isolated Administration in the Prevention of Ocular Infection/Inflammation After LASIK Surgery [NCT01218737]Phase 3101 participants (Actual)Interventional2009-01-31Completed
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)
Population Pharmacokinetics of Anti-tuberculosis Drugs in Children With Tuberculosis [NCT03625739]800 participants (Anticipated)Observational [Patient Registry]2018-07-01Recruiting
A Randomized, Double Blind, Phase II Multicenter Trial to Evaluate the Safety and Efficacy of PRO-157 Ophthalmic Solution in Three Different Dosing Regimen Versus Moxifloxacin Versus Gatifloxacin in Patients With Bacterial Conjunctivitis. [NCT02980523]Phase 2150 participants (Actual)Interventional2015-03-31Completed
[NCT00414011]40 participants (Actual)InterventionalCompleted
A Single-Center, Randomized, Masked Study Comparing the Concentration of Besifloxacin, Gatifloxacin, and Moxifloxacin in Human Conjunctiva After a Single Topical Instillation [NCT00905762]Phase 1119 participants (Actual)Interventional2009-03-31Completed
[NCT00703313]Phase 472 participants (Anticipated)Interventional2008-05-31Completed
A Randomized Clinical Trial Comparing the Effect of Moxifloxacin Versus Gatifloxacin Following Pterygium Excision on Corneal Epithelial Healing and Epithelial Toxicity. [NCT00892918]40 participants (Anticipated)Interventional2009-06-30Not yet recruiting
Swiss PACK-CXL (Photoactivated Chromophore for Infectious Keratitis Cross-linking) Multicenter Trial for the Treatment of Infectious Keratitis [NCT02717871]Phase 335 participants (Actual)Interventional2016-03-31Completed
Lessdrops™ Prophylactic Treatment After Routine Phacoemulsification Compared to Standard Drops Regimen [NCT03578276]Phase 435 participants (Actual)Interventional2018-06-22Completed
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
Effect of Gatifloxacin 0.3% and Moxifloxacin 0.5% on Epithelial Wound Healing After Photorefractive Keratectomy [NCT00569881]22 participants (Actual)Observational2007-01-31Completed
[NCT00651586]Phase 2129 participants (Actual)Interventional2003-10-31Completed
The Effect of Preoperative Topical Gatifloxacin on Anterior Chamber Sample Cultures After Cataract Surgery. [NCT00335231]0 participants (Actual)Interventional2006-06-30Withdrawn(stopped due to Protocol changes underway. Trial never started)
Randomized, Open-label, Superiority Trial of the Effectiveness of Gatifloxacin Versus Ceftriaxone for the Treatment of Uncomplicated Enteric Fever. [NCT01421693]Phase 4300 participants (Actual)Interventional2011-09-30Completed
[NCT00874887]Phase 466 participants (Actual)Interventional2009-03-31Completed
[NCT00433225]Phase 40 participants InterventionalCompleted
Prospective Randomized Comparison of Zymar(Gatifloxacin) and Vigamox (Moxifloxacin) in Killing Conjunctival Bacterial Flora Following a One-hour [NCT00466570]0 participants (Actual)Interventional2007-04-30Withdrawn
An Open-Label, Randomized Assessment of the Concentrations of Besifloxacin, Moxifloxacin, or Gatifloxacin in the Aqueous Humor of Subjects After a Single Topical Dose [NCT00824070]Phase 1105 participants (Actual)Interventional2009-02-28Completed
Prospective Study Comparing the Effectiveness of Zymar and Vigamox for Preoperative Antibiotic Sterilization of the Ocular Surface After Loading Dose [NCT00347828]Phase 440 participants Interventional2006-06-30Active, not recruiting
[NCT00410891]Phase 4129 participants (Actual)Interventional2008-07-31Completed
A Randomised Open-Label Controlled Trial of a 4-Month Gatifloxacin-Containing Regimen Versus Standard Regimen for the Treatment of Adult Patients With Pulmonary Tuberculosis [NCT00216385]Phase 32,070 participants Interventional2005-01-31Recruiting
[NCT00407017]Phase 40 participants InterventionalCompleted
One Hour Preoperative Gatifloxacin [NCT00350363]Phase 460 participants (Actual)Interventional2007-01-31Completed
[NCT00518089]Phase 3859 participants (Actual)Interventional2008-02-29Completed
[NCT00509873]Phase 3578 participants (Actual)Interventional2007-08-31Completed
[NCT00464438]Phase 4171 participants (Actual)Interventional2007-06-30Completed
A Single-site, Single Masked, Prospective Comparison of Three Fluoroquinolone Topical Therapies (Besifloxacin 0.6% or Gatifloxacin 0.5% or Moxifloxacin 0.5%) in the Treatment of Infectious Corneal Ulcers. [NCT01928693]Phase 22 participants (Actual)Interventional2013-07-31Terminated(stopped due to study terminated due to slow accrual)
