Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative

MP Wentland, RB Perni, PH Dorff…

文献索引：Wentland; Perni; Dorff; Rake Journal of Medicinal Chemistry, 1988 , vol. 31, # 9 p. 1694 - 1697

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被引用次数: 32

摘要

A novel conformationally restricted 1-cyclopropylquinolone (1) that incorporates structural features of both ofloxacin and ciprofloxacin has been prepared. Compound 1 was found to be a DNA gyrase inhibitor having potency similar to ofloxacin but less than ciprofloxacin. The cellular inhibitory and in vivo antibacterial potencies of 1 were found to be less than those of the two reference agents.