Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1, 3] thiazeto [3, 2-a] quinoline-3-carboxylic acids

…, K Kazuno, M Matsuoka, I Shirahase…

文献索引：Segawa, Jun; Kitano, Masahiko; Kazuno, Kenji; Matsuoka, Masato; Shirahase, Ichiro; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 25 p. 4727 - 4738

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被引用次数: 45

摘要

A series of [1, 3] thiazeto [3, 2-alquinoline-3-carboxylic acids and their esters were prepared and evaluated for antibacterial activity. The derivatives with a hydrogen or methyl group at (2- 1, fluorine at (2-6, and piperazinyl or 4-methyl-1-piperazinyl group at C-7 showed superior in vitro antibacterial activity, and the derivatives with 4-methyl-1-piperazinyl group at C-7 had potent in vivo activity. Compound 29a (NM394) showed excellent in vitro antibacterial ...