Page last updated: 2024-12-06

amifloxacin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Amifloxacin is a synthetic fluoroquinolone antibiotic that exhibits potent antibacterial activity against a broad spectrum of gram-positive and gram-negative bacteria. Its mechanism of action involves inhibiting DNA gyrase and topoisomerase IV, essential enzymes involved in bacterial DNA replication. Amifloxacin's importance lies in its effectiveness against multidrug-resistant bacteria, making it a valuable therapeutic option for infections caused by these strains. The compound's high oral bioavailability, long half-life, and ability to penetrate tissues have contributed to its widespread use in clinical settings. Research efforts focus on understanding its pharmacodynamics, pharmacokinetics, and potential applications in treating various infections. Studies aim to identify optimal dosage regimens, assess its efficacy in different bacterial strains, and explore its safety profile in various patient populations.'

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

Cross-References

ID SourceID
PubMed CID55492
CHEMBL ID6231
CHEBI ID169231
SCHEMBL ID48001
MeSH IDM0121025

Synonyms (47)

Synonym
6-luoro-1-(methylamino)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
CHEBI:169231
win-493753
D02902
amifloxacin (usan/inn)
6-fluoro-1,4-dihydro-1-(methylamino)-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
amifloxacin
win-49375
6-fluoro-1-(methylamino)-7-(4-methylpiperazin-1-yl)-4-oxo-quinoline-3-carboxylic acid
86393-37-5
CHEMBL6231
win 49,375
win-49,375
6-fluoro-1-(methylamino)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
win 49375
amifloxacine
5tu5227kyq ,
amifloxacine [french]
unii-5tu5227kyq
amifloxacino
3-quinolinecarboxylic acid, 6-fluoro-1,4-dihydro-1-(methylamino)-7-(4-methyl-1-piperazinyl)-4-oxo-
einecs 289-231-8
amifloxacino [spanish]
amifloxacinum
amifloxacinum [latin]
amifloxacin [usan:inn:ban]
amifloxacin [usan]
amifloxacin [mart.]
amifloxacin [inn]
SCHEMBL48001
RUXPNBWPIRDVTH-UHFFFAOYSA-N
6-fluoro-1,4-dihydro-1-methylamino-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
6-fluoro-methylamino-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
6-fluoro-1-methylamino-7-(4-methyl-piperazino)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid
DTXSID20235519
6-fluoro-1-(methylamino)-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
AKOS030530713
CS-7366
HY-U00221
Q4746186
FT-0711169
win49375
gtpl10758
win 49, 375
compound 7 [pmid: 2834557]
BS-49143
F87536

Research Excerpts

Overview

Amifloxacin is a fluoroquinolone with a spectrum of activity similar to that of ofloxACin, pefloxac in, enoxacIn, norfloxAcin and ciprofloxicin.

ExcerptReferenceRelevance
"Amifloxacin is a fluoroquinolone with a spectrum of activity similar to that of ofloxacin, pefloxacin, enoxacin, norfloxacin and ciprofloxacin. "( Comparative in vitro activity of amifloxacin and five other fluoroquinolone antimicrobial agents and preliminary criteria for the disk susceptibility test.
Barry, AL; Jones, RN, 1987
)
2

Toxicity

ExcerptReferenceRelevance
" Clinically significant adverse reactions, including pruritus and transaminase elevations, occurred only at doses of 1,200 mg/day or above."( Multiple-dose pharmacokinetics and safety of oral amifloxacin in healthy volunteers.
Brown, RR; Cook, JA; Nix, DE; Schelling, DJ; Schentag, JJ; Silverman, MH; Stroshane, RM, 1990
)
0.53

Pharmacokinetics

Amifloxacin was tested after intravenous administration to rhesus monkeys. Mean (standard deviation) pharmacokinetic parameters for amifl Oxacin were as follows: maximum observed concentration in plasma, 1.

