Synthesis and structural optimization of 7-(3,3-disubstituted-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-mehtoxy-4-oxo-3-quinolinecarboxylic acids as antibacterial agents

被引:12
|
作者
Kitani, H
Kuroda, T
Moriguchi, A
Ao, H
Hirayama, F
Ikeda, Y
Kawakita, T
机构
[1] Research Laboratories, Yoshitomi Pharmaceut. Indust., Ltd., Chikujo-gun, Fukuoka 871, 955 Koiwai, Yoshitomi-cho
关键词
D O I
10.1016/S0960-894X(97)00054-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of the titled compounds were synthesized and tested for antibacterial activities in comparison with typical fluoroquinolones. (S)-3-Aminomethyl-3-fluoromethyl derivative (Y-688) was confirmed to be optimal because ofbeing most active especially against Gram-positive bacteria including fluoroquinolone-resistant strains and showing high photostability. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:515 / 520
页数:6
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