Compounds > pd 118879
Page last updated: 2024-12-07

pd 118879

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Cross-References

ID SourceID
PubMed CID99921
CHEMBL ID276583
SCHEMBL ID4575476
MeSH IDM0194909

Synonyms (16)

Synonym
1,8-naphthyridine-3-carboxylic acid, 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-
pd 118879
96568-33-1
7-(3-aminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
pd-118879
OPREA1_592820
CHEMBL276583 ,
7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
7-[3-amino-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
MUKSDTOOLRNSIO-UHFFFAOYSA-N ,
7-[3-amino-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4- dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
SCHEMBL4575476
AKOS030559253
7-(3-aminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
DTXSID70914448
bdbm50230833
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (89)

Assay IDTitleYearJournalArticle
AID117684Protective dose in vivo was determined in acute, lethal systemic infections in female Charles River CD-1 mice against Streptococcus pyogenes C-2031993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains.
AID133966In vivo potency against acute systemic infection in mouse caused by Pseudomonas aeruginosa. UI-18. on subcutaneous injection.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID23546Aqueous solubility1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
AID208922In vitro minimum inhibitory concentration against Streptococcus bovis A5169 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
AID23549Solubility (at pH 7.4)1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
AID53451Inhibition against DNA gyrase1993Journal 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.
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.
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.
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.
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.
AID133968In vivo potency against acute systemic infection in mouse caused by Streptococcus pneumoniae SV-1 on oral administration by gavage.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
AID117682Protective dose in vivo was determined in acute, lethal systemic infections in female Charles River CD-1 mice against Escherichia coli Vogel1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains.
AID66105In vitro minimum inhibitory concentration against Enterococcus faecium ATCC 8043 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
AID78549In vitro concentration inhibiting DNA gyrase induced cleavage in Escherichia coli H5601992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
AID201951In vitro antibacterial activity against gram positive Streptococcus pneumoniae SV-1.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID201273In vitro antibacterial activity against gram positive Staphylococcus aureus H-228.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
AID65397In vitro antibacterial activity against gram positive Enterococcus faecalis MGH-2.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID30275In vitro minimum inhibitory concentration against Acinetobacter CMX 669 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
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.
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.
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.
AID53322Inhibition of the gyrase mediated cleavage of supercoiled DNA1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains.
AID133962In vivo potency against acute systemic infection in mouse caused by Escherichia coli vogel on subcutaneous injection.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID133970In vivo potency against acute systemic infection in mouse caused by Streptococcus pneumoniae SV-1 on subcutaneous injection.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID201409In vitro antibacterial activity against gram positive Staphylococcus aureus UC76.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID94148In vitro antibacterial activity against gram negative Klebsiella pneumoniae. MGH-21992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID202109In vitro antibacterial activity against gram positive Streptococcus pyogenes C-203.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID65233In vitro antibacterial activity against gram negative Escherichia coli Vogel.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID70772In vitro minimum inhibitory concentration against Escherichia coli Juhl using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
AID203284In vitro minimum inhibitory concentration against Staphylococcus aureus A 5177 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
AID133972In vivo potency against acute systemic infection in mouse caused by Streptococcus pyogenes C-203 on oral administration by gavage1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas 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.
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.
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.
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.
AID67874In vitro minimum inhibitory concentration against Enterobacter aerogenes ATCC 13048 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
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.
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.
AID203290In vitro minimum inhibitory concentration against Staphylococcus epidermidis 3159 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
AID210254In vitro minimum inhibitory concentration against Streptococcus pyogenes 930 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
AID64389In vitro antibacterial activity against gram negative Enterobacter cloacae MA 2646.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID94220In vitro minimum inhibitory concentration against Klebsiella pneumoniae 8045 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
AID151528In vitro antibacterial activity against gram negative Pseudomonas aeruginosa UI-18.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID74728Geometric mean of MIC was determined in vitro against gram-negative strains using standard microtitration techniques1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains.
AID164088In vitro minimum inhibitory concentration against Pseudomonas aeruginosa K799 / WT using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
AID133960In vivo potency against acute systemic infection in mouse caused by Escherichia coli Vogel on oral administration by gavage.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
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.
AID203286In vitro minimum inhibitory concentration against Staphylococcus aureus CMX 553 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
AID207547In vitro minimum inhibitory concentration against Staphylococcus aureus ATCC 6538P using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
AID208884In vitro minimum inhibitory concentration against Streptococcus agalactiae CMX 508 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
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.
AID163947In vitro minimum inhibitory concentration against Pseudomonas aeruginosa A5007 using brain-heart infusion agar1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
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.
AID208936Antibacterial activity expressed as Minimum 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.
AID213589Clonogenic cytotoxicity against hamster V-79 cells1993Journal 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.
AID213606Clonogenic 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.
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.
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.
AID50848In 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.
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.
AID23544Solubility (at pH 4)1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID124937phototoxic 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.
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.
AID130070Compound was evaluated for phototoxicity no-effect dose 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.
AID74854Geometric mean of MIC was determined in vitro against gram-positive strains using standard microtitration techniques1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Quinolone antibacterials: synthesis and biological activity of carbon isosteres of the 1-piperazinyl and 3-amino-1-pyrrolidinyl side chains.
AID133974In vivo potency against acute systemic infection in mouse caused by Streptococcus pyogenes C-203 on subcutaneous injection1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
AID23542Solubility (in 0.1 N HCl)1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
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.
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.
AID133965In vivo potency against acute systemic infection in mouse caused by Pseudomonas aeruginosa UI-18 on oral administration by gavage.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
AID152317In vitro antibacterial activity against gram negative Providencia rettgeri M-1771.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Quinolone antibacterial agents. Synthesis and structure-activity relationships of a series of amino acid prodrugs of racemic and chiral 7-(3-amino-1-pyrrolidinyl)quinolones. Highly soluble quinolone prodrugs with in vivo pseudomonas activity.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (11.11)18.7374
1990's7 (77.78)18.2507
2000's1 (11.11)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: 12.96

