Page last updated: 2024-12-08

sitafloxacin

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Description

sitafloxacin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID461399
CHEMBL ID108821
CHEBI ID4304
SCHEMBL ID74553
MeSH IDM0205162
PubMed CID6918203
CHEMBL ID3989504
SCHEMBL ID1060786
MeSH IDM0205162

Synonyms (69)

Synonym
AC-1388
gracevit
7-((7s)-7-amino-5-azaspiro[2.4]hept-5-yl)-1-((1s,2s)-2-fluorocyclopropyl)-8-chloro-6-fluoro-4-oxohydroquinoline-3-carboxylic acid
7-[(7s)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-4-oxo-quinoline-3-carboxylic acid
3-quinolinecarboxylic acid, 7-[(7s)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-
du 6859
du-6859
127254-12-0
3-quinolinecarboxylic acid, 7-((7s)-7-amino-5-azaspiro(24)hept-5-yl)-8-chloro-6-fluoro-1-((1r,2s)-2-fluorocyclopropyl)-1,4-dihydro-4-oxo-
3-quinolinecarboxylic acid, 7-(7-amino-5-azaspiro(2.4)hept-5-yl)-8-chloro-6-fluoro-1-(2-fluorocyclopropyl)-1,4-dihydro-4-oxo-, (1r-(1alpha(s*),2alpha))-
(-)-7-((7s)-amino-5-azaspiro(2,4)hept-5-yl)-8-chloro-6-fluoro-1-((1r,2s)-2-fluorocyclopropyl)-1,4-dihydro-4-oxoq-3-uinolonecarboxylic acid
7-(7-amino-5-azaspiro(2.4)heptan-5-yl)-8-chloro-6-fluoro-1-(2-fluorocyclopropyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid sesquihydrate
7-((7s)-amino-5-azaspiro(2,4)heptan-5-yl)-8-chloro-6-fluoro-1-((1r,2r)-cis-2-fluoro-1-cyclopropyl)-1,4-dihydro-4-oxoquinolone-3-carboxylic acid
sitafloxacin [inn]
7-[(7s)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylic acid
chebi:4304 ,
CHEMBL108821
167355-47-7
A805673
7-[(7s)-7-azanyl-5-azaspiro[2.4]heptan-5-yl]-8-chloranyl-6-fluoranyl-1-[(1r,2s)-2-fluoranylcyclopropyl]-4-oxidanylidene-quinoline-3-carboxylic acid
7-[(7s)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-4-oxo-3-quinolinecarboxylic acid
A805671
AKOS015962212
3gjc60u4q8 ,
unii-3gjc60u4q8
7-((s)-7-amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1r,2s)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
sitafloxacin [mi]
sitafloxacin anhydrous
sitafloxacin [who-dd]
HY-B0395
SCHEMBL74553
AM85541
AB01568244_01
J-519022
7-((s)-7-amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1r,2s)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
(-)-7-[(7s)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluoro-1-cyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
163157-04-8
155421-11-7
3-quinolinecarboxylic acid, 7-[(7s)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2
du6859a
gtpl11040
compound 33 [pmid: 7932562]
273401-03-9
rel-7-((r)-7-amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1s,2r)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
sitafloxacin 100 microg/ml in acetonitrile
spifloxacin hydrate
sitafloxacin hydrate
du-6859a
sitafloxacin
AKOS005145900
sitafloxacin sesquihydrate
sitafloxacin monohydrate
unii-45ip57b62b
45ip57b62b ,
163253-37-0
3-quinolinecarboxylic acid, 7-(7-amino-5-azaspiro(2.4)hept-5-yl)-8-chloro-6-fluoro-1-(2-fluorocyclopropyl)-1,4-dihydro-4-oxo-, monohydrate, (1r-(1alpha(s*),2alpha))-
3-quinolinecarboxylic acid, 7-((7s)-7-amino-5-azaspiro(2.4)hept-5-yl)-8-chloro-6-fluoro-1-((1r,2s)-2-fluorocyclopropyl)-1,4-dihydro-4-oxo-, hydrate (1:1)
3-quinolinecarboxylic acid, 7-(7-amino-5-azaspiro(2.4)hept-5-yl)-8-chloro-6-fluoro-1-(2-fluorocyclopropyl)-1,4-dihydro-4-oxo-, monohydrate, (1r-(1.alpha.(s*),2.alpha.))-
SCHEMBL1060786
3-quinolinecarboxylicacid,7-[(7s)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-1,4-dihydro-4-oxo-,hydrate(2:3)
AM85615
3-quinolinecarboxylicacid,7-[(7s)-7-amino-5-azaspiro[2.4]hept-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-1,4-dihydro-4- oxo-,hydrate (2:3)
J-524203
sitafloxacin (monohydrate)
7-[(7s)-7-amino-5-azaspiro[2.4]heptan-5-yl]-8-chloro-6-fluoro-1-[(1r,2s)-2-fluorocyclopropyl]-4-oxoquinoline-3-carboxylic acid;hydrate
CHEMBL3989504
Q27258838
HY-B0395B
CS-0009318

