Synthesis and biological activity of 1β-methyl-2-[5-(2-N-substituted aminoethylcarbamoyl)pyrrolidin-3-ylthio]carbapenem derivatives

被引：11
作者：
Oh, CH
Lee, SC
Cho, JH [1 ]
机构：
[1] Korea Inst Sci & Technol, Med Chem Res Ctr, Seoul 130650, South Korea
[2] Hawon Pharm Co, Seoul 135080, South Korea
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 38卷 / 09期
关键词：
1; beta-methylcarbapenem; antibacterial activity; substituent effect;
D O I：
10.1016/S0223-5234(03)00143-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of a new series of 1beta-methylcarbapenems having the substituted aminoethylcarbamoylpyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive including MRSA and Gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. In particular, the compound 11g having piperazinyl urea moiety showed the most potent antibacterial activity and Ilk exhibited excellent anti-MRSA. (C) 2003 editions scientifiques et medicales Elsevier SAS. All rights reserved.
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收藏
页码：841 / 850
页数：10
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