Evaluation of the Safety and Efficacy of Topical Besifloxacin Ophthalmic Suspension, 0.6% Compared With Gatifloxacin, 0.3% Ophthalmic Solution for the Treatment of Presumed Bacterial Conjunctivitis in Subjects From Birth to 31 Days of Age [NCT01330355]Phase 333 participants (Actual)Interventional2011-05-31Terminated(stopped due to Lack of enrollment)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00350363 (1) [back to overview]Number of Participant With Positive Culture
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]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]Pharmacokinetic Parameters: Area Under the Curve (AUC) 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]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]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]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)
NCT00410891 (1) [back to overview]Positive Culture
NCT00414011 (1) [back to overview]Corneal Epithelial Healing Time
NCT00464438 (4) [back to overview]Percentage of Patients With Clearing (Clinical Success) of Conjunctival Erythema and Conjunctival Discharge at Day 7
NCT00464438 (4) [back to overview]Percentage of Patients With Improvement in Ocular Signs for Conjunctival Discharge at Day 7
NCT00464438 (4) [back to overview]Percentage of Patients With Improvement in Ocular Signs for Lid Erythema
NCT00464438 (4) [back to overview]Percentage of Patients With Microbiological Improvement
NCT00509873 (5) [back to overview]Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge at Day 6
NCT00509873 (5) [back to overview]Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge Up to Day 6
NCT00509873 (5) [back to overview]Percentage of Patients With Clinical Improvement of Ocular Signs at Day 6
NCT00509873 (5) [back to overview]Percentage of Patients With Clinical Improvement of Ocular Symptoms at Day 6
NCT00509873 (5) [back to overview]Percentage of Patients With Microbiological Cure at Day 6
NCT00518089 (5) [back to overview]Percentage of Patients With Microbiological Cure Up to Day 6
NCT00518089 (5) [back to overview]Percentage of Patients With Clinical Improvement of Ocular Symptoms Up to Day 6
NCT00518089 (5) [back to overview]Percentage of Patients With Clinical Improvement of Ocular Signs Up to Day 6
NCT00518089 (5) [back to overview]Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge Up to Day 6
NCT00518089 (5) [back to overview]Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge at Day 6
NCT00824070 (1) [back to overview]The Aqueous Humor Drug Concentration.
NCT00874887 (1) [back to overview]Percentage of Subjects With Strain Resistance of the Conjunctiva as Determined by Minimum Inhibitory Concentration (MIC) at Day 14
NCT01330355 (4) [back to overview]Microbial Outcome
NCT01330355 (4) [back to overview]Clinical Resolution
NCT01330355 (4) [back to overview]Clinical Resolution
NCT01330355 (4) [back to overview]Microbial Eradication
NCT01928693 (6) [back to overview]Complete Healing
NCT01928693 (6) [back to overview]Healing Rate
NCT01928693 (6) [back to overview]Patient Pain Scores
NCT01928693 (6) [back to overview]Patient Satisfaction Scores
NCT01928693 (6) [back to overview]Scarring
NCT01928693 (6) [back to overview]Number of Participants With Treatment Failure
NCT02980523 (7) [back to overview]Change From Baseline Bacterial Culture
NCT02980523 (7) [back to overview]Number of Cases of Conjunctival Hyperemia
NCT02980523 (7) [back to overview]Eyelid Edema Frequency
NCT02980523 (7) [back to overview]Chemosis Frequency
NCT02980523 (7) [back to overview]Frequency of Corneal Epithelial Defects
NCT02980523 (7) [back to overview]Cases Frequency of Ocular Secretion
NCT02980523 (7) [back to overview]Adverse Events
NCT03578276 (3) [back to overview]Change From Baseline (Preoperative Exam) in Pachymetry (Corneal Thickness)
NCT03578276 (3) [back to overview]Change From Baseline (Preoperative Exam) in Macular Thickness
NCT03578276 (3) [back to overview]Change From Baseline (Preoperative Exam) in Intraocular Pressure (IOP)
NCT03696342 (3) [back to overview]Presence of Clinical Remission Defined as Absence of Hyperemia and Secretion by the Final Visit
NCT03696342 (3) [back to overview]Presence of Bacterial Eradication Compared to Baseline Culture Results
NCT03696342 (3) [back to overview]Adverse Events

