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4-吡咯烷基硫代碳青霉烯类化合物的合成及其抗菌活性:含杂芳环作为侧链

Synthesis and antibacterial activities of 4-pyrrolidinylthio carbapenems: containing heteroaromatics as a side chain.

作者信息

Cho Han-Won, Oh Chang-Hyun, Lee Ju-Shin, Lee Soo-Chul, Choi Jung-Hoon, Cho Jung-Hyuck

机构信息

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

出版信息

Arch Pharm (Weinheim). 2003 Nov;336(11):495-503. doi: 10.1002/ardp.200300728.

Abstract

The synthesis of a new series of 2-alkyl-4-pyrrolidinylthio-b-methylcarbapenems containing the substituted heteroaromatic moieties is described. Their in vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested. The effect of substituents on the nitrogen atoms at heteroaromatic rings was investigated. Particular compounds (14 b, 14 c) containing 3-methyl- and 3, 5-dimethylpyrazolethio substituted moiety showed the most potent antibacterial activity.

摘要

描述了一系列含取代杂芳基部分的新型2-烷基-4-吡咯烷基硫代-β-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。研究了杂芳环上氮原子上取代基的影响。含有3-甲基和3,5-二甲基吡唑硫代取代部分的特定化合物(14b,14c)表现出最强的抗菌活性。

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