Page last updated: 2024-12-07

garenoxacin

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Description

garenoxacin: a des-fluoro(6) quinolone with antibacterial activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

garenoxacin : A quinolinemonocarboxylic acid that is 1,4-dihydroquinoline-3-carboxylic acid that is substituted by a cyclopropyl group at position 1, an oxo group at position 4, a (1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl group at position 7, and a difluoromethoxy group at position 8. [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 CID124093
CHEMBL ID215303
CHEBI ID131716
SCHEMBL ID2103727
MeSH IDM0378262

Synonyms (50)

Synonym
t-3811
1-cyclopropyl-8-(difluoromethoxy)-7-[(1r)-1-methylisoindolin-5-yl]-4-oxo-quinoline-3-carboxylic acid
t 3811
1-cyclopropyl-8-(difluoromethoxy)-7-[(1r)-(1-methyl-2,3-dihydro-1h-5-isoindolyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
t-3811mea
garenoxacin
bms-284756 (*mesylate salt*)
bms 284756 (*mesylate salt*)
CHEMBL215303
1-cyclopropyl-8-(difluoromethoxy)-7-[(1r)-1-methyl-2,3-dihydro-1h-isoindol-5-yl]-4-oxoquinoline-3-carboxylic acid
garenoxacine
194804-75-6
bms284756
CHEBI:131716
garenoxacino
garenoxacinum
AKOS015920281
BCP9000709
v72h9867wb ,
garenoxacin [inn:ban]
unii-v72h9867wb
194804-75-6 pound not223652-90-2
BCPP000224
S5908
(r)-1-cyclopropyl-8-(difluoromethoxy)-7-(1-methylisoindolin-5-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
1-cyclopropyl-8-(difluoromethoxy)-7-[(1r)-2,3-dihydro-1-methyl-1h-isoindol-5-yl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
ganefloxacin
(r)-1-cyclopropyl-8-difluoromethoxy-7-(1-methyl-2, 3-dihydro-1h-5-isoindolyl)-4-oxo-1, 4-dihydro-3-quinolinecarboxylic acid
(r)-1-cyclopropyl-8-difluoromethoxy-7-(1-methyl-2,3-dihydro-1h-5-isoindolyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
(r)-1-cyclopropyl-8-difluoromethoxy-7-(1-methyl-2,3-dihydro-1h-5-isoindolyl)-4-oxo-1,4-dihydro-3-quinoline-carboxylic acid
garenoxacin [mi]
garenoxacin [who-dd]
garenoxacin [mart.]
garenoxacin [inn]
CS-4989
garenfloxacin
SCHEMBL2103727
HY-17460
DTXSID30173135
J-521409
bdbm50481219
J-012614
Q3758306
DB06160
BCP01415
EX-A3040
A16856
AMY8881
1-cyclopropyl-8-(difluoromethoxy)-7-[(1r)-1-methyl-2,3-dihydro-1h-isoindol-5-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
gtpl12402

Research Excerpts

Overview

Garenoxacin is a fluoroquinolone against respiratory infections, not against urethritis in Japan. Its in-vitro antimicrobial activity against MG is known as similar to or higher than that of moxifloxacins. Garenoxa is a novel des-F(6) quinolone with a broad antimicrobial spectrum.

