Synthesis and antibacterial activity of novel 4-pyrrolidinylthio carbapenems .1. 2-alkoxymethyl derivatives

被引：8

作者：

Azami, H

Tsutsumi, H

Matsuda, K

Barrett, D

Hattori, K

Nakajima, T

Kuroda, S

Kamimura, T

Murata, M

机构：

[1] Med. Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka 532, 2-1-6 Kashima, Yodogawa-ku

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 11期

关键词：

D O I：

10.1016/S0968-0896(97)00142-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis and in vitro antibacterial activity of a novel series of 2-alkoxymethyl-4-pyrrolidinylthio-1 beta-methyl carbapenems are described. As a result of these studies, we discovered that FR27743 (19j) containing a novel,2-fluoroethoxymethyl substituent possesses a broad spectrum of antibacterial activity against both Gram-positive and Gram-negative organisms, including Pseudomonas aeruginosa. Furthermore, FR27743 exhibited excellent stability against renal dehydropeptidase-I (DHP-I), good urinary recovery, and superior in vivo activity compared to that for Meropenem against several systemic infections. (C) 1997 Elsevier Science Ltd.

引用

页码：2069 / 2087

页数：19

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