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The incidence, severity and type of adverse events were similar in both treatment groups."( An open, randomised, multi-centre study comparing the safety and efficacy of sitafloxacin and imipenem/cilastatin in the intravenous treatment of hospitalised patients with pneumonia.
Briggs, A; Feldman, C; Flitcroft, A; O'Grady, J; Richards, G; White, H, 2001
)
0.31
" 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
)
0.51

Pharmacokinetics

The study was to evaluate the pharmacokinetic characteristics of a single dose of sitafloxacin in healthy Chinese volunteers.

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" The clinical efficacy, pneumococci eradication rate, safety, and pharmacokinetic and pharmacodynamic indices of the two groups were then assessed."( Clinical dose findings of sitafloxacin treatment: pharmacokinetic-pharmacodynamic analysis of two clinical trial results for community-acquired respiratory tract infections.
Aoki, N; Fujita, J; Hori, S; Kadota, J; Kaku, M; Kohno, S; Niki, Y; Tanigawara, Y; Watanabe, A; Yanagihara, K, 2013
)
0.39
" A population pharmacokinetic analysis of sitafloxacin was conducted using clinical data of five clinical pharmacology studies and one clinical PK-PD study in patients with RTIs."( Population pharmacokinetics and pharmacodynamics of sitafloxacin in patients with community-acquired respiratory tract infections.
Kaku, M; Saito, A; Tanigawara, Y; Totsuka, K; Tsuge, H, 2013
)
0.39
" Pharmacokinetic parameters and dialyzability of sitafloxacin were evaluated."( Dialyzability and pharmacokinetics of sitafloxacin following multiple oral dosing in infected hemodialysis patients.
Hayasaka, T; Saito, T; Tsuruoka, S; Yamagata, K; Yokota, N, 2013
)
0.39
" This method was successfully applied to the pharmacokinetic study of sitafloxacin in healthy Chinese volunteers."( Determination of sitafloxacin in human plasma by liquid chromatography-tandem mass spectrometry method: application to a pharmacokinetic study.
Chen, L; Ding, Y; Duan, R; He, Q; Huang, K; Xu, WY; Xu, XJ; Yang, J; Zhang, J, 2014
)
0.4
" This study was to evaluate the pharmacokinetic characteristics of a single dose of sitafloxacin in healthy Chinese volunteers."( Pharmacokinetics and safety of sitafloxacin after single oral doses in healthy volunteers.
Hu, X; Liu, J; Shentu, J; Wu, G; Wu, L; Zhai, Y; Zheng, Y; Zhou, H; Zhu, M, 2014
)
0.4
" Pharmacokinetic parameters were calculated and analyzed statistically."( Pharmacokinetics and safety of sitafloxacin after single oral doses in healthy volunteers.
Hu, X; Liu, J; Shentu, J; Wu, G; Wu, L; Zhai, Y; Zheng, Y; Zhou, H; Zhu, M, 2014
)
0.4

Compound-Compound Interactions

The antimicrobial effect of sitafloxacin (DU-6859a), used either singly or in combination with rifampicin, was evaluated in vitro against Mycobacterium ulcerans. The results were compared with those obtained with ofloxAcin. Similar to ofl Oxacin and levoflOxacin, sitafLoxACin exhibited synergistic activity when combined with either rifabutin or KRM-1648.