ExcerptReferenceRelevance
"Garenoxacin mesylate is a novel des-fluoro(6) quinolone, approved and marketed for human use in Japan under the name Geninax."( QbD-Based Development and Validation of Novel Stability-Indicating Method for the Assay and Dissolution of Garenoxacin in Garenoxacin Tablets.
Azhakesan, A; Kuppusamy, S, 2022
)
2.38
"Garenoxacin (GRNX) is a fluoroquinolone against respiratory infections, not against urethritis in Japan, but its in-vitro antimicrobial activity against MG is known as similar to or higher than that of moxifloxacin."( The clinical efficacy of garenoxacin for male non-gonococcal urethritis.
Egawa, S; Endo, K; Hosobe, T; Ito, S; Kiyota, H; Onodera, S; Shiono, Y; Yamada, H, 2020
)
1.58
"Garenoxacin is a type of fluoroquinolone antibacterial agents. "( Pharmacokinetic study of garenoxacin in severe renal failure patients.
Hagihara, M; Hamada, Y; Imai, H; Kimura, Y; Mikamo, H; Yamagishi, Y, 2015
)
2.16
"Garenoxacin is a des-(6)-fluoroquinolone exhibiting a comparatively low chondrotoxic potential in juvenile animals. "( Ultrastructural changes induced by the des-F(6)-quinolone garenoxacin (BMS-284756) and two fluoroquinolones in Achilles tendon from immature rats.
Shakibaei, M; Stahlmann, R, 2003
)
2.01
"Garenoxacin is a new des-F(6)-quinolone with a broad antimicrobial spectrum. "( Effect of garenoxacin on eubacteria in the normal intestinal microflora when administered concomitantly with digoxin.
Bello, A; Gajjar, DA; Grasela, DM; Meurling, L; Nord, CE; Russo, RL, 2003
)
2.16
"Garenoxacin is a novel des-F(6)-quinolone with good anti-anaerobe activity. "( Accumulation of garenoxacin by Bacteroides fragilis compared with that of five fluoroquinolones.
Piddock, L; Ricci, V, 2003
)
2.11
"Garenoxacin is a novel des-F(6)quinolone that has shown excellent antimicrobial activity against a wide range of clinically important microorganisms. "( Comparative activity of garenoxacin and other agents by susceptibility and time-kill testing against Staphylococcus aureus, Streptococcus pyogenes and respiratory pathogens.
Esposito, S; Ianniello, F; Leone, S; Noviello, S, 2003
)
2.07
"Garenoxacin is a novel quinolone that does not have a fluorine substituent at the C-6 position in the quinoline ring. "( Metabolism and disposition of novel des-fluoro quinolone garenoxacin in experimental animals and an interspecies scaling of pharmacokinetic parameters.
Fukumoto, H; Fukushima, Y; Hayakawa, H; Kadota, T; Kato, H; Kuroiwa, H; Nishigaki, J; Tsuji, A; Yamamoto, H, 2003
)
2.01
"Garenoxacin is a new des-F(6)-quinolone with broad-spectrum activity against both gram-positive cocci and gram-negative bacilli. "( Pharmacodynamics of the new des-f(6)-quinolone garenoxacin in a murine thigh infection model.
Andes, D; Craig, WA, 2003
)
2.02
"Garenoxacin is a des-F(6)-quinolone with a broad antibacterial spectrum, which has previously been shown to exhibit low chondrotoxicity in juvenile dogs compared with several other quinolones. "( Concentrations of the des-F(6)-quinolone garenoxacin in plasma and joint cartilage of immature rats.
Baumann-Wilschke, I; Bello, A; Kastner, M; Rahm, U; Stahlmann, R, 2004
)
2.03
"Garenoxacin is a novel des-F(6) quinolone with enhanced in vitro activities against both gram-positive and gram-negative bacteria. "( Activities of garenoxacin against quinolone-resistant Streptococcus pneumoniae strains in vitro and in a mouse pneumonia model.
Azoulay-Dupuis, E; Bédos, JP; Cherbuliez, C; Fantin, B; Isturiz, R; Köhler, T; Mohler, J; Moine, P; Péchère, JC; Peytavin, G; Rieux, V, 2004
)
2.13
"Garenoxacin appears to be a widely usable and highly active agent against S."( Bactericidal activity of garenoxacin tested by kill-curve methodology against wild type and QRDR mutant strains of Streptococcus pneumoniae.
Anderegg, TR; Jones, RN, 2004
)
1.35
"Garenoxacin is a novel des-F(6)-quinolone with a chemical structure that lacks the C6 position fluorine and has a unique difluoromethoxy substitution at position C8. "( In vitro activity of garenoxacin tested against a worldwide collection of ciprofloxacin-susceptible and ciprofloxacin-resistant Enterobacteriaceae strains (1999-2004).
Fritsche, TR; Jones, RN; Sader, HS, 2007
)
2.1
"Garenoxacin appears to be a welcome addition to the CAP treatment options, particularly for the emerging MDR pneumococci strains."( Garenoxacin activity against isolates form patients hospitalized with community-acquired pneumonia and multidrug-resistant Streptococcus pneumoniae.
Fritsche, TR; Jones, RN; Sader, HS; Stilwell, MG, 2007
)
2.5
"Garenoxacin is a novel des-F(6)-quinolone that exhibits broad-spectrum activity against a wide range of aerobic and anaerobic pathogens of clinical importance. "( Tissue and fluid penetration of garenoxacin in surgical patients.
Edmiston, CE; Gajjar, DA; Johnson, CP; Krepel, CJ; Krishna, G; Loehrl, TA; Otterson, MF; Seabrook, GR; Smith, TL; Towne, JB; Wackym, PA, 2007
)
2.07
"Garenoxacin is a des-F(6)-quinolone with broad-spectrum antimicrobial activity and a favorable pharmacokinetic/pharmacodynamic profile."( Retrospective analysis of electrocardiographic changes after administration of oral or intravenous garenoxacin in five phase I, placebo-controlled studies in healthy volunteers.
Grasela, DM; Krishna, G; Wang, Z, 2007
)
1.28
"Garenoxacin is a des-F(6)-quinolone with in vitro activity against key respiratory pathogens, including Streptococcus pneumoniae, Hemophilus influenzae, Staphylococcus aureus, and Moraxella catarrhalis. "( Oral garenoxacin in the treatment of acute bacterial maxillary sinusitis: a Phase II, multicenter, noncomparative, open-label study in adult patients undergoing sinus aspiration.
Kostrica, R; Lopez Sisniega, J; Profant, M; Waskin, H, 2007
)
2.3

