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Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.

作者信息

Wentland M P, Perni R B, Dorff P H, Rake J B

机构信息

Department of Medicinal Chemistry, Sterling-Winthrop Research Institute, Rensselaer, New York 12144.

出版信息

J Med Chem. 1988 Sep;31(9):1694-7. doi: 10.1021/jm00117a005.

DOI:10.1021/jm00117a005
PMID:2842501
Abstract

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.

摘要

相似文献

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引用本文的文献

1
Significance of the methyl group on the oxazine ring of ofloxacin derivatives in the inhibition of bacterial and mammalian type II topoisomerases.氧氟沙星衍生物恶嗪环上甲基在抑制细菌和哺乳动物II型拓扑异构酶中的意义。
Antimicrob Agents Chemother. 1991 Feb;35(2):309-12. doi: 10.1128/AAC.35.2.309.