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对革兰氏阳性菌具有选择性活性的喹诺酮类药物的制备及其体外和体内评价。

Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.

作者信息

Cooper C S, Klock P L, Chu D T, Hardy D J, Swanson R N, Plattner J J

机构信息

Anti-infective Research Division, Abbott Laboratories, Abbott Park, Illinois 60064-3500.

出版信息

J Med Chem. 1992 Apr 17;35(8):1392-8. doi: 10.1021/jm00086a007.

Abstract

A series of quinolones were prepared which contained oximes or substituted oximes as replacements for the amine substituents normally found on the pyrrolidine or piperidine fragments of quinolone antibacterial agents. These substituents led to compounds that had selective activity against Gram-positive organisms. These compounds showed in vivo activity against Staphylococcus aureus. Only compound 29 had in vivo activity against Streptococcus pneumoniae.

摘要

制备了一系列喹诺酮类化合物,其中含有肟或取代肟,以取代喹诺酮抗菌剂的吡咯烷或哌啶片段上通常存在的胺取代基。这些取代基产生了对革兰氏阳性菌具有选择性活性的化合物。这些化合物在体内对金黄色葡萄球菌有活性。只有化合物29在体内对肺炎链球菌有活性。

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