Effects

Garenoxacin (GRNX) has been reported to be more effective than LVFX against gram-positive bacteria especially Streptococcus pneumoniae. No studies have compared the effectiveness of LVFX and GRNX.

ExcerptReferenceRelevance
"Garenoxacin (GRNX) has been reported to be more effective than LVFX against gram-positive bacteria especially Streptococcus pneumoniae."( [Comparison of garenoxacin and levofloxacin for the prophylaxis of febrile neutropenia].
Fujita, S; Hata, A; Kaji, R; Katakami, N; Kitajima, N; Masuda, Y; Ose, T; Takashima, K; Takeshita, J; Tanaka, K, 2014
)
1.48
"Garenoxacin (GRNX), which has been investigated in Japan, has stronger antibacterial activity than LVFX against gram-positive bacteria; however, no studies have compared the effectiveness of LVFX and GRNX."( Comparison of levofloxacin and garenoxacin for antibacterial prophylaxis during neutropenia.
Akahoshi, Y; Ashizawa, M; Ishihara, Y; Kako, S; Kanda, J; Kanda, Y; Kawamura, K; Kikuchi, M; Kimura, SI; Machishima, T; Nakano, H; Nakasone, H; Nishida, J; Sakamoto, K; Sato, M; Terasako-Saito, K; Ugai, T; Wada, H; Yamasaki, R; Yamazaki, R, 2017
)
1.46

Toxicity

Garenoxacin injected intravitreally appeared safe at concentrations of < or =4,000 microg/0. These results suggest that garenxacin is a highly effective and safe antimicrobial agent in the treatment of upper respiratory infections.

ExcerptReferenceRelevance
"Garenoxacin injected intravitreally appeared safe at concentrations of < or =4,000 microg/0."( Intravitreal toxicity of garenoxacin.
Aydin, E; Dellacroce, JT; Esfahani, MR; Kazi, AA; Peyman, GA, 2006
)
2.08
" There were 8 adverse events (8."( Efficacy and safety of garenoxacin in the treatment of upper respiratory tract infections.
Hatano, M; Ito, M; Kondo, S; Maruyama, Y; Miwa, T; Murono, S; Nakanishi, S; Wakisaka, N; Yoshizaki, T, 2012
)
0.69
"These results suggest that garenoxacin is a highly effective and safe antimicrobial agent in the treatment of community-acquired upper respiratory infections."( Efficacy and safety of garenoxacin in the treatment of upper respiratory tract infections.
Hatano, M; Ito, M; Kondo, S; Maruyama, Y; Miwa, T; Murono, S; Nakanishi, S; Wakisaka, N; Yoshizaki, T, 2012
)
0.99
" There were few differences in the frequency of adverse effects between the two groups."( Effectiveness and safety of the pre-prescription of garenoxacin in comparison to moxifloxacin for low-risk febrile neutropenia in breast cancer patients undergoing adjuvant and neoadjuvant chemotherapy.
Asano, Y; Kashiwagi, S; Nagayama, K; Noda, S; Ogawa, K; Ohira, M; Onoda, N; Takahashi, K; Takahashi, M; Takashima, T, 2019
)
0.76
" No significant differences were observed in the incidence rates of drug-related adverse events between the sitafloxacin (20."( The efficacy and safety of sitafloxacin and garenoxacin for the treatment of pneumonia in elderly patients: A randomized, multicenter, open-label trial.
Fukuda, Y; Fukushima, K; Hashiguchi, K; Higashiyama, Y; Imamura, Y; Inoue, Y; Izumikawa, K; Kobayashi, T; Koga, H; Kohno, S; Kondo, A; Mikushi, S; Miyazaki, T; Morinaga, Y; Mukae, H; Nagayoshi, Y; Nakamura, S; Saijo, T; Sasaki, E; Takazono, T; Yamamoto, K; Yanagihara, K; Yoshida, M, 2019
)
0.78

Pharmacokinetics

The bactericidal activity and resistance selectivity of garenoxacin against Streptococcus pneumoniae with mutations in ParC (S79F) or both GyrA (S81F) and ParC were investigated using in vitro pharmacokinetic models. The mean elimination half-life for garen Oxacin in plasma appeared to be independent of dose.