ExcerptReferenceRelevance
" When combined with amphotericin B (AmB), however, DU-6859a clearly enhanced the in vitro antifungal activity of AmB against Candida albicans, Candida tropicalis, Candida krusei, Candida glabrata, and Cryptococcus neoformans in microdilution checkerboard studies."( In vitro and in vivo antifungal activities of DU-6859a, a fluoroquinolone, in combination with amphotericin B and fluconazole against pathogenic fungi.
Kitamura, A; Nakajima, R; Sato, K; Someya, K; Tanaka, M, 1995
)
0.29
"The in vitro activity of DU-6859a (DU) alone and in combination with various antimicrobials was evaluated against multiresistant enterococci including some isolates with defined gyrA mutations."( Bactericidal activity of the fluoroquinolone DU-6859a alone and in combination with other antimicrobial agents against multiresistant enterococci.
Erdem, I; Korten, V; Murray, BE, 1996
)
0.29
" It is concluded that DU-6859a and trovafloxacin are very potent against enterococci, especially when combined with gentamicin."( In vitro activity of quinupristin/dalfopristin and newer quinolones combined with gentamicin against resistant isolates of Enterococcus faecalis and Enterococcus faecium.
Giamarellos-Bourboulis, EJ; Giamarellou, H; Grecka, P; Sambatakou, H, 1998
)
0.3
"We studied the activities of clarithromycin and fluoroquinolones (gatifloxacin, sitafloxacin, levofloxacin) in combination with other antimycobacterial drugs against extracellular and intramacrophage Mycobacterium avium complex (MAC)."( Antimicrobial activities of clarithromycin, gatifloxacin and sitafloxacin, in combination with various antimycobacterial drugs against extracellular and intramacrophage Mycobacterium avium complex.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.31
"Studies were undertaken in order to assess the anti- Mycobacterium tuberculosis (MTB) activities of newly developed fluoroquinolones in combination with other antituberculous drugs."( Anti-Mycobacterium tuberculosis activities of new fluoroquinolones in combination with other antituberculous drugs.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.31
"A new C-8-methoxyl fluoroquinolone, gatifloxacin (GFLX), and a new C-8-chloro fluoroquinolone, sitafloxacin (STFX), in combination with other drugs were examined for their activities against extracellular growing MTB organisms and those replicating in RAW264."( Anti-Mycobacterium tuberculosis activities of new fluoroquinolones in combination with other antituberculous drugs.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.31
" Both GFLX and STFX exhibited combined activities against intramacrophage MTB, when used in combination with rifampin, rifalazil, isoniazid, pyrazinamide, ethambutol, streptomycin, or clofazimine."( Anti-Mycobacterium tuberculosis activities of new fluoroquinolones in combination with other antituberculous drugs.
Sano, C; Sato, K; Shimizu, T; Tomioka, H, 2002
)
0.31
"The antimicrobial effect of sitafloxacin (DU-6859a), used either singly or in combination with rifampicin, was evaluated in vitro against Mycobacterium ulcerans."( In vitro activity of sitafloxacin (DU-6859a) alone, or in combination with rifampicin, against Mycobacterium ulcerans.
Dhople, AM; Namba, K, 2002
)
0.31
"The antimicrobial effects of sitafloxacin (DU-6859a) against Mycobacterium leprae, either singly or in combination with either rifampicin, rifabutin or KRM-1648, were studied using a mouse footpad assay technique and the results were compared with those obtained with ofloxacin."( In vivo susceptibility of Mycobacterium leprae to sitafloxacin (DU-6859a), either singly or in combination with rifampicin analogues.
Dhople, AM; Namba, K, 2003
)
0.32
" Similar to ofloxacin and levofloxacin, sitafloxacin also exhibited synergistic activity when combined with either rifabutin or KRM-1648, but not with rifampin."( In-vitro activity of sitafloxacin (DU-6859a), either singly or in combination with rifampin analogs, against Mycobacterium leprae.
Dhople, AM; Namba, K, 2003
)
0.32
" Either used singly or in combination with rifampin, the effects of sitafloxacin were bactericidal."( Activities of sitafloxacin (DU-6859a), either singly or in combination with rifampin, against Mycobacterium ulcerans infection in mice.
Dhople, AM; Namba, K, 2003
)
0.32

Bioavailability

ExcerptReferenceRelevance
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
") formulation infused over 1 h (dose of 400 mg sitafloxacin) in healthy male and female subjects and to estimate the absolute bioavailability of sitafloxacin from the capsule formulation."( Pharmacokinetics and absolute bioavailability of sitafloxacin, a new fluoroquinolone antibiotic, in healthy male and female Caucasian subjects.
Atarashi, S; Briggs, A; Kobayashi, H; Milatovic, D; O'Grady, J; Smith, RL; Ward, C; Ward, J, 2001
)
0.31

Dosage Studied

In healthy Chinese subjects, single dosing of sitafloxacin resulted in linear plasma pharmacokinetics. An optimal dosage regimen was considered based on a pharmacokinetic and pharmacodynamics analysis in patients with community-acquired respiratory tract infections.

