Synthesis of antimicrobial agents. 1. Syntheses and antibacterial activities of 7-(azole substituted)quinolones.
作者信息
Uno T, Takamatsu M, Inoue Y, Kawahata Y, Iuchi K, Tsukamoto G
机构信息
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
出版信息
J Med Chem. 1987 Dec;30(12):2163-9. doi: 10.1021/jm00395a001.
PMID:3681887
Abstract
A series of 6-fluoro- and 6,8-difluoro-7-(azole substituted)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids were prepared. Structure-activity relationship studies indicated that the antibacterial potency was better when the 6,8-substituents were fluorine atoms and the 7-substituent was either 1-imidazolyl, 20, or 4-methyl-1-imidazolyl, 25. From the results of studies on pharmacokinetic profile and toxicity, 20 and 25 were found to possess excellent antibacterial activities and to show high blood levels after oral administration to mice with low toxicity.
摘要
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