ExcerptReferenceRelevance
" The mean peak concentration in plasma of 10."( Single-dose pharmacokinetics and penetration of BMS 284756 into an inflammatory exudate.
Andrews, JM; Gee, T; Marshall, G; Wise, R, 2002
)
0.31
" The objective of this study was to define the pharmacodynamic profile of BMS-284756 against Streptococcus pneumoniae."( Pharmacodynamics of a novel des-F(6)-quinolone, BMS-284756, against Streptococcus pneumoniae in the thigh infection model.
Banevicius, M; Mattoes, HM; Nicolau, DP; Nightingale, CH; Xuan, D, 2003
)
0.32
" The mean elimination half-life for garenoxacin in plasma appeared to be independent of dose and ranged from 13."( Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects.
Bello, A; Christopher, L; Gajjar, DA; Ge, Z; Grasela, DM, 2003
)
0.85
" Metabolic profiles and pharmacokinetic parameters were investigated focusing on the species differences and the allometric scaling of pharmacokinetic parameters."( Metabolism and disposition of novel des-fluoro quinolone garenoxacin in experimental animals and an interspecies scaling of pharmacokinetic parameters.
Fukumoto, H; Fukushima, Y; Hayakawa, H; Kadota, T; Kato, H; Kuroiwa, H; Nishigaki, J; Tsuji, A; Yamamoto, H, 2003
)
0.56
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
"The pharmacodynamic parameter that best correlates with bacteriological eradication for fluoroquinolones is the free (f) area under the 24 h serum concentration curve (AUC24) to MIC (fAUC24/MIC) ratio."( Pharmacodynamic activity of garenoxacin against ciprofloxacin-resistant Streptococcus pneumoniae.
Derkatch, S; Hoban, DJ; James, J; Laing, N; Noreddin, AM; Zhanel, GG, 2006
)
0.63
" The in vitro pharmacodynamic model was inoculated with 1 x 10(6) cfu/mL and garenoxacin was dosed once daily at 0 and 24 h to simulate fAUC24 and t1/2 obtained after standard oral doses in healthy volunteers (400 mg once daily, free AUC24 20 mg."( Pharmacodynamic activity of garenoxacin against ciprofloxacin-resistant Streptococcus pneumoniae.
Derkatch, S; Hoban, DJ; James, J; Laing, N; Noreddin, AM; Zhanel, GG, 2006
)
0.86
"Plasma and urine or dialysate samples were analyzed for garenoxacin, and single-dose pharmacokinetic parameters were estimated."( Garenoxacin pharmacokinetics in subjects with renal impairment.
Gajjar, D; Grasela, DM; Krishna, G; Marbury, T; Swan, S; Wang, Z, 2007
)
2.03
" The terminal half-life was prolonged in subjects with severe renal impairment compared with healthy controls (26."( Garenoxacin pharmacokinetics in subjects with renal impairment.
Gajjar, D; Grasela, DM; Krishna, G; Marbury, T; Swan, S; Wang, Z, 2007
)
1.78
"This study used Monte Carlo simulations to assess the potential for attainment of pharmacodynamic targets with the fluoroquinolones garenoxacin, gemifloxacin, and moxifloxacin against Streptococcus pneumoniae in serum and epithelial lining fluid (ELF) from hospitalized patients with community-acquired pneumonia (CAP)."( Comparative pharmacodynamics of garenoxacin, gemifloxacin, and moxifloxacin in community-acquired pneumonia caused by Streptococcus pneumoniae: a Monte Carlo simulation analysis.
Hoban, DJ; Noreddin, AM; Ostroski, M; Reese, AA; Zhanel, GG, 2007
)
0.83
"Data on the free AUC over 24 hours (fAUC(0-24)), a measure of drug exposure, were derived from previously described population pharmacokinetic models for therapeutic doses of the 3 fluoroquinolones."( Comparative pharmacodynamics of garenoxacin, gemifloxacin, and moxifloxacin in community-acquired pneumonia caused by Streptococcus pneumoniae: a Monte Carlo simulation analysis.
Hoban, DJ; Noreddin, AM; Ostroski, M; Reese, AA; Zhanel, GG, 2007
)
0.62
" Plasma GRNX concentrations were determined and pharmacokinetic parameters were estimated by Bayesian predictions using reported population pharmacokinetic parameters."( Pharmacokinetics of garenoxacin in elderly patients with respiratory tract infections.
Fujiuchi, S; Kishino, S; Morita, K; Ohsaki, Y; Okumura, S; Takeda, H, 2010
)
0.68
"The bactericidal activity and resistance selectivity of garenoxacin against Streptococcus pneumoniae with mutations in ParC (S79F) or both GyrA (S81F) and ParC (D83Y and K137N) were investigated using in vitro pharmacokinetic models simulating plasma concentrations for a standard clinical regimen [400mg once daily (q."( In vitro pharmacodynamic evaluation of garenoxacin against quinolone-resistant Streptococcus pneumoniae.
Fukuda, Y; Nomura, N; Shinmura, Y; Sugiura, Y; Takahata, M, 2012
)
0.89
" By measuring blood concentration of garenoxacin, pharmacodynamics parameters, such as the peak plasma concentration (C(max)) and the area under the concentration curve (AUC), were calculated with NONMEM."( Pharmacokinetic study of garenoxacin in severe renal failure patients.
Hagihara, M; Hamada, Y; Imai, H; Kimura, Y; Mikamo, H; Yamagishi, Y, 2015
)
0.99