ExcerptRelevanceReference
" It appears that although DU-6859a has a weak inhibitory effect on TP metabolism in vitro, its concomitant use with TP at clinical dosage levels does not cause any adverse effects, showing only a slight increase in blood TP concentrations and a decrease in urinary metabolites."( Effects of DU-6859a, a new quinolone antimicrobial, on theophylline metabolism in in vitro and in vivo studies.
Itokawa, K; Niki, Y; Okazaki, O, 1998
)
0.3
" Gemifloxacin was found to be highly bactericidal against these bacteria, producing a biphasic dose-response curve typical of the fluoroquinolones."( The bactericidal activity of gemifloxacin (SB-265805).
Clark, S; Mathias, I; Morrissey, I, 2000
)
0.31
" In a second study, two dosage regimens of sitafloxacin were compared with placebo in Oriental subjects."( A randomized controlled trial (volunteer study) of sitafloxacin, enoxacin, levofloxacin and sparfloxacin phototoxicity.
Dawe, RS; Ferguson, J; Ibbotson, SH; Sanderson, JB; Thomson, EM, 2003
)
0.32
" The urinary recoveries of radioactivity after intravenous dosing were 45."( Pharmacokinetics, tissue distribution, and excretion of sitafloxacin, a new fluoroquinolone antibiotic, in rats, dogs, and monkeys.
Jin, Y; Mitsugi, K; Okazaki, O; Tachibana, M; Takaichi, M; Tanaka, M, 2004
)
0.32
" No obvious differences in the efficacy and safety were observed between the dosage groups."( Clinical dose findings of sitafloxacin treatment: pharmacokinetic-pharmacodynamic analysis of two clinical trial results for community-acquired respiratory tract infections.
Aoki, N; Fujita, J; Hori, S; Kadota, J; Kaku, M; Kohno, S; Niki, Y; Tanigawara, Y; Watanabe, A; Yanagihara, K, 2013
)
0.39
"An optimal dosage regimen of sitafloxacin was considered based on a pharmacokinetics and pharmacodynamics (PK-PD) analysis in patients with community-acquired respiratory tract infections (RTI)."( Population pharmacokinetics and pharmacodynamics of sitafloxacin in patients with community-acquired respiratory tract infections.
Kaku, M; Saito, A; Tanigawara, Y; Totsuka, K; Tsuge, H, 2013
)
0.39
" Oral dosing of this drug at 50 mg daily in maintenance hemodialysis patients provides a safe drug concentration compatible with that of healthy subjects orally receiving 100 mg daily."( Dialyzability and pharmacokinetics of sitafloxacin following multiple oral dosing in infected hemodialysis patients.
Hayasaka, T; Saito, T; Tsuruoka, S; Yamagata, K; Yokota, N, 2013
)
0.39
"In healthy Chinese subjects, single dosing of sitafloxacin resulted in linear plasma pharmacokinetics."( Pharmacokinetics and safety of sitafloxacin after single oral doses in healthy volunteers.
Hu, X; Liu, J; Shentu, J; Wu, G; Wu, L; Zhai, Y; Zheng, Y; Zhou, H; Zhu, M, 2014
)
0.4
" Here, we present an eradication regimen consisting of four-times-daily dosing (q."( Four-times-daily Dosing of Rabeprazole with Sitafloxacin, High-Dose Amoxicillin, or Both for Metronidazole-Resistant Infection with Helicobacter pylori in Japan.
Andoh, A; Ban, H; Furuta, T; Ichikawa, H; Kagami, T; Otsuka, T; Sahara, S; Sugimoto, M, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
quinolone antibioticAn organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.
fluoroquinolone antibioticAn organonitrogen heterocyclic antibiotic containing a quinolone (or quinolone-like) moiety and which have a fluorine atom attached to the central ring system.
[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]

Bioassays (141)

