Page last updated: 2024-11-07

pd-117596

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

Description

PD-117596: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122796
CHEMBL ID15464
SCHEMBL ID1387312
MeSH IDM0161360

Synonyms (23)

Synonym
7-(3-amino-pyrrolidin-1-yl)-1-cyclopropyl-6,8-difluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid
7-(3-aminopyrrolidinyl)-1-cyclopropyl-6,8-difluoro-4-oxohydroquinoline-3-carboxylic acid
99734-98-2
pd117596 ,
7-(3-aminopyrrolidin-1-yl)-1-cyclopropyl-6,8-difluoro-4-oxo-quinoline-3-carboxylic acid
pd 117596-2
3-quinolinecarboxylic acid, 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-
CHEMBL15464 ,
ci-938
unii-oph24o2pwb
pd-117596
pd 117596
oph24o2pwb ,
7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
SCHEMBL1387312
7-[3-amino-1-pyrrolidinyl]-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
7-(3-amino 1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3quinolinecarboxylic acid
UHBXZNXCIZHGFF-UHFFFAOYSA-N
7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3quinolinecarboxylic acid
7-(3-aminopyrrolidin-1-yl)-1-cyclopropyl-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
DTXSID00912518
bdbm50231263
Q27285776

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Azithromycin was more potent than the other macrolides in experimental animal infection, eradicating the organism in all animals tested at a dosage of 8 mg/kg."( Comparative antimicrobial activity of the new macrolides against Borrelia burgdorferi.
Gross, B; Preac-Mursic, V; Schierz, G; Süss, E; Wilske, B, 1989
)
0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA topoisomerase 2-alphaHomo sapiens (human)EC50 (µMol)340.00000.72001.29003.0000AID211292
DNA topoisomerase 2-betaHomo sapiens (human)EC50 (µMol)340.00000.72001.29003.0000AID211292
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
hematopoietic progenitor cell differentiationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-alphaHomo sapiens (human)
DNA ligationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA damage responseDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome segregationDNA topoisomerase 2-alphaHomo sapiens (human)
female meiotic nuclear divisionDNA topoisomerase 2-alphaHomo sapiens (human)
apoptotic chromosome condensationDNA topoisomerase 2-alphaHomo sapiens (human)
embryonic cleavageDNA topoisomerase 2-alphaHomo sapiens (human)
regulation of circadian rhythmDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of apoptotic processDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIDNA topoisomerase 2-alphaHomo sapiens (human)
rhythmic processDNA topoisomerase 2-alphaHomo sapiens (human)
negative regulation of DNA duplex unwindingDNA topoisomerase 2-alphaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-alphaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-alphaHomo sapiens (human)
neuron migrationDNA topoisomerase 2-betaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-betaHomo sapiens (human)
axonogenesisDNA topoisomerase 2-betaHomo sapiens (human)
B cell differentiationDNA topoisomerase 2-betaHomo sapiens (human)
forebrain developmentDNA topoisomerase 2-betaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-betaHomo sapiens (human)
cellular response to hydrogen peroxideDNA topoisomerase 2-betaHomo sapiens (human)
cellular response to ATPDNA topoisomerase 2-betaHomo sapiens (human)
cellular senescenceDNA topoisomerase 2-betaHomo sapiens (human)
positive regulation of double-strand break repair via nonhomologous end joiningDNA topoisomerase 2-betaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-betaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
magnesium ion bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
RNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-alphaHomo sapiens (human)
protein kinase C bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP-dependent activity, acting on DNADNA topoisomerase 2-alphaHomo sapiens (human)
DNA binding, bendingDNA topoisomerase 2-alphaHomo sapiens (human)
protein homodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
ubiquitin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein heterodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
DNA bindingDNA topoisomerase 2-betaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-betaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-betaHomo sapiens (human)
protein bindingDNA topoisomerase 2-betaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-betaHomo sapiens (human)
ribonucleoprotein complex bindingDNA topoisomerase 2-betaHomo sapiens (human)
metal ion bindingDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
nuclear chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
centrioleDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome, centromeric regionDNA topoisomerase 2-alphaHomo sapiens (human)
condensed chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
male germ cell nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
cytoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA topoisomerase 2-alphaHomo sapiens (human)
protein-containing complexDNA topoisomerase 2-alphaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleolusDNA topoisomerase 2-betaHomo sapiens (human)
heterochromatinDNA topoisomerase 2-betaHomo sapiens (human)
nucleusDNA topoisomerase 2-betaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-betaHomo sapiens (human)
nucleolusDNA topoisomerase 2-betaHomo sapiens (human)
cytosolDNA topoisomerase 2-betaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-betaHomo sapiens (human)
nucleusDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (149)