Bioavailability

The relative bioavailability of garenoxacin was not affected by administration as crushed tablets, regardless of enteral feeding. The low chondrotoxicity in comparison with other quinolones is unlikely to be explained by differences in the pharmacokinetics of these compounds.

ExcerptReferenceRelevance
" Garenoxacin was well absorbed following oral administration then underwent phase II metabolism in all species tested."( Metabolism and disposition of novel des-fluoro quinolone garenoxacin in experimental animals and an interspecies scaling of pharmacokinetic parameters.
Fukumoto, H; Fukushima, Y; Hayakawa, H; Kadota, T; Kato, H; Kuroiwa, H; Nishigaki, J; Tsuji, A; Yamamoto, H, 2003
)
1.47
" Since garenoxacin appeared to be well absorbed following oral administration and concentrations in cartilage tended to be higher than those in plasma, it is unlikely that the low chondrotoxicity in comparison with other quinolones is explained by differences in the pharmacokinetics of these compounds."( Concentrations of the des-F(6)-quinolone garenoxacin in plasma and joint cartilage of immature rats.
Baumann-Wilschke, I; Bello, A; Kastner, M; Rahm, U; Stahlmann, R, 2004
)
1.04
" The current study was conducted to assess whether the bioavailability of garenoxacin was affected by administration as crushed tablets with and without concomitant enteral nutrition."( Nasogastric administration of garenoxacin as crushed tablets with and without concomitant enteral feeding in healthy subjects.
Grasela, D; Krishna, G; Noveck, R; Vargas, R; Wang, Z, 2007
)
0.86
"25, suggesting that the bioavailability of garenoxacin was not affected by delivery of crushed tablets via NG tube, regardless of concomitant enteral feeding, compared with oral delivery of intact tablets."( Nasogastric administration of garenoxacin as crushed tablets with and without concomitant enteral feeding in healthy subjects.
Grasela, D; Krishna, G; Noveck, R; Vargas, R; Wang, Z, 2007
)
0.89
"The relative bioavailability of garenoxacin was not affected by administration as crushed tablets, regardless of enteral feeding."( Nasogastric administration of garenoxacin as crushed tablets with and without concomitant enteral feeding in healthy subjects.
Grasela, D; Krishna, G; Noveck, R; Vargas, R; Wang, Z, 2007
)
0.91
"The effect of coadministration of omeprazole on the bioavailability of oral garenoxacin was evaluated in an open-label study in 14 healthy subjects."( The effect of omeprazole on the bioavailability and safety of garenoxacin in healthy volunteers.
Grasela, DM; Kisicki, JC; Krishna, G; Olsen, S; Wang, Z, 2007
)
0.81
" Pharmacokinetic parameters such as oral clearance, oral volume of distribution of the central compartment, time to reach maximum plasma concentration, absorption rate constant, and half-life in humans were predicted from animals using allometric scaling."( Prediction of Plasma Concentration-time Profiles of Drugs in Humans from Animals Following Oral Administration: An Allometric Approach.
Mahmood, I, 2016
)
0.43

Dosage Studied

This was a retrospective analysis of 5 randomized, double-blind, placebo-controlled studies. 224 healthy volunteers received oral or intravenous garenoxacin (50-1200 mg/d) for 1 to 28 days' dosing duration. Population pharmacokinetic/pharmacodynamic (PK/PD) modeling and Monte Carlo simulations were used to optimize dosage regimens.

