Synthesis and biological evaluation of novel tricyclic carbapenems (trinems)

被引:6
作者
Kanno, O
Shimoji, Y
Ohya, S
Kawamoto, I
机构
[1] Sankyo Co Ltd, Med Chem Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
[2] Sankyo Co Ltd, Biol Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
关键词
D O I
10.7164/antibiotics.53.404
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Synthesis of new tricyclic carbapenems (trinems) with a pyrrolidinyl moiety at the C-4 position of the tricyclic ring and their antimicrobial activities were studied. These trinems showed potent activities against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). Among them, (4R)-[(S)-pyrrolidin-3-ylthiomethyl]trinem (14a) exhibited good activity against MRSA in vitro and in vivo.
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收藏
页码:404 / 414
页数:11
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