Assay IDTitleYearJournalArticle
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID285294Effect on 4 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID285286Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID565323Antibacterial activity against Mycoplasma genitalium M6285 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID285287Effect on 1 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID565308Antibacterial activity against Mycoplasma genitalium by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID163270Minimum inhibitory concentration in vitro against Pseudomonas aeruginosa (32104)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID285300Effect on 4 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
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.
AID565309Antibacterial activity against Mycoplasma genitalium by quantitative TaqMan PCR method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID324748Antibacterial activity in Mycobacterium leprae infected mouse foot-pad model assessed as parasite killing at 25 mg/kg/day 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.
AID285278Susceptibility of penicillin-resistant Streptococcus pneumoniae 335 by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1653545Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0469 ug/ml in presence of 0.2 ug/ml rifampin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID69597Antibacterial activity was evaluated against Escherichia coli2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID206786Inhibitory activity against MRSA1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID565328Antibacterial activity against Mycoplasma genitalium M6282 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID206358Minimum inhibitory concentration in vitro against Streptococcus epidermis (56556)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID524825Antibacterial activity against erythromycin susceptible Campylobacter sp. by agar plate dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID206087Inhibitory activity against all group A and B Streptococci1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID565324Antibacterial activity against Mycoplasma genitalium M6286 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID285306Effect on 16 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
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.
AID565312Antibacterial activity against Mycoplasma genitalium R32 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID67913Inhibitory activity against strain of Enterococcus faecalis1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID285301Effect on 8 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID285299Effect on 0.5 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID285283Effect on 16 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID524824Antibacterial activity against erythromycin resistant Campylobacter sp. by agar plate dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID285282Effect on 16 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1653572Antimicrobial activity against Mycobacterium leprae assessed as fractional inhibitory concentration index at 0.0469 ug/ml in presence of 0.0062 ug/ml KRM-1648 measured at 4 weeks2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
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.
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.
AID565319Antibacterial activity against Mycoplasma genitalium M2321 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID285291Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID68529Minimum inhibitory concentration in vitro against Enterobacter cloacae (03400)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID285304Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID285310Susceptibility of drug-selected vancomycin-resistant Enterococcus species mutant by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID164231Antibacterial activity was evaluated against Pseudomonas aeruginosa2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID285280Effect on 0.5 ug/ml sitofloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID285309Susceptibility of vancomycin-resistant Enterococcus species single-step mutant by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID565315Antibacterial activity against Mycoplasma genitalium TW48-5G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID285285Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID565327Antibacterial activity against Mycoplasma genitalium M6151 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
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.
AID21569Urinary recovery by oral administration to rats in conjugate form of compound at 20 mg/kg1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID285288Effect on 4 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID21570Urinary recovery by oral administration to rats in unchanged form of compound at 20 mg/kg1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID67922Antibacterial activity evaluated against Enterococcus faecalis2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID1653547Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0938 ug/ml in presence of 0.2 ug/ml rifampin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID565322Antibacterial activity against Mycoplasma genitalium M6280 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID565316Antibacterial activity against Mycoplasma genitalium UTMB-10G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID20893Aqueous solubility was calculated by measuring the maximum UV absorption of the solution1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID285284Susceptibility of penicillin-resistant Streptococcus pneumoniae 334 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID565311Antibacterial activity against Mycoplasma genitalium M30 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID285302Susceptibility of penicillin-resistant Streptococcus pneumoniae 218 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID285295Effect on 32 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID208037Minimum inhibitory concentration in vitro against Streptococcus marcescens (10100)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID285307Effect on 16 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1653546Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0938 ug/ml in presence of 0.1 ug/ml rifampin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID285292Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID285289Effect on 32 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID163417Minimum inhibitory concentration in vitro against Proteus vulgaris (08601)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID565321Antibacterial activity against Mycoplasma genitalium M6257 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID285303Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1653550Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0469 ug/ml in presence of 0.0031 ug/ml KRM-1648 measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653549Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0469 ug/ml in presence of 0.05 ug/ml rifabutin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID565330Antibacterial activity against Mycoplasma genitalium M6284 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID209253Minimum inhibitory concentration in vitro against Streptococcus faecalis (ATCC 19433)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
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.
AID285298Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID285305Effect on 2 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID285281Effect on 1 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID565310Antibacterial activity against Mycoplasma genitalium G37 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID285290Susceptibility of penicillin-resistant Streptococcus pneumoniae 216 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1653570Antimicrobial activity against Mycobacterium leprae assessed as fractional inhibitory concentration index at 0.0938 ug/ml in presence of 0.2 ug/ml rifampin measured at 4 weeks2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID69640Minimum inhibitory concentration in vitro against Escherichia coli (NIHJ)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID1653551Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0469 ug/ml in presence of 0.0062 ug/ml KRM-1648 measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID565320Antibacterial activity against Mycoplasma genitalium M2341 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID66099Inhibitory activity against strain of Enterococcus faecium1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID565318Antibacterial activity against Mycoplasma genitalium M2300 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID285293Effect on 2 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID203450Inhibitory activity against Staphylococci1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
New directions in antibacterial research.
AID285279Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID26183Half-life in plasma was determined by oral administration to rats at 20 mg/kg1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID20865Apparent partition coefficient was measured by using CHCl3/0.1M phosphate buffer(pH 7.4)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID1653548Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.0469 ug/ml in presence of 0.025 ug/ml rifabutin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID565326Antibacterial activity against Mycoplasma genitalium M6090 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID205847Minimum inhibitory concentration in vitro against Streptococcus aureus (209P)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID565329Antibacterial activity against Mycoplasma genitalium M6283 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID565317Antibacterial activity against Mycoplasma genitalium M2282 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1653571Antimicrobial activity against Mycobacterium leprae assessed as fractional inhibitory concentration index at 0.0469 ug/ml in presence of 0.05 ug/ml rifabutin measured at 4 weeks2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID285308Susceptibility of methicillin-sensitive/resistant Staphylococcus aureus single-step mutant by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID209772Minimum inhibitory concentration in vitro against Streptococcus pyogenes (G36)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID285297Effect on 0.03 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID565314Antibacterial activity against Mycoplasma genitalium TW10-6G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID14072Maximum concentration in plasma was determined by oral administration to rats at 20 mg/kg1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID206728Antibacterial activity was evaluated against Staphylococcus aureus2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID565331Antibacterial activity against Mycoplasma genitalium M6287 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID565313Antibacterial activity against Mycoplasma genitalium TW10-5G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID565325Antibacterial activity against Mycoplasma genitalium M6328 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID285296Susceptibility of penicillin-resistant Streptococcus pneumoniae 217 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID93896Minimum inhibitory concentration in vitro against Klebsiella pneumoniae (type-2)1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(Fluorocyclopropyl)quinolones. 2. Synthesis and Stereochemical structure-activity relationships of chiral 7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-(2-fluorocyclopropyl)quinolone antibacterial agents.
AID556009Antibacterial activity against Helicobacter pylori2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Sitafloxacin and garenoxacin may overcome the antibiotic resistance of Helicobacter pylori with gyrA mutation.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (194)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's51 (26.29)18.2507
2000's50 (25.77)29.6817
2010's75 (38.66)24.3611
2020's18 (9.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.64

