一种新型碳青霉烯类抗生素SM-7338的构效关系。

A novel carbapenem antibiotic, SM-7338 structure-activity relationships.

作者信息

Sunagawa M, Matsumura H, Inoue T, Fukasawa M, Kato M

机构信息

Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd., Osaka, Japan.

出版信息

J Antibiot (Tokyo). 1990 May;43(5):519-32. doi: 10.7164/antibiotics.43.519.

DOI:10.7164/antibiotics.43.519

PMID:2358404

Abstract

A series of new carbapenem compounds, which have a pyrrolidin-3'-ylthio group substituted with various aminocarbonyl group at C-5' position as C-2 side chain, have been prepared. The antibacterial activity and the stability to renal dehydropeptidase-I of these compounds were investigated, and the structure-activity relationships were discussed. In this series, SM-7338; (1R,5S,6S)-2-[(3S,5S)-5-dimethylaminocarbonylpyrrolidin-3-ylthi o]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid (5a) was the most interesting compound.

摘要

已经制备了一系列新的碳青霉烯化合物，其在C-2侧链的C-5′位具有被各种氨基羰基取代的吡咯烷-3'-硫基。研究了这些化合物的抗菌活性和对肾脱氢肽酶-I的稳定性，并讨论了构效关系。在该系列中，SM-7338；(1R,5S,6S)-2-[(3S,5S)-5-二甲基氨基羰基吡咯烷-3-硫基]-6-[(R)-1-羟乙基]-1-甲基碳青霉-2-烯-3-羧酸(5a)是最引人关注的化合物。