Compounds > pd 124816
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pd 124816

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Description

PD 124816: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID130713
CHEMBL ID15186
SCHEMBL ID8922019
MeSH IDM0164477

Synonyms (16)

Synonym
3-quinolinecarboxylic acid, 1,4-dihydro-5-amino-7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-4-oxo-
pd 124816
CHEMBL15186 ,
5-amino-7-(3-aminopyrrolidin-1-yl)-1-cyclopropyl-6,8-difluoro-4-oxoquinoline-3-carboxylic acid
112654-98-5
3-quinolinecarboxylic acid, 5-amino-7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-
4fjj4s79yv ,
5-amino-7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
unii-4fjj4s79yv
3-quinolinecarboxylicacid,5-amino-7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-
SCHEMBL8922019
pd-124816
DTXSID50920860
5-amino-7-(3-aminopyrrolidin-1-yl)-1-cyclopropyl-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
bdbm50227274
Q27259527
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (91)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
AID65042In vitro concentration inhibiting DNA gyrase induced cleavage in Escherichia coli H560.1992Journal 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.
AID165206In vitro antibacterial activity was tested for Pseudomonas aeruginosa UI-181995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
AID209232In vitro antibacterial activity was tested for Streptococcus faecalis MGH-21995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
AID213599Clonogenic cytotoxicity against Chinese hamster V-79 cells1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
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.
AID209612In vitro antibacterial activity was tested for Streptococcus pyogenes C2031995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
AID68676In vitro antibacterial activity was tested for Escherichia coli Vogel1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID163740In vitro antibacterial activity was tested for Providencia rettgeri H17711995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
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.
AID68339In vitro antibacterial activity was tested for Enterobacter cloacae HA26461995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID96407In vitro antibacterial activity was tested for Klebsiella pneumoniae MGH-21995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID94147In vitro antibacterial activity against gram negative Klebsiella pneumoniae 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.
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.
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.
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.
AID206764In vitro antibacterial activity was tested for Staphylococcus aureus H2281995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
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.
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.
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.
AID206765In vitro antibacterial activity was tested for Staphylococcus aureus UC-761995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
AID68675In vitro antibacterial activity was tested for Escherichia coli H5601995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
AID208121In vitro antibacterial activity was tested for Streptococcus pneumoniae SV-11995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
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.
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.
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.
AID118113Phototoxic skin reaction in depilated female CD-1 mice1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
The synthesis, structure-activity, and structure-side effect relationships of a series of 8-alkoxy- and 5-amino-8-alkoxyquinolone antibacterial agents.
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.
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.
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.
AID130079Compounds were 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.
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.
[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-19902 (22.22)18.7374
1990's6 (66.67)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: 12.42

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 Index12.42 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.82 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.42)

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%
Other10 (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.		3.3770aminoquinoline;
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
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.		2.6830fluoroquinolone 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.		2.38203-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.		2.9401,8-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.		2.3820monohydroxyquinoline;
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.		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.		2.3920amino 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]		2.6730fluoroquinolone 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		3.0850
pd 118879
[no description available]		3.0850
ci 934
CI 934: structure given in first source		2.6830
pd-117596
PD-117596: structure given in first source		3.0850
8-fluorociprofloxacin
8-fluorociprofloxacin: structure given in first source		2.6730
pd 135042
PD 135042: inhibits DNA gyrase and topoisomerase IV; structure in first source		2.6830
ConditionIndicatedRelationship StrengthStudiesTrials
Bacterial Disease
[description not available]		01.9710
Bacterial Infections
Infections by bacteria, general or unspecified.		01.9710
Dermatitis, Contact, Phototoxic
[description not available]		01.9810
Abnormalities, Autosome
[description not available]		01.9910
Chromosome-Defective Micronuclei
[description not available]		01.9910
E coli Infections
[description not available]		01.9710
Escherichia coli Infections
Infections with bacteria of the species ESCHERICHIA COLI.		01.9710