A NOVEL CARBAPENEM ANTIBIOTIC, SM-7338 STRUCTURE-ACTIVITY-RELATIONSHIPS

被引：195

作者：

SUNAGAWA, M

MATSUMURA, H

INOUE, T

FUKASAWA, M

KATO, M

机构：

[1] Research Laboratories, Sumitomo Pharmaceuticals Co., Ltd., Osaka 554

来源：

JOURNAL OF ANTIBIOTICS | 1990年 / 43卷 / 05期

关键词：

D O I：

10.7164/antibiotics.43.519

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：

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-ylthio]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid (5a) was the most interesting compound. © 1990, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.

引用

页码：519 / 532

页数：14

共 12 条

[1]

ANDRUS A, 1985, RECENT ADV CHEM BETA, P86

[2]

CAMBELL BJ, 1970, METHOD ENZYMOL, V19, P722

[3] PREPARATION OF LAEVOROTATORY TRANS-(4S,6S)-4,6-DIMETHYL-1,3-DITHIANE AND TRANS-(4S,6S)-4,6-DIMETHYL-1,3-OXATHIANE - INTERNAL DISPLACEMENT OF A SECONDARY SULFONATE LEADING TO A CYCLIC THIOACETAL [J].