2-硫醚连接的喹诺酮基碳青霉烯类化合物的制备及抗菌活性评估

Preparation and antimicrobial assessment of 2-thioether-linked quinolonyl-carbapenems.

作者信息

Hershberger P M, Switzer A G, Yelm K E, Coleman M C, Devries C A, Rourke F J, Davis B W, Kraft W G, Twinem T L, Koenigs P M, Paule S M, Siehnel R J, Zoutendam P H, Imbus R, Demuth T P

机构信息

Procter & Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040-8006, USA.

出版信息

J Antibiot (Tokyo). 1998 Sep;51(9):857-71. doi: 10.7164/antibiotics.51.857.

DOI:10.7164/antibiotics.51.857

PMID:9820237

Abstract

This reports the synthesis and in vitro antimicrobial properties of a series of 2-thioether-linked quinolonyl-carbapenems. Although the title compounds exhibited broad spectrum activity, the MICs were generally higher than those observed for selected benchmark carbapenems, quinolonyl-penems, and quinolones. Enzyme assays suggested that the title compounds are potent inhibitors of penicillin binding proteins and inefficient inhibitors of bacterial DNA-gyrase. Uptake studies indicated that the new compounds are not substrates for the norA encoded quinolone efflux pump.

摘要

本文报道了一系列2-硫醚连接的喹诺酮基碳青霉烯类化合物的合成及其体外抗菌性能。尽管标题化合物表现出广谱活性，但其最低抑菌浓度（MIC）通常高于所选基准碳青霉烯类、喹诺酮基青霉烯类和喹诺酮类化合物所观察到的MIC。酶分析表明，标题化合物是青霉素结合蛋白的有效抑制剂，而对细菌DNA促旋酶的抑制作用较弱。摄取研究表明，新化合物不是norA编码的喹诺酮外排泵的底物。