Assay IDTitleYearJournalArticle
AID209232In vitro antibacterial activity was tested for Streptococcus faecalis MGH-21995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID198174Antibacterial activity was determined against gram positive organism, Streptococcus pneumoniae (SV-1)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID74853Antibacterial activity against five Gram-positive bacteria targeting topoisomerase II (DNA gyrase B GyrB)1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity, and antimicrobial activity.
AID197877Antibacterial activity was determined against gram positive organism, Staphylococcus aureus H2281991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID57388Minimum inhibitory concentration against Escherichia coli DNA-gyrase in supercoiling assay1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID117664In vivo subcutaneous protective dose was determined in female charles river CD-1 mice infected with Escherichia coli (vogel)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID117861Dose required to induce phototoxic reaction in 50% of mice by probit method at different dosage forms.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID209729Antibacterial activity was determined against Gram-negative Streptococcus pneumoniae SV-1 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID163044Antibacterial activity was determined against Gram-negative Providencia rettgeri H1771 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID70705Minimum inhibitory concentration (MIC) against gram negative bacteria Escherichia coli Vogel.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID230840MIC ratio measured as the mean MICs of gram-positive bacteria1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID68676In vitro antibacterial activity was tested for Escherichia coli Vogel1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID201953In vivo efficacy (orally) against Streptococcus pneumoniae SV-1 in mouse protection test1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID103830In vitro antimicrobial activity against strain Morganella morganii 151531992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID65234In vivo efficacy in mouse protection test in Escherichia coli Vogel administered by subcutaneous injection.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID122563Dose which has no effect to induce phototoxic reaction in 50% of mice by probit method.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID200230Antibacterial activity was determined against gram positive organism, Staphylococcus aureus (H228)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID205945Minimum inhibitory concentration (MIC) against gram positive bacteria Streptococcus pneumoniae SV-1.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID117653In vivo oral protective dose was determined in female charles river CD-1 mice infected with Streptococcus pneumoniae1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID117692The in vivo potency was determined in female charles river CD-1 mice infected with Streptococcus pyogenes after sc administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID69759Antibacterial activity in vitro against Escherichia coli Vogel1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID151052Antibacterial activity was determined against gram negative organism, Pseudomonas aeruginosa UI-181991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID210071Antibacterial activity measured as mouse protection against Streptococcus pyogenes C 203 after subcutaneous administration1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID64254Antibacterial activity was determined against gram negative organism, E. coli(vogel)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID200254In vitro antimicrobial activity against strain Staphylococcus aureus 95371992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID64064In vitro antimicrobial activity against strain Escherichia coli 151191992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID163914In vivo efficacy (s.c.) against Pseudomonas aeruginosa in mouse protection test1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID205944Minimum inhibitory concentration (MIC) against gram positive bacteria Streptococcus faecalis MGH-2.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID64251Antibacterial activity was determined against gram negative organism, Escherichia coli vogel1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID95531Minimum inhibitory concentration (MIC) against gram negative bacteria Klebsiella pneumoniae MGH-2.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID70293Protective dose against Escherichia coli H560 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID213604Clonogenic cytotoxicity against Hamster V-79 cells1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID51918Mammalian cell cytotoxicity test in chinese hamster V79 cells (clonogenic cytotoxicity)1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity, and antimicrobial activity.
AID94123Antibacterial activity was determined against gram negative organism, K. pneumoniae (MGH-2)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID207478Antibacterial activity was determined against Gram-negative Staphylococcus aureus H228 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID69639Minimum inhibitory concentration against Escherichia coli2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Artificial neural network applied to prediction of fluorquinolone antibacterial activity by topological methods.
