Studies on quinolone antibacterials. IV. Structure-activity relationships of antibacterial activity and side effects for 5-or 8-substituted and 5, 8-disubstituted-7-(3-amino-1 …

…, M KAKIUCHI, Y TAKAHASHI, M ITAKURA…

Index: Yoshida; Yamamoto; Orita; Kakiuchi; Takahashi; Itakura; Kado; Mitani; Yasuda; Kato; Itoh Chemical and Pharmaceutical Bulletin, 1996 , vol. 44, # 5 p. 1074 - 1085

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Citation Number: 29

Abstract

A series of 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-1, 4-dihydro-4-oxoquinoline-3- carboxylic acids bearing various substituents (H, F, Cl, Me, OH, OMe, OEt, OCH 2 F, OCHF 2, OCF 3, SMe) at the C-8 position was prepared and evaluated for in vitro antibacterial activity against both standard laboratory strains and bacteria resistant to quinolones such as ciprofloxacin (CPFX, 1) and ofloxacin (OFLX, 2) from clinical isolates. The 8-methyl (8a), 8- ...