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具有螺[2,4]庚烷部分的新型1β-甲基碳青霉烯类化合物的合成及体外活性

Synthesis and in-vitro activity of novel 1beta-methylcarbapenems having spiro[2,4]heptane moieties.

作者信息

Park Hyeong Beom, Jo Nam Hyun, Hong Joon Hee, Choi Jung Hoon, Cho Jung-Hyuck, Yoo Kyung Ho, Oh Chang-Hyun

机构信息

Department of Chemistry, Hanyang University, Seoul, Korea.

出版信息

Arch Pharm (Weinheim). 2007 Oct;340(10):530-7. doi: 10.1002/ardp.200700060.

Abstract

The synthesis of a new series of 1beta-methylcarbapenems having spiro[2,4]heptane moieties is described. Their in-vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. Most compounds were shown to be more active than the compared meropenem and imipenem against Escherichia coli. One particular compound, IIIb, having hydroxy a moiety showed the most potent antibacterial activity.

摘要

描述了一系列具有螺[2,4]庚烷部分的新型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,并研究了取代基对吡咯烷环的影响。结果表明,大多数化合物对大肠杆菌的活性比对照美罗培南和亚胺培南更强。一种具有羟基部分的特定化合物IIIb表现出最有效的抗菌活性。

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