ExcerptRelevanceReference
" Eight subjects were assigned to each of five dose panels (100, 200, 400, 800 and 1200 mg BMS-284756) and received daily oral dosing with either BMS-284756 (n = 6) or placebo (n = 2) for 14 days."( Ecological impact of the des-F(6)-quinolone, BMS-284756, on the normal intestinal microflora.
Gajjar, DA; Grasela, DM; Nord, CE, 2002
)
0.31
" Its spectrum remains equivalent only if dosing schedules substantiate a proposed susceptible breakpoint of < or =4 mg/L."( Comparative antimicrobial spectrum and activity of the desfluoroquinolone BMS284756 (T-3811) tested against non-fermentative Gram-negative bacilli.
Biedenbach, DJ; Howard, W; Jones, RN, 2002
)
0.31
" Sixteen hours after inoculation, therapy was given by intravenous administration of BMS at 20 mg/kg of body weight, followed 5 h later by administration at a dosage of 10 mg/kg (n = 9 animals) or MOX as two doses of 20 mg/kg every 5 h (n = 8 animals)."( Garenoxacin (BMS-284756) and moxifloxacin in experimental meningitis caused by vancomycin-tolerant pneumococci.
Barton, T; Bowlware, K; Hardy, RD; Iglehart, J; Katz, K; McCoig, CC; McCracken, GH; Michelow, IC; Rodriguez-Cerrato, V; Saavedra, J, 2003
)
1.76
" The corresponding values for the geometric mean area under the concentration-time curve over the dosing interval (AUC(tau)) for garenoxacin in plasma at the 100- and 1200-mg doses were within the ranges of 11."( Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects.
Bello, A; Christopher, L; Gajjar, DA; Ge, Z; Grasela, DM, 2003
)
0.78
"7) CFU of Streptococcus pneumoniae strain ATCC 10813 or Staphylococcus aureus strain ATCC 33591 per thigh when they were treated for 24 h with garenoxacin at a dose of 4 to 128 mg/kg/day fractionated for 3-, 6-, 12-, and 24-hour dosing regimens."( Pharmacodynamics of the new des-f(6)-quinolone garenoxacin in a murine thigh infection model.
Andes, D; Craig, WA, 2003
)
0.78
" Additional groups of rats were orally dosed with 600 mg/kg ofloxacin and ciprofloxacin."( Concentrations of the des-F(6)-quinolone garenoxacin in plasma and joint cartilage of immature rats.
Baumann-Wilschke, I; Bello, A; Kastner, M; Rahm, U; Stahlmann, R, 2004
)
0.59
"The emergence of resistance to antibiotics is a serious problem often related to suboptimal drug dosing; such suboptimal dosing results in the preferential killing of drug-susceptible microbial subpopulations, allowing amplification of drug-resistant microbial subpopulations."( Bacterial-population responses to drug-selective pressure: examination of garenoxacin's effect on Pseudomonas aeruginosa.
Deziel, MR; Drusano, GL; Leary, R; Liu, W; Louie, A; Tam, VH, 2005
)
0.56
" pneumoniae, MPC results were below susceptible breakpoints and within clinically achievable and sustainable drug concentrations for >24 hours of the dosing interval against."( Comparison of the minimum inhibitory, mutant prevention and minimum bactericidal concentrations of ciprofloxacin, levofloxacin and garenoxacin against enteric Gram-negative urinary tract infection pathogens.
Blondeau, JM; Hansen, GT, 2005
)
0.53
" The in vitro pharmacodynamic model was inoculated with 1 x 10(6) cfu/mL and garenoxacin was dosed once daily at 0 and 24 h to simulate fAUC24 and t1/2 obtained after standard oral doses in healthy volunteers (400 mg once daily, free AUC24 20 mg."( Pharmacodynamic activity of garenoxacin against ciprofloxacin-resistant Streptococcus pneumoniae.
Derkatch, S; Hoban, DJ; James, J; Laing, N; Noreddin, AM; Zhanel, GG, 2006
)
0.86
"This was a retrospective analysis of 5 randomized, double-blind, placebo-controlled studies in which 224 healthy volunteers received oral or intravenous garenoxacin (50-1200 mg/d) for 1 to 28 days' dosing duration (( Retrospective analysis of electrocardiographic changes after administration of oral or intravenous garenoxacin in five phase I, placebo-controlled studies in healthy volunteers.
Grasela, DM; Krishna, G; Wang, Z, 2007
)
0.75
" Population pharmacokinetic/pharmacodynamic (PK/PD) modeling and Monte Carlo simulations were used to optimize garenoxacin dosage regimens."( Optimal dose finding of garenoxacin based on population pharmacokinetics/pharmacodynamics and Monte Carlo simulation.
Nozawa, K; Tanigawara, Y; Tsuda, H, 2012
)
0.9
" We were able to show that the optimal garenoxacin dosage regimens were successfully determined using prospective population PK/PD analysis and clinical trial simulations."( Optimal dose finding of garenoxacin based on population pharmacokinetics/pharmacodynamics and Monte Carlo simulation.
Nozawa, K; Tanigawara, Y; Tsuda, H, 2012
)
0.96
" In this case, the drug-exposure AUC, exposure concentration × 24 μg h/ml, was 64-128 % for GRNX and 121 % for LVFX of free AUC at the clinical dosage in humans, respectively."( Bactericidal activity of garenoxacin against in vitro biofilm formed by nontypeable Haemophilus influenzae.
Fukuda, Y; Nomura, N; Shinmura, Y; Sugiura, Y; Takahata, M, 2013
)
0.69
" The effect of garenoxacin mesylate API particle size in the tablet dosage form was studied using particles of 92 µm and 220 µm [90% of the total particles are smaller than this size (D90)] and it was found that there was no impact on the in vitro dissolution profile."( QbD-Based Development and Validation of Novel Stability-Indicating Method for the Assay and Dissolution of Garenoxacin in Garenoxacin Tablets.
Azhakesan, A; Kuppusamy, S, 2022
)
1.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
[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 (6)