AID96407In vitro antibacterial activity was tested for Klebsiella pneumoniae MGH-21995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID67884Minimum inhibitory concentration was evaluated in vitro against Enterococcus faecalis MGH-21993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID206368Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus faecalis MGH-21990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID206684Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus pneumoniae SV-11990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID209272Antibacterial activity was determined against Gram-negative Streptococcus pyogenes C203 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID70735Evaluated for minimum inhibitory concentration against gram-negative bacteria Escherichia coli Vogel1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID197882Antibacterial activity was determined against gram positive organism, Staphylococcus aureus UC761991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID63900In vitro antimicrobial activity against strain Enterobacter cloacae 96561992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID134132In vivo antibacterial activity against Streptococcus pyogenes after following subcutaneous administration1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID56592Number of mice which show positive phototoxic reaction in 15 mice1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID56591Days of the first positive reaction in depleted mice.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID209733Protective dose against Streptococcus pneumonia bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID163915In vivo efficacy (orally) against Pseudomonas aeruginosa in mouse protection test1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID202111In vivo efficacy (orally) against Streptococcus pyogenes C-203 in mouse protection test1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID68675In vitro antibacterial activity was tested for Escherichia coli H5601995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID50999In vitro antibacterial activity against Clostridium perfringens CP 3-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID117691The in vivo potency was determined in female charles river CD-1 mice infected with Streptococcus pyogenes after peroral administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID157244In vitro antibacterial activity was tested for Pepto asac PA 3-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID209771Minimum inhibitory concentration against Streptococcus pyogenes C2031994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID200231Antibacterial activity was determined against gram positive organism, Staphylococcus aureus (UC76)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID164268Evaluated for minimum inhibitory concentration against gram-negative bacteria Pseudomonas rettgeri H17711990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID161378Minimum inhibitory concentration (MIC) against gram negative bacteria Prot. rettgeri M-1771.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID67532Minimum inhibitory concentration (MIC) against gram negative bacteria Enterobacter cloacae MA-2646.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID209727Minimum inhibitory concentration was evaluated in vitro against Streptococcus pneumoniae SV-11993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID74734MIC ratio measured as the mean MICs of gram-positive bacteria1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID151374Antibacterial activity was determined against gram negative organism, Providencia rettgeri. M17711991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID208314Minimum inhibitory concentration tested against Streptococcus pneumoniae SV-11994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID206812Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus pyogenes C2031990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID163733Minimum inhibitory concentration was evaluated in vitro against Providencia rettgeri M17711993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID117652In vivo oral protective dose was determined in female charles river CD-1 mice infected with Escherichia coli (vogel)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID117665In vivo subcutaneous protective dose was determined in female charles river CD-1 mice infected with Streptococcus pneumoniae1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID118113Phototoxic skin reaction in depilated female CD-1 mice1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID150908Antibacterial activity was determined against gram negative organism, Pseudomonas aeruginosa (UI-18)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID164873Evaluated for minimum inhibitory concentration against gram-negative bacteria Pseudomonas aeruginosa UI-181990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID151366In vitro antimicrobial activity against strain Proteus mirabilis 99001992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID63898Antibacterial activity was determined against gram negative organism, Enterobacter cloacae MA26461991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID96239Evaluated for minimum inhibitory concentration against gram-negative bacteria Klebsiella pneumoniae MGH-21990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID54107Minimum inhibitory concentration required to inhibit DNA gyrase supercoiling.1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID68019Minimum inhibitory concentration in vitro against Enterobacter cloacae MA 26461993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID198021Antibacterial activity was determined against gram positive organism, Streptococcus faecalis MGH-21991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID163269Minimum inhibitory concentration against U1-18 cell line from Pseudomonas aeruginosa1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID209252Minimum inhibitory