Number of Participant With Positive Culture

(NCT00350363)
Timeframe: 2 weeks

Interventionparticipants (Number)
1 Day of Gatifloxacin17

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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

[back to top]

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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Positive Culture

The percentage of patients with a positive bacterial culture following administration of study treatment is presented. (NCT00410891)
Timeframe: Study day 1, assessed following administration of study treatment

Interventionpercentage of patients (Number)
Topical Antibiotic8

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Corneal Epithelial Healing Time

patients' eyes will be observed daily after surgery until the corneal epithelium has completely healed (usually 3 to 4 days) (NCT00414011)
Timeframe: 3 to 4 days after surgery

Interventiondays to complete epithelial healing (Median)
Moxifloxacin4
Gatifloxacin4

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Percentage of Patients With Clearing (Clinical Success) of Conjunctival Erythema and Conjunctival Discharge at Day 7

Percentage of patients that achieved clinical success, defined as a score of 0 for both conjunctival erythema and conjunctival discharge at Day 7. Conjunctival erythema and conjunctival discharge were each assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00464438)
Timeframe: Day 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%78.6
Moxifloxacin 0.5%84.4

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Percentage of Patients With Improvement in Ocular Signs for Conjunctival Discharge at Day 7

"Percentage of patients with at least a 1-grade improvement in ocular signs for conjunctival discharge at Day 7 from Day 1 (Baseline). Conjunctival discharge was assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate,~+3=severe)." (NCT00464438)
Timeframe: Day 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%94.6
Moxifloxacin 0.5%92.2

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Percentage of Patients With Improvement in Ocular Signs for Lid Erythema

Percentage of patients with at least a 1-grade improvement in ocular signs for lid erythema at Day 7 from Day 1 (Baseline). Lid erythema was assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00464438)
Timeframe: Days 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%76.8
Moxifloxacin 0.5%75.0

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Percentage of Patients With Microbiological Improvement

Percentage of patients with microbiological improvement, defined such that all bacteria present above threshold at Day 1 (Baseline) are eradicated (absent) or reduced at Day 7 based on a Classification of Microbial Response (Eradication=pathogen is absent in follow-up culture; Reduction=pathogen is reduced from baseline below threshold count in follow-up culture; Persistence=pathogen reduced from baseline but is above or equal to threshold count in follow-up culture; and Proliferation=pathogen has increased in count from baseline in follow-up culture). (NCT00464438)
Timeframe: Day 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%94.6
Moxifloxacin 0.5%92.2

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Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge at Day 6

Percentage of patients that achieved clinical success, defined as achievement of a score of zero for both conjunctival hyperemia and conjunctival discharge in the study eye at Day 6. Conjunctival hyperemia and conjunctival discharge were each assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00509873)
Timeframe: Day 6

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops74.9
Placebo Eye Drops65.2

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Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge Up to Day 6

"Percentage of patients that achieved clinical success, defined as achievement of a score of zero for both conjunctival hyperemia and conjunctival discharge in the study eye up to Day 6. Conjunctival hyperemia and conjunctival discharge were each assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (Note: The Up to Day 6 analysis included all data up to the Day 6 time point but excluded any Day 6 visit data that was collected after the Day 6 time point)." (NCT00509873)
Timeframe: 6 Days

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops64.1
Placebo Eye Drops50.0

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Percentage of Patients With Clinical Improvement of Ocular Signs at Day 6

Percentage of patients with clinical improvement of ocular signs at Day 6 based on a 4-point scale (0 = none, 1 = mild, 2 = moderate, and 3 = severe), defined as a decrease (improvement) from Day 1 (Baseline) in the total score of conjunctival hyperemia and mucopurulent discharge (pus),with no increase (worsening) from Day 1 (Baseline) in either individual variable in the study eye. (NCT00509873)
Timeframe: Day 6

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops97.0
Placebo Eye Drops96.2

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Percentage of Patients With Clinical Improvement of Ocular Symptoms at Day 6

Percentage of patients with clinical improvement of ocular symptoms at Day 6, defined as a decrease (improvement) from Day 1 (Baseline) in the total score of itching and tearing (each on 4-point scale: 0 = none, 1 = mild, 2 = moderate, and 3 = severe), with no increase (worsening) from Day 1 (Baseline) in any individual score in the study eye diagnosed with bacterial conjunctivitis (NCT00509873)
Timeframe: Day 6

