A novel antibacterial 8-chloroquinolone with a distorted orientation of the N1-(5-amino-2, 4-difluorophenyl) group

…, Y Ohshita, J Yoshida, A Yazaki, M Shiro…

Index: Kuramoto, Yasuhiro; Ohshita, Yoshihiro; Yoshida, Jiro; Yazaki, Akira; Shiro, Motoo; Koike, Tohru Journal of Medicinal Chemistry, 2003 , vol. 46, # 10 p. 1905 - 1917

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Citation Number: 40

Abstract

Fluoroquinolones represent a major class of antibacterial agents with great therapeutic potential. In this study, we designed m-aminophenyl groups as novel N-1 substituents of naphthyridones and quinolones. Among newly synthesized compounds, 7-(3-aminoazetidin- 1-yl)-1-(5-amino-2, 4-difluorophenyl)-8-chloro-6-fluoro-4-oxo-1, 4-dihydroquinoline-3- carboxylic acid (4) has extremely potent antibacterial activities against Gram (+) as well as ...