concentration against Streptococcus faecalis MGH-21994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID68339In vitro antibacterial activity was tested for Enterobacter cloacae HA26461995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID201952In vivo efficacy (s.c.) against Streptococcus pneumoniae SV-1 in mouse protection test1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID198179In vitro antimicrobial activity against strain Streptococcus pneumoniae 95851992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID69934Antibacterial activity was determined against Gram-negative Escherichia coli H560 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID205840Minimum inhibitory concentration against Staphylococcus aureus H 2281994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID68528Minimum inhibitory concentration against Enterobacter cloacae MA 26461994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID206765In vitro antibacterial activity was tested for Staphylococcus aureus UC-761995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID70721Evaluated for minimum concentration needed to produce linear DNA at an intensity relative to oxolinic acid at 10 mg/mL. by gyrase mediated cleavage of DNA in Escherichia coli 560.1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID198176Antibacterial activity was determined against gram positive organism, Streptococcus pneumoniae SV-11991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID198316Antibacterial activity was determined against gram positive organism, Streptococcus pyogenes (C203)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID96058Minimum inhibitory concentration was evaluated in vitro against Klebsiella pneumoniae MGH21993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID134129In vivo antibacterial activity against Escherichia coli after following oral administration1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID64404The in vivo potency was determined in female charles river CD-1 mice infected with Escherichia coli after peroral administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID160372In vitro antibacterial activity was tested for Propion acnes PA5-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID203107Minimum inhibitory concentration (MIC) against gram positive bacteria Staphylococcus aureus UC-76.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID65231Antibacterial activity was determined against Gram-negative Escherichia coli Vogel bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID207479Antibacterial activity was determined against Gram-negative Staphylococcus aureus UC-76 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID50853In vitro antibacterial activity was tested for Clostridium diff CD1-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID117689The in vivo potency was determined in female charles river CD-1 mice infected with Streptococcus pneumoniae after peroral administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID163064Minimum inhibitory concentration against M1771 strain of Providencia rettgeri1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID205842Minimum inhibitory concentration against Staphylococcus aureus UC-761994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID210074Protective dose against Streptococcus pyogenes bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID211292Tested for inhibition of topoisomerase II isolated from HeLa cells by DNA-cleavage assay1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Mammalian topoisomerase II inhibitory activity of 1-cyclopropyl-6,8- difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolinecarb oxylic acid and related derivatives.
AID41263In vitro antibacterial activity against Bacteroides fragilis BFA1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID213599Clonogenic cytotoxicity against Chinese hamster V-79 cells1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID70283Antibacterial activity against Escherichia coli Vogel after subcutaneous administration in mouse1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID63899Antibacterial activity against gram negative organism, Escherichia cloacae (MA2646)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID117690The in vivo potency was determined in female charles river CD-1 mice infected with Streptococcus pneumoniae after sc administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID205964Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus aureus H2281990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID74723MIC ratio measured as the mean MICs of gram-negative bacteria1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID134130In vivo antibacterial activity against Escherichia coli after following subcutaneous administration1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID94125In vitro antimicrobial activity against strain Klebsiella pneumoniae 96641992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID210070Compounds were evaluated in vivo for antibacterial activity for mouse protection against Streptococcus pyogenes C 203 after oral administration1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID230838MIC ratio measured as the mean MICs of gram-negative bacteria1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID64405The in vivo potency was determined in female charles river CD-1 mice infected with Escherichia coli after sc administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID74727Antibacterial activity against five Gram-negative bacteria1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity, and antimicrobial activity.