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops85.5
Placebo Eye Drops82.2

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Percentage of Patients With Microbiological Cure at Day 6

Percentage of patients with microbiological cure, defined such that all bacteria present in the study eye at Day 1 (Baseline) are eradicated (or absent) at Day 6 based on a Classification of Microbial Response. (Eradication=pathogen is absent in follow-up culture; Reduction=pathogen is reduced from baseline below threshold count in follow-up culture; Persistence=pathogen reduced from baseline but is above or equal to threshold count in follow-up culture; and Proliferation=pathogen has increased in count from baseline in follow-up culture) (NCT00509873)
Timeframe: Day 6

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops89.2
Placebo Eye Drops61.4

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Percentage of Patients With Microbiological Cure Up to Day 6

Percentage of patients with microbiological cure, defined such that all bacteria present in the study eye at Day 1 (Baseline) are eradicated up to Day 6 based on a Classification of Microbial Response. (Eradication=pathogen is absent in follow-up culture; Reduction=pathogen is reduced from baseline below threshold count in follow-up culture; Persistence=pathogen reduced from baseline but is above or equal to threshold count in follow-up culture; and Proliferation=pathogen has increased in count from baseline in follow-up culture). (NCT00518089)
Timeframe: 6 Days

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops92.2
Placebo Eye Drops80.2

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Percentage of Patients With Clinical Improvement of Ocular Symptoms Up to Day 6

Percentage of patients with clinical improvement of ocular symptoms, defined as a decrease (improvement) up to Day 6 from Day 1 (Baseline) in the total score of itching and tearing (each on 4-point scale: 0 = none, 1 = mild, 2 = moderate, and 3 = severe), with no increase (worsening) from Day 1 (Baseline) in any individual score in the study eye diagnosed with bacterial conjunctivitis. (NCT00518089)
Timeframe: 6 Days

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops92.8
Placebo Eye Drops88.6

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Percentage of Patients With Clinical Improvement of Ocular Signs Up to Day 6

Percentage of patients with clinical improvement of ocular signs up to Day 6 based on a 4-point scale (0 = none, 1 = mild, 2 = moderate, and 3 = severe), defined as a decrease (improvement) from Day 1 (Baseline) in the total score of conjunctival hyperemia and mucopurulent discharge (pus), with no increase (worsening) from Day 1 (Baseline) in either individual variable in the study eye. (NCT00518089)
Timeframe: 6 Days

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops97.0
Placebo Eye Drops92.2

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Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge Up to Day 6

Percentage of patients that achieved clinical success, defined as achievement of a score of zero for both conjunctival hyperemia and conjunctival discharge in the study eye up to Day 6. Conjunctival hyperemia and conjunctival discharge were each assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00518089)
Timeframe: 6 Days

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops51.8
Placebo Eye Drops41.3

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Percentage of Patients With Clearing (Clinical Success) of Conjunctival Hyperemia and Conjunctival Discharge at Day 6

Percentage of patients that achieved clinical success, defined as achievement of a score of zero for both conjunctival hyperemia and conjunctival discharge in the study eye at Day 6. Conjunctival hyperemia and conjunctival discharge were each assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00518089)
Timeframe: Day 6

InterventionPercentage of Patients (Number)
Gatifloxacin 0.5% Eye Drops59.6
Placebo Eye Drops46.7

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The Aqueous Humor Drug Concentration.

An aqueous humor specimen was collected from the study eye for determination of drug concentration 60 min after study drug instillation. (NCT00824070)
Timeframe: Visit 2, 1-14 days following screening visit

Interventionµg/mL (Mean)
Besifloxacin0.1349
Moxifloxacin0.6681
Gatifloxacin0.1251

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Percentage of Subjects With Strain Resistance of the Conjunctiva as Determined by Minimum Inhibitory Concentration (MIC) at Day 14

Percentage of subjects with strain resistance as determined by Minimum Inhibitory Concentration (MIC) of the conjunctiva (clear membrane covering the white surface of the eye) at day 14. MIC is the lowest concentration of an antimicrobial that inhibits the visible growth of a microorganism after incubation. The MIC cut-off values include: Intermediate is 1 to less than 2; Resistant is greater than or equal to 2. (NCT00874887)
Timeframe: Day 14

