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1β-甲基-2-(5-取代咪唑啉基吡咯烷-3-硫基)碳青霉烯衍生物的合成及其抗菌活性

Synthesis and antibacterial activity of 1 beta-methyl-2-(5-substituted imidazolino pyrrolidin-3-ylthio)carbapenem derivatives.

作者信息

Oh Chang-Hyun, Lee Chang-Sik, Lee Jong-Sun, Cho Jung-Hyuck

机构信息

Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul 130-650, Korea.

出版信息

Arch Pharm (Weinheim). 2003 Nov;336(11):504-9. doi: 10.1002/ardp.200300756.

Abstract

The synthesis of a new series of 1 beta-methylcarbapenems containing a substituted imidazolino pyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of the substituent on the imidazoline ring was investigated. Compound 13 g which has a N-sulfonylmethyl substituted imidazoline moiety showed the most potent antibacterial activity.

摘要

描述了一系列含有取代咪唑啉吡咯烷部分的新型1β-甲基碳青霉烯的合成。测试了它们对革兰氏阳性菌和革兰氏阴性菌的体外抗菌活性,并研究了咪唑啉环上取代基的影响。具有N-磺酰基甲基取代咪唑啉部分的化合物13g表现出最强的抗菌活性。

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