SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 7-[3-(1-AMINOALKYL)PYRROLIDINYL]QUINOLONE AND 7-[3-(1-AMINOCYCLOALKYL)PYRROLIDINYL]QUINOLONE ANTIBACTERIALS

Authors
KIMURA Y ATARASHI S TAKAHASHI M HAYAKAWA I
Citation
Y. Kimura et al., SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF 7-[3-(1-AMINOALKYL)PYRROLIDINYL]QUINOLONE AND 7-[3-(1-AMINOCYCLOALKYL)PYRROLIDINYL]QUINOLONE ANTIBACTERIALS, Chemical and Pharmaceutical Bulletin, 42(7), 1994, pp. 1442-1454
Citations number
23
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
42
Issue
7
Year of publication
1994
Pages
1442 - 1454
Database
ISI
SICI code
0009-2363(1994)42:7<1442:SASO7>2.0.ZU;2-N
Abstract
A series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1-pyrrolidinyl] quinolones have been prepared and their biological properties evaluate d. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacte rial activities against gram-positive and gram-negative organisms. The y had moderate lipophilicity and high aqueous solubility compared to t heir aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidin yl compound (83) showed superior pharmacokinetic properties to its ami nomethyl counterpart (6).