Compounds > pd 117588
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pd 117588

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Description

PD 117588: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID73366
CHEMBL ID6210
SCHEMBL ID8922444
MeSH IDM0166844

Synonyms (23)

Synonym
3-quinolinecarboxylic acid, 1-cyclopropyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-
pd 117558
ci-948
1-cyclopropyl-7-[3-(ethylaminomethyl)pyrrolidin-1-yl]-6,8-difluoro-4-oxo-quinoline-3-carboxylic acid
pd117558 ,
99734-97-1
1-cyclopropyl-7-{3-[(ethylamino)methyl]pyrrolidin-1-yl}-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
pd-117558
CHEMBL6210
1-cyclopropyl-7-[3-(ethylaminomethyl)pyrrolidin-1-yl]-6,8-difluoro-4-oxoquinoline-3-carboxylic acid
3-quinolinecarboxylic acid, 1-cyclopropyl-7-(3-((ethylamino)methyl)-1-pyrrolindinyl)-6,7-difluoro-1,4-dihydro-4-oxo-
pd 117588
pd-117588
1-cyclopropyl-7-(3-((ethylamino)methyl)-1-pyrrolidinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
SCHEMBL8922444
WDBGUJBLPRXPIX-UHFFFAOYSA-N ,
1-cyclopropyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
AKOS030618329
DTXSID60912519
116874-46-5
bdbm50227275
3-quinolinecarboxylic acid, 1-cyclopropyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4
1-cyclopropyl-7-(3-((ethylamino)methyl)pyrrolidin-1-yl)-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (144)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
AID133946In vivo activity against Pseudomonas aeruginosa (po)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.
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.
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.
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.
AID133951In vivo activity against Streptococcus pyogenes (sc)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.
AID117660In vivo potency against Streptococcus pneumoniae using mouse protection assay following s.c. administration.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
AID163732Antibacterial activity against Providencia rettgeri M17711988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
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.
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.
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.
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.
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.
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.
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.
AID56593Number of mice which show positive phototoxic reaction in 5 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.
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.
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.
AID202131Compounds were evaluated in vivo for antibacterial activity for 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.
AID133823In vivo activity against Escherichia coli (po)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.
AID7869250% inhibitory concentration against DNA-gyrase1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
AID209247Minimum inhibitory concentration against Streptococcus faecalis MGH-2 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
AID133950In vivo activity against Streptococcus pyogenes (po)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.
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.
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.
AID3062Antibacterial activity was determined against gram negative organism, Enterobacter 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.
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.
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.
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.
AID206877Antibacterial activity against Staphylococcus aureus H-2281988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID69339Minimum inhibitory concentration against Escherichia coli H560 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
AID94153Evaluated 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.
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.
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.
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.
AID206890Antibacterial activity against Staphylococcus aureus UC761988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
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.
AID133948In vivo activity against Streptococcus pneumoniae (po)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.
AID95916Antibacterial activity against Klebsiella pneumoniae MGH-21988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
AID69340Minimum inhibitory concentration against Escherichia coli vogel in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID117674Median protective dose against Escherichia coli, determined in acute, lethal systemic infection in female charles river CD-1 mice (po)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
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.
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.
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.
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.
AID117675Median protective dose against Escherichia coli, determined in acute, lethal systemic infection in female charles river CD-1 mice (sc)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID69626Antibacterial activity against Escherichia coli Vogel1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
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.
AID163093Minimum inhibitory concentration against Pseudomonas aeruginosa UI-18 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
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.
AID133949In vivo activity against Streptococcus pneumoniae (sc)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.
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.
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.
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.
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.
AID117657In vivo potency against Staphylococcus aureus using mouse protection assay following s.c. administration.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-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.
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.
AID164245Antibacterial activity against Pseudomonas aeruginosa UI-181988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
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.
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.
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.
AID93881Minimum inhibitory concentration against Klebsiella pneumoniae MGH-2 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
AID209067Antibacterial activity against Streptococcus faecalis MGH-21988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
AID209126Antibacterial activity against Streptococcus pyogenes C2031988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
AID68013Antibacterial activity against Enterobacter cloacae MA26461988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
AID207974Minimum inhibitory concentration against Staphylococcus aureus H228 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID117656In vivo potency against Staphylococcus aureus using mouse protection assay following p.o. administration.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
AID207975Minimum inhibitory concentration against Staphylococcus aureus UC-76 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
AID69048Minimum concentration needed to produce linear DNA at an intensity relative to oxolinic at 10 ug/mL in Escherichia coli H560 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
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.
AID209894Antibacterial activity against Streptococcus pneumoniae SV-11988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
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.
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.
AID117659In vivo potency against Streptococcus pneumoniae using mouse protection assay following p.o. administration.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-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.
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.
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.
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.
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.
AID71070Concentration required to produce linear DNA from closed circular DNA by the denaturation of the drug-gyrase-DNA complex1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID202130Compounds 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.
AID69619Antibacterial activity against Escherichia coli H5601988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID163051Minimum inhibitory concentration against Providencia rettgeri H1771 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-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.
AID209759Minimum inhibitory concentration against Streptococcus pyogenes C203 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
AID208301Minimum inhibitory concentration against Streptococcus pneumoniae SV-1 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
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.
AID133824In vivo activity against Escherichia coli (sc)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.
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.
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.
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.
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.
AID117654In vivo potency against Escherichia coli vogel using mouse protection assay when given perorally1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
AID117655In vivo potency against Escherichia coli vogel using mouse protection assay when given subcutaneously1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
AID68519Minimum inhibitory concentration against Enterobacter cloacae HA 2646 in vitro.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids.
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.
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.
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.
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.
AID133947In vivo activity against Pseudomonas aeruginosa (sc)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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (36.36)18.7374
1990's6 (54.55)18.2507
2000's1 (9.09)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: 12.09