ExcerptReferenceRelevance
" The methods were employed in a pharmacokinetic analysis of amifloxacin after intravenous administration to rhesus monkeys."( Analysis of amifloxacin in plasma and urine by high-pressure liquid chromatography and intravenous pharmacokinetics in rhesus monkeys.
Benziger, DP; Crawmer, BP; McCoy, LF, 1985
)
0.89
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33

Dosage Studied

Amifloxacin at 400 mg twice a day tended to cause adverse events more frequently than did TMP-SMX. Mean amiflOxacin concentrations in urine on day 11 in samples collected 0 to 2 h after dosing were 105, 417, 376, 336, 518, and 464 micrograms/ml for the 200-, 400-, and 600-mg regimens.

ExcerptRelevanceReference
" Amifloxacin at a dosage of 200 mg twice a day appeared as safe and effective as TMP-SMX, but amifloxacin at 400 mg twice a day tended to cause adverse events more frequently than did TMP-SMX."( Randomized, controlled trial of a 10-day course of amifloxacin versus trimethoprim-sulfamethoxazole in the treatment of acute, uncomplicated urinary tract infection. Amifloxacin Multi-Center Trial Group.
Boyko, EJ; Iravani, A; Schelling, DJ; Silverman, MH; Wright, RA, 1990
)
1.44
" Therefore, a modification in amifloxacin dosage regimen based solely on age may not be necessary."( Preliminary study of the pharmacokinetics of oral amifloxacin in elderly subjects.
Boddy, AW; Brown, RR; Cook, JA; Sauerschell, R; Silverman, MH; Stroshane, RM, 1990
)
0.82
" Mean amifloxacin concentrations in urine on day 11 in samples collected 0 to 2 h after dosing were 105, 417, 376, 336, 518, and 464 micrograms/ml for the 200-, 400-, and 600-mg q12h and 400-, 600-, and 800-mg q8h regimens, respectively."( Multiple-dose pharmacokinetics and safety of oral amifloxacin in healthy volunteers.
Brown, RR; Cook, JA; Nix, DE; Schelling, DJ; Schentag, JJ; Silverman, MH; Stroshane, RM, 1990
)
1.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

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.
[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 (81)