InterventionPercentage of Subjects (Number)
Vigamox®9.4
Zymar®0

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Microbial Outcome

"Microbial outcome for the following groups of accepted ocular bacterial species that were present at or above threshold at baseline:~over all bacterial species~over all and individual gram-positive bacterial species~over all and individual gram-negative bacterial species" (NCT01330355)
Timeframe: Visit 3 (Day 3) and Visit 5 (Day 8+1)

,
Interventionevents (Number)
Visit 3 (Day 3) Gram-PositiveVisit 3 (Day 3) Gram-NegativeVisit 5 (Day 8) Gram-PositiveVisit 5 (Day8) Gram-Negative
Besivance166176
Gatifloxacin63124

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Clinical Resolution

Clinical resolution defined as the absence of both conjunctival discharge and conjunctival hyperemia. (NCT01330355)
Timeframe: Visit 3 (Day 3)

Interventionparticipants (Number)
Besivance3
Gatifloxacin5

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Clinical Resolution

Clinical resolution defined as the absence of both conjunctival discharge and conjunctival hyperemia. (NCT01330355)
Timeframe: Visit 5 (Day 8+1)

Interventionparticipants (Number)
Besivance12
Gatifloxacin12

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Microbial Eradication

Eradication defined as the absence of all accepted ocular bacterial species (as measured on the ordinal scale) that were present at or above threshold at baseline (NCT01330355)
Timeframe: Visit 5 (Day 8+1)

Interventionparticipants (Number)
Besivance12
Gatifloxacin8

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Complete Healing

The primary outcome will be complete healing of the corneal ulcer, defined as complete reepithelialization by Day 29. (NCT01928693)
Timeframe: 29 days

Interventionparticipant (Number)
Zymaxid 0.5% Ophthalmic Solution1
Vigamox 0.5% Ophthalmic Solution1

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Healing Rate

Time to corneal ulcer reduction and/or total healing over a treatment course of 21 days. (NCT01928693)
Timeframe: 29 days

InterventionDays (Number)
Zymaxid 0.5% Ophthalmic Solution21
Vigamox 0.5% Ophthalmic Solution21

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Patient Pain Scores

Patients will be asked to grade the overall pain of the affected eye at each visit on a Scale= 0--None, 1- Mild, 2- Moderate, 3- Severe (NCT01928693)
Timeframe: Average of 6 times in a 29 day period

Interventionunits on a scale (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution2

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Patient Satisfaction Scores

Patient satisfaction outcomes will be assessed using a series of survey questions ranging in both categorical and continuous outcomes. Treatment will be compared using either methods for differences in binomial proportions or the Wilcoxon Rank Sum test. Scale= 0- Very Comfortable, 1- Comfortable, 2- Uncomfortable, 3- Very Uncomfortable (NCT01928693)
Timeframe: Average of 6 times in a 29 day period

Interventionunits on a scale (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution2

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Scarring

Scarring will be evaluated and measured in millimeters at Day 29 and classified as either peripheral or central. (NCT01928693)
Timeframe: 29 days

Interventionmillimeters (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution0

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Number of Participants With Treatment Failure

(NCT01928693)
Timeframe: 29 days

Interventionparticipants (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution0

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Change From Baseline Bacterial Culture

"Efficacy will be determined comparing the cultures of the lower conjunctival pouch, of the baseline (day 1) against final visit (day 8), quantifying and identifying the colony forming units (CFU) by genus and species.~The evaluated variable is discrete quantitative type and the scale of measurement used will be CFU x mL considering the eradication, reduction or proliferation of the bacterial agent. It will be determined as effective if there is a reduction in number of bacterial flora in at least 95% of the evaluated subjects." (NCT02980523)
Timeframe: up to one week

,,,,
Interventioncultures (Number)
basal cultures positivesfinal cultures negatives
Gatifloxacin (Zymar®)1715
Moxifloxacin (Vigamox®)2928
PRO-157 BID (2 Times Per Day)3017
PRO-157 QID (4 Times Per Day)2616
PRO-157 TID (3 Times Per Day)1614

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Number of Cases of Conjunctival Hyperemia

Conjunctival hyperemia: qualitative ordinal variable. The conjunctival hyperemia was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group. (NCT02980523)
Timeframe: up to one week

Interventionhyperemia cases reported (Number)
PRO-157 BID (2 Times Per Day)17
PRO-157 TID (3 Times Per Day)1
PRO-157 QID (4 Times Per Day)5
Moxifloxacin (Vigamox®)7
Gatifloxacin (Zymar®)8

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Eyelid Edema Frequency

"Eyelid edema: qualitative ordinal variable, measurement scale absent or present.Between baseline (day 0) versus final visit (day 7).~The eyelid edema was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group." (NCT02980523)
Timeframe: Up to one week