AID64255In vitro antimicrobial activity against strain Enterococcus faecalis 98091992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID205946Minimum inhibitory concentration (MIC) against gram positive bacteria Streptococcus pyogenes C-203.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID151373Antibacterial activity was determined against gram negative organism, Providencia rettgeri. (M1771)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID70743Gyrase-drug induced cleavage against Escherichia coli1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID165206In vitro antibacterial activity was tested for Pseudomonas aeruginosa UI-181995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID163740In vitro antibacterial activity was tested for Providencia rettgeri H17711995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID68028Antibacterial activity was determined against Gram-negative Enterobacter cloacae HA2646 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID163916Minimum inhibitory concentration (MIC) against gram negative bacteria Pseudomonas aeruginosa UI-18.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID93894Minimum inhibitory concentration against Klebsiella pneumoniae MGH-21994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID95886Antibacterial activity was determined against Gram-negative Klebsiella pneumoniae MGH-2 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID208121In vitro antibacterial activity was tested for Streptococcus pneumoniae SV-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID70282Antibacterial activity against Escherichia coli Vogel after oral administration in mouse1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID198317Antibacterial activity was determined against gram positive organism, Streptococcus pyogenes C2031991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID206764In vitro antibacterial activity was tested for Staphylococcus aureus H2281995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID202110In vivo efficacy (s.c.) against Streptococcus pyogenes C-203 in mouse protection test1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID207046Minimum inhibitory concentration was evaluated in vitro against Staphylococcus aureus UC 761993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID133761Maximum tolerance dose was measured for phototoxic skin reaction by po administration1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID135138The no effect dose (NED) for phototoxicity in mouse1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID69638Minimum inhibitory concentration against Escherichia coli Vogel1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID65235In vivo efficacy in mouse protection test in Escherichia coli Vogel dose administered orally by gavage.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID94001Antibacterial activity was determined against gram negative organism, Klebsiella pneumoniae MGH-21991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-amino- and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure-activity relationship.
AID209612In vitro antibacterial activity was tested for Streptococcus pyogenes C2031995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID207045Minimum inhibitory concentration was evaluated in vitro against Staphylococcus aureus H 2281993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID68183Evaluated for minimum inhibitory concentration against gram-negative bacteria Enterobacter cloacae HA 26461990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID70704Minimum inhibitory concentration (MIC) against gram negative bacteria Escherichia coli H-560.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID198020Antibacterial activity was determined against gram positive organism, Streptococcus faecalis (MGH-2)1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
AID164375Minimum inhibitory concentration was evaluated in vitro against Pseudomonas aeruginosa UI-181993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID150900In vitro antimicrobial activity against strain Pseudomonas aeruginosa 98431992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
AID164391Antibacterial activity was determined against Gram-negative Pseudomonas aeruginosa UI-18 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID205965Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus aureus UC-761990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID209130Minimum inhibitory concentration was evaluated in vitro against Streptococcus pyogenes C 2031993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy.
AID134131In vivo antibacterial activity against Streptococcus pyogenes after following oral administration1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
Synthesis and antibacterial activity of new quinolones containing a 7-[3-(1-amino-1-methylethyl)-1-pyrrolidinyl] moiety. Gram-positive agents with excellent oral activity and low side-effect potential.
AID203106Minimum inhibitory concentration (MIC) against gram positive bacteria Staphylococcus aureus H-228.1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8-fluoro group with reduced phototoxic risk.
AID209073Antibacterial activity was determined against Gram-negative Streptococcus faecalis MGH-2 bacteria1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
New quinolone antibacterial agents. Synthesis and biological activity of 7-(3,3- or 3,4-disubstituted-1-pyrrolidinyl)quinoline-3-carboxylic acids.
AID117862Phototoxic skin reaction in depilated female CD-1 mice1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (10.00)18.7374
1990's16 (80.00)18.2507
2000's2 (10.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.25

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

MetricThis Compound (vs All)
Research Demand Index12.25 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index5.34 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other21 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]