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1β-甲基-2-[5-(1-甲氧基亚氨基-2-取代磺酰胺基乙基)吡咯烷-3-硫基]碳青霉烯类及其相关化合物的合成与抗菌活性评价

Synthesis and antibacterial evaluation of 1beta-methyl-2-[5-(1-methoxyimino-2-substituted sulfonamide ethyl)pyrrolidin-3-ylthio]carbapenems and their related compounds.

作者信息

Jeon Heechol, Jo Nam Hyun, Yoo Kyung Ho, Choi Joung-Hoon, Cho Heeyeong, Cho Jung-Hyuck, Oh Chang-Hyun

机构信息

Department of Chemistry, Hanyang University, Seoul 133-791, Republic of Korea.

出版信息

Eur J Med Chem. 2007 Mar;42(3):358-64. doi: 10.1016/j.ejmech.2006.10.006. Epub 2006 Dec 6.

DOI:10.1016/j.ejmech.2006.10.006
PMID:17156896
Abstract

The synthesis of a new series of 1beta-methylcarbapenems having methoxyimine and substituted sulfonamide 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. A particular compound (IIIc) having methylaminosulfonamide moiety showed the most potent antibacterial activity.

摘要

描述了一系列具有甲氧基亚胺和取代磺酰胺部分的新型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。具有甲氨基磺酰胺部分的特定化合物（IIIc）表现出最强的抗菌活性。

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