Interventioneyelid edema cases reported (Number)
PRO-157 BID (2 Times Per Day)6
PRO-157 TID (3 Times Per Day)0
PRO-157 QID (4 Times Per Day)4
Moxifloxacin (Vigamox®)4
Gatifloxacin (Zymar®)6

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Chemosis Frequency

Chemosis: qualitative ordinal variable, measurement scale absent or present. The chemosis was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group. (NCT02980523)
Timeframe: up to one week

Interventionchemosis cases reported (Number)
PRO-157 BID (2 Times Per Day)0
PRO-157 TID (3 Times Per Day)0
PRO-157 QID (4 Times Per Day)0
Moxifloxacin (Vigamox®)6
Gatifloxacin (Zymar®)2

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Frequency of Corneal Epithelial Defects

"Corneal epithelial defects: qualitative ordinal variable, measurement scale present or absent.~The corneal epithelial defects was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group." (NCT02980523)
Timeframe: Up to one week

InterventionCorneal defects cases reported (Number)
PRO-157 BID (2 Times Per Day)9
PRO-157 TID (3 Times Per Day)4
PRO-157 QID (4 Times Per Day)6
Moxifloxacin (Vigamox®)5
Gatifloxacin (Zymar®)5

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Cases Frequency of Ocular Secretion

Secretion ocular: qualitative ordinal variable. The secretion was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group. (NCT02980523)
Timeframe: Up to one week.

Interventionsecretion cases reported (Number)
PRO-157 BID (2 Times Per Day)0
PRO-157 TID (3 Times Per Day)3
PRO-157 QID (4 Times Per Day)0
Moxifloxacin (Vigamox®)7
Gatifloxacin (Zymar®)2

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Adverse Events

Number of adverse events: dependent variable, discrete quantitative, the number of adverse events per group will be compared at the end of the study and it will be considered safe if there is not greater increase of 5% of serious adverse events. (NCT02980523)
Timeframe: during the intervention period for 7 days, and 15 days after the final visit

Interventionevents (Number)
PRO-157 BID (2 Times Per Day)7
PRO-157 TID (3 Times Per Day)5
PRO-157 QID (4 Times Per Day)7
Moxifloxacin (Vigamox®)4
Gatifloxacin (Zymar®)7

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Change From Baseline (Preoperative Exam) in Pachymetry (Corneal Thickness)

Thickness of the cornea measured in microns, measured as the change from baseline (NCT03578276)
Timeframe: Month 1

Interventionmicrons (Mean)
LessDrops3.18
Standard of Care0.63

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Change From Baseline (Preoperative Exam) in Macular Thickness

Thickness of the macula measured in microns, recorded as the change from baseline. (NCT03578276)
Timeframe: Month 1

Interventionmicrons (Mean)
LessDrops4.91
Standard of Care1.30

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Change From Baseline (Preoperative Exam) in Intraocular Pressure (IOP)

Measurement of the pressure inside the eye in mmHg, recorded as the change from baseline (NCT03578276)
Timeframe: Month 1

InterventionmmHg (Mean)
LessDrops-0.33
Standard of Care-0.21

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Presence of Clinical Remission Defined as Absence of Hyperemia and Secretion by the Final Visit

"The clinical remission in the visits will be evaluated as Yes or No, to report Yes it must have a grade of 0 in conjunctival hyperemia and 0 in secretion; otherwise, you must report as No." (NCT03696342)
Timeframe: will be evaluated at the end of the treatment (day 8, final visit)

InterventionParticipants (Count of Participants)
PRO-15715
Zymar19

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Presence of Bacterial Eradication Compared to Baseline Culture Results

The conjunctival secretion sample will be taken prior to the instillation of any medication, the result of the basal crop will be compared against the results of the final crop and the absence of bacterial species that were present in the culture of the baseline visit is considered bacterial eradication. (NCT03696342)
Timeframe: will be evaluated at the end of the treatment (day 8, final visit)

InterventionParticipants (Count of Participants)
PRO-15719
Zymar22

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Adverse Events

The evaluation of adverse events requires a questioning conducted by the principal investigator and the appropriate exploratory techniques for its detection. the number of adverse events per study group will be considered for the analysis (NCT03696342)
Timeframe: day 0 to day 17 (visit 0 to security call)

,
Interventionnumber of adverse events (Number)
Mild Adverse EventModerate Adverse Event
PRO-157250
Zymar272

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