Assay IDTitleYearJournalArticle
AID78707MIC at which cleaved DNA (linear) is observed at an intensity relative to oxolinic acid at 10 ug/mL by using Gyrase Induced DNA-Cleavage assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID70458Biological activity against Escherichia coli N1HJ JC-2 relative to Norfloxacin.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Three-dimensional structure-activity relationships and receptor mapping of N1-substituents of quinolone antibacterials.
AID133806Compound was evaluated for antibacterial activity in mice after peroral administration with 0.5 mL of Escherichia coli Vogel inoculum1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships.
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.
AID209087Compound was tested for inhibition of the gram-negative organism Streptococcus faecalis MGH-21986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID210022Antibacterial activity against Streptococcus pneumoniae (SV-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
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.
AID209763Minimum inhibitory concentration against Streptococcus pyogenes (C203).1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID69784Antibacterial activity against Escherichia coli (vogel)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID164709Compound was tested for inhibition of the gram-negative organism Pseudomonas aeruginosa UI-181986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID78688Inhibitory concentration in supercoiling inhibition Escherichia coli DNA gyrase assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
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]
AID1918194Lipophilicity, log D of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID68506Minimum inhibitory concentration against Enterobacter cloacae. (MA2446).1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID207175Antibacterial activity against Staphylococcus aureus (H228)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID93887Minimum inhibitory concentration against Klebsiella pneumoniae (MGH-2)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID207212In vitro minimum inhibitory concentration against growth of Staphylococcus aureus Smith1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID209248Minimum inhibitory concentration against Streptococcus faecalis (MGH-2).1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID69469Minimum inhibitory concentration against Escherichia coli (H560)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID133812Compound was evaluated for protective dose against the Escherichia coli vogel lethal infection following sc administration in mouse1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID133814Compound was evaluated for protective dose against the Streptococcus aureus UC-76 lethal infection following po administration in mouse; No data1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
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]
AID68850In vitro minimum inhibitory concentration against growth of Escherichia coli Vogel1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships.
AID69782Antibacterial activity against Escherichia coli (H560)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID163738Compound was tested for inhibition of the gram-negative organism Providencia rettgeri H17711986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID78550Concentration required for 50% inhibition of gyrase.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID209302Compound was tested for inhibition of the gram-negative organism Streptococcus pyogenes C203.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID163100Minimum inhibitory concentration against Pseudomonas aeruginosa. (UI-18)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID205531Minimum inhibitory concentration against Staphylococcus aureus (H-228).1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID67545Activity against Enterobacter aerogenes2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Search compounds with antimicrobial activity by applying molecular topology to selected quinolones.
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
AID164385Antibacterial activity against Pseudomonas aeruginosa (UI-18)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID133817Compound was evaluated for protective dose against the Streptococcus pneumoniae SV-1 lethal infection following po administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID208894Compound was tested for inhibition of the gram-negative organism Streptococcus aureus UC-76.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1918193Dissociation constant, pKa of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID205543Minimum inhibitory concentration against Staphylococcus aureus (UC76).1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID133810Compound was evaluated for protective dose against the Escherichia coli vogel lethal infection following peroral administration in mouse1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID96422In vitro minimum inhibitory concentration against growth of Klebsiella pneumoniae strain 396451984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships.
AID162778In vitro minimum inhibitory concentration against growth of Pseudomonas aeruginosa MGH-21984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships.
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.
AID163052Minimum inhibitory concentration against Providencia rettgeri. (M1771)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID96229Compound was tested for inhibition of the gram-negative organism Klebsiella pneumoniae MGH-21986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID69470Minimum inhibitory concentration against Escherichia coli (vogel)1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID133816Compound was evaluated for protective dose against the Streptococcus aureus UC-76 lethal infection following sc administration in mouse; No data1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
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]
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID95885Antibacterial activity against Klebsiella pneumonia (MGH-2)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID222085Minimum inhibitory concentration against gram-negative enterobacteriaceae.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID78687Lowest concentration necessary to induce DNA gyrase-mediated cleavage of DNA1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
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]
AID70860Compound was tested for inhibition of the gram-negative organism Escherichia cloacae HA 26461986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID133805Antibacterial activity in mice after intraperitoneal administration with 0.5 mL of Escherichia coli Vogel inoculum1984Journal of medicinal chemistry, Sep, Volume: 27, Issue:9
Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationships.
AID208893Compound was tested for inhibition of the gram-negative organism Streptococcus aureus H228.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID210196Compound was tested for inhibition of the gram-negative organism Streptococcus pneumoniae SV-11986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID208310Minimum inhibitory concentration against Streptococcus pneumoniae (SV-1).1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
1-Substituted 7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8- difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids. New quantitative structure-activity relationships at N1 for the quinolone antibacterials.
AID78709Inhibition of DNA gyrase of Escherichia coli H560 cells1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID133807Compound was evaluated for protective dose against Streptococcus pneumoniae SV-1 lethal infection following sc administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID70571Compound was tested for inhibition of the gram-negative organism Escherichia coli vogel1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
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]
AID70570Compound was tested for inhibition of the gram-negative organism Escherichia coli H5601986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-199039 (76.47)18.7374
1990's7 (13.73)18.2507
2000's3 (5.88)29.6817
2010's1 (1.96)24.3611
2020's1 (1.96)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.11

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

MetricThis Compound (vs All)
Research Demand Index25.11 (24.57)
Research Supply Index4.01 (2.92)
Research Growth Index4.44 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (3.85%)5.53%
Reviews1 (1.92%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other49 (94.23%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]