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 Index12.09 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.09)

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		3.68100aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
fleroxacin
Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.		2.3820difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
lomefloxacin
lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.		1.9710fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antimicrobial agent;
antitubercular agent;
photosensitizing agent
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		3.3670fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		2.67303-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		210N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
tosufloxacin
tosufloxacin: quinolone anti-infective agent; structure given in first source. tosufloxacin : A racemate comprising equimolar amounts of (R)- and (S)-tosufloxacin.. 7-(3-aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 3-aminopyrrolidin-1-yl substituents at positions 1, 6 and 7 respectively.		2.68301,8-naphthyridine derivative;
amino acid;
aminopyrrolidine;
monocarboxylic acid;
organofluorine compound;
primary amino compound;
quinolone antibiotic;
tertiary amino compound
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		1.9710monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
pefloxacin
Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.		2.3820fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
amifloxacin
amifloxacin: structure in UD		1.9710quinolines
difloxacin
difloxacin: RN & structure given in first source. difloxacin : A quinolone that is pefloxacin in which the ethyl group at position 1 of the quinolone has been replaced by a p-fluorophenyl group. A broad-spectrum antibiotic effective against both Gram-positive and Gram-negative bacteria, it is used (usually as the monohydrochloride salt) for the treatment of bacterial infections in dogs.		1.9710fluoroquinolone antibiotic;
monocarboxylic acid;
monofluorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
Mycoplasma genitalium metabolite
temafloxacin
temafloxacin: structure given in first source. temafloxacin : A racemate comprising equimolar amounts of (R)- and (S)-temafloxacin. Both enantiomers both exhibit similar pharmacological profiles. Temafloxacin was briefly used (either as the free base or as the hydrochloride salt) as an antibacterial drug but was withdrawn worldwide in 1992 following reports of serious side effects, including severe hypoglycaemia, haemolytic anaemia, liver and kidney dysfunction, anaphylaxis, and death.. 1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid : A quinolone that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted at positions 1, 6, and 7 by 2,4-difluorophenyl, fluorine, and 3-methylpiperazin-1-yl groups, respectively.		2.6730amino acid;
monocarboxylic acid;
N-arylpiperazine;
organofluorine compound;
quinolone antibiotic;
quinolone;
secondary amino compound;
tertiary amino compound
clinafloxacin
clinafloxacin: structure given in first source; RN given is for monoHCl		2.940quinolines
sparfloxacin
[no description available]		1.9710fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
enrofloxacin
Enrofloxacin: A fluoroquinolone antibacterial and antimycoplasma agent that is used in veterinary practice.. enrofloxacin : A quinolinemonocarboxylic acid that is 1,4-dihydroquinoline-3-carboxylic acid substituted by an oxo group at position 4, a fluoro group at position 6, a cyclopropyl group at position 1 and a 4-ethylpiperazin-1-yl group at position 7. It is a veterinary antibacterial agent used for the treatment of pets.		210cyclopropanes;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone		antibacterial agent;
antimicrobial agent;
antineoplastic agent
grepafloxacin
grepafloxacin: structure in first source		1.9710fluoroquinolone antibiotic;
quinolines;
quinolone antibiotic
pd 118879
[no description available]		2.940
ci 934
CI 934: structure given in first source		3.0850
pd-117596
PD-117596: structure given in first source		3.3670
8-fluorociprofloxacin
8-fluorociprofloxacin: structure given in first source		3.2360
pd 124816
PD 124816: structure given in first source		3.0850
pd 135042
PD 135042: inhibits DNA gyrase and topoisomerase IV; structure in first source		2.3920
ConditionIndicatedRelationship StrengthStudiesTrials
Bacterial Disease
[description not available]		02.6730
Actinic Reticuloid Syndrome
[description not available]		01.9810
Bacterial Infections
Infections by bacteria, general or unspecified.		02.6730
Benign Neoplasms
[description not available]		01.9710
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		01.9710