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 Index48.64 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.91 (4.65)
Search Engine Demand Index71.11 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.64)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials22 (11.89%)5.53%
Reviews2 (12.50%)6.00%
Reviews10 (5.41%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies7 (3.78%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other14 (87.50%)84.16%
Other146 (78.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT02729116]Phase 2/Phase 330 participants (Anticipated)Interventional2016-07-31Active, not recruiting
A Multicenter, Randomized, Open-Label, Parallel-Controlled Clinical Study to Evaluate the Efficacy and Safety of Sitafloxacin in Adult Subjects With Acute Exacerbation of Chronic Obstructive Pulmonary Disease [NCT05400369]Phase 4268 participants (Anticipated)Interventional2022-08-10Recruiting
A Randomized Controlled Trial of Sitafloxacin and Ertapenem Treatment for Acute Pyelonephritis Caused by Extended-Spectrum ß-lactamase-producing Escherichia Coli [NCT02537847]Phase 296 participants (Anticipated)Interventional2012-11-30Recruiting
Efficacy and Safety of Sitafloxacin in the Treatment of Acute Exacerbation of Bronchiectasis in Adults :A Multi-center, Randomized, Evaluator-blinded, Levofloxacin Parallel-controlled Clinical Study [NCT05313750]Phase 4256 participants (Anticipated)Interventional2021-06-30Active, not recruiting
A Randomized Controlled Non-Inferiority Study for Shortening Tuberculosis Treatment With Sitafloxacin-Containing Regimens [NCT05454345]Phase 3620 participants (Anticipated)Interventional2022-10-01Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]