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 Index12.96 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index5.26 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.96)

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%
Other9 (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.		3.4880aminoquinoline;
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.		1.9810difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
nalidixic acid
[no description available]		1.97101,8-naphthyridine derivative;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
DNA synthesis inhibitor
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.		2.3920fluoroquinolone 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.		1.98103-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.		2.420N-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.		3.23601,8-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
4-nitrosodimethylaniline
4-nitrosodimethylaniline: structure; RN given refers to parent cpd. N,N-dimethyl-4-nitrosoaniline : A member of the class of dimethylanilines that is N,N-dimethylaniline having a nitroso group at the 4-position.		1.9710dimethylaniline;
nitroso compound;
tertiary amino compound
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.		1.9810fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
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.		210amino 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		2.6830quinolines
sparfloxacin
[no description available]		2.3920fluoroquinolone 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
pd 131628
PD 131628: CI-990 is L-alanylamide prodrug of PD-131628; structure given in first source		1.9810
pd 117588
PD 117588: structure given in first source		2.940
ci 934
CI 934: structure given in first source		2.3920
pd-117596
PD-117596: structure given in first source		3.0850
8-fluorociprofloxacin
8-fluorociprofloxacin: structure given in first source		2.3820
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		2.6830
thiobarbituric acid
thiobarbituric acid: RN given refers to parent cpd. 2-thiobarbituric acid : A barbiturate, the structure of which is that of barbituric acid in which the oxygen at C-2 is replaced by sulfur.		1.9710barbituratesallergen;
reagent
ConditionIndicatedRelationship StrengthStudiesTrials
E coli Infections
[description not available]		01.9810
Escherichia coli Infections
Infections with bacteria of the species ESCHERICHIA COLI.		01.9810
Dermatitis, Contact, Phototoxic
[description not available]		01.9810
Extravascular Hemolysis
[description not available]		01.9710
Hemolysis
The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.		01.9710