ClassDescription
quinolone antibioticAn organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.
quinolinemonocarboxylic acidAny aromatic carboxylic acid that contains a quinoline moiety that is substituted by one carboxy substituent.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
cyclopropanesCyclopropane and its derivatives formed by substitution.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
isoindoles
[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 (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GLS proteinHomo sapiens (human)Potency12.58930.35487.935539.8107AID624170
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (246)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID560149Antibacterial activity against Helicobacter pylori clinical isolates harboring gyrA gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Sitafloxacin activity against Helicobacter pylori isolates, including those with gyrA mutations.
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.
AID559208Antibacterial activity against Streptococcus pneumoniae S0012009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
AID1398606Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
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.
AID1557288Antibacterial activity against Clostridium perfringens by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1557281Antibacterial activity against Klebsiella by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
AID728913Antibacterial activity against Mycoplasma pneumoniae 18-1 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
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.
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.
AID560147Antibacterial activity against Helicobacter pylori clinical isolates harboring gyrA Asp91 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Sitafloxacin activity against Helicobacter pylori isolates, including those with gyrA mutations.
AID559216Antibacterial activity against Streptococcus pneumoniae S001 assessed as resistant isolates with ParC79 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559229Antibacterial activity against Streptococcus pneumoniae S002 assessed as resistant isolates with GyrA81 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID279555Antibacterial activity against ciprofloxacin-resistant methicillin-resistant Staphylococcus aureus by broth macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
The relationship between quinolone exposures and resistance amplification is characterized by an inverted U: a new paradigm for optimizing pharmacodynamics to counterselect resistance.
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.
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.
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.
AID559209Antibacterial activity against Streptococcus pneumoniae S0022009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
AID559226Antibacterial activity against Streptococcus pneumoniae W001 assessed as resistant isolates with GyrA81 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
AID559206Antibacterial activity against Streptococcus pneumoniae W0012009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID560146Antibacterial activity against Helicobacter pylori clinical isolates harboring gyrA Asn87 mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Sitafloxacin activity against Helicobacter pylori isolates, including those with gyrA mutations.
AID1427527Effective permeability of the compound at pH 7.4 after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
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.
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.
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.
AID560148Antibacterial activity against Helicobacter pylori clinical isolates harboring mutation in gyrA gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Sitafloxacin activity against Helicobacter pylori isolates, including those with gyrA mutations.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
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.
AID1557285Antibacterial activity against Streptococcus pneumoniae by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
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.
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
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?
AID559220Antibacterial activity against Streptococcus pneumoniae W002 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID456042Antibacterial activity against levofloxacin, 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.
AID559221Antibacterial activity against Streptococcus pneumoniae S002 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID279553Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by broth macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
The relationship between quinolone exposures and resistance amplification is characterized by an inverted U: a new paradigm for optimizing pharmacodynamics to counterselect resistance.
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.
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.
AID559215Antibacterial activity against Streptococcus pneumoniae W002 assessed as resistant isolates with ParC79 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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?
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.
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.
AID728910Antibacterial activity against Chlamydophila pneumoniae CM-1 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
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.
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.
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.
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.
AID559234Antibacterial activity against Streptococcus pneumoniae S002 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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?
AID1557279Antibacterial activity against Escherichia coli by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
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.
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.
AID1557303Cmax in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
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?
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.
AID559233Antibacterial activity against Streptococcus pneumoniae S001 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID1557282Antibacterial activity against Bacteroides fragilis by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
AID559212Antibacterial activity against Streptococcus pneumoniae D0012009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID559218Antibacterial activity against Streptococcus pneumoniae S004 assessed as resistant isolates with ParC79 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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.
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.
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.
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.
AID559227Antibacterial activity against Streptococcus pneumoniae W002 assessed as resistant isolates with GyrA81 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID1557306Protein binding in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
AID1427528Permeability of the compound at 100 ug/ml after 18 hrs by PAMPA2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
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.
AID559236Antibacterial activity against Streptococcus pneumoniae S004 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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.
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.
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.
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.
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.
AID559237Antibacterial activity against Streptococcus pneumoniae D002 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559230Antibacterial activity against Streptococcus pneumoniae D001 assessed as resistant isolates with GyrA81 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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.
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.
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.
AID559232Antibacterial activity against Streptococcus pneumoniae W002 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID728909Antibacterial activity against levofloxacin-intermediate and levofloxacin-resistant Streptococcus pneumoniae after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
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.
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.
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.
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.
AID559210Antibacterial activity against Streptococcus pneumoniae S0032009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
AID559207Antibacterial activity against Streptococcus pneumoniae W0022009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
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.
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.
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.
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.
AID279554Antibacterial activity against ciprofloxacin-susceptible methicillin-resistant Staphylococcus aureus by broth macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
The relationship between quinolone exposures and resistance amplification is characterized by an inverted U: a new paradigm for optimizing pharmacodynamics to counterselect resistance.
AID1557287Antibacterial activity against Enterococcus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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?
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.
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.
AID559223Antibacterial activity against Streptococcus pneumoniae S004 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
AID1557283Antibacterial activity against Haemophilus influenzae with horse blood by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
AID1557280Antibacterial activity against Pseudomonas aeruginosa by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
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.
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.
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.
AID559211Antibacterial activity against Streptococcus pneumoniae S0042009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID559217Antibacterial activity against Streptococcus pneumoniae S003 assessed as resistant isolates with ParC79 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559224Antibacterial activity against Streptococcus pneumoniae D001 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID279556Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by broth macrodilution method at 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
The relationship between quinolone exposures and resistance amplification is characterized by an inverted U: a new paradigm for optimizing pharmacodynamics to counterselect resistance.
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.
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.
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.
AID279558Antibacterial activity against ciprofloxacin-resistant methicillin-resistant Staphylococcus aureus at 48 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
The relationship between quinolone exposures and resistance amplification is characterized by an inverted U: a new paradigm for optimizing pharmacodynamics to counterselect resistance.
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.
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.
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.
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?
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.
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.
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.
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.
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.
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?
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.
AID1557284Antibacterial activity against Staphylococcus aureus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1557286Antibacterial activity against Streptococcus pyogenes by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
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.
AID559213Antibacterial activity against Streptococcus pneumoniae D0022009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
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.
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.
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.
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.
AID1557305Half life in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID559235Antibacterial activity against Streptococcus pneumoniae S003 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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?
AID559225Antibacterial activity against Streptococcus pneumoniae D002 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
AID559222Antibacterial activity against Streptococcus pneumoniae S003 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
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.
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.
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.
AID279557Antibacterial activity against ciprofloxacin-susceptible methicillin-resistant Staphylococcus aureus at 48 hrs by broth macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
The relationship between quinolone exposures and resistance amplification is characterized by an inverted U: a new paradigm for optimizing pharmacodynamics to counterselect resistance.
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.
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.
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.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
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.
AID1557304AUC in human at 0.4 g, po2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
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.
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.
AID728912Antibacterial activity against Mycoplasma pneumoniae ATCC 29085 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
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.
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.
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.
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.
AID559214Antibacterial activity against Streptococcus pneumoniae W001 assessed as resistant isolates with ParC79 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID728911Antibacterial activity against Chlamydophila pneumoniae AR39 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
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.
AID559219Antibacterial activity against Streptococcus pneumoniae W001 assessed as resistant isolates with ParC83 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559228Antibacterial activity against Streptococcus pneumoniae S001 assessed as resistant isolates with GyrA81 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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?
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.
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.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID559231Antibacterial activity against Streptococcus pneumoniae W001 assessed as resistant isolates with GyrA85 mutation in quinolone resistance-determining regions2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
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.
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.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (190)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's141 (74.21)29.6817
2010's45 (23.68)24.3611
2020's4 (2.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.81

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.81 (24.57)
Research Supply Index5.37 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index72.72 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials19 (9.74%)5.53%
Reviews5 (2.56%)6.00%
Case Studies10 (5.13%)4.05%
Observational0 (0.00%)0.25%
Other161 (82.56%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]