6-(1-hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C β-lactamases -: II.

被引：16

作者：

Bitha, P ^{[1
]}

Li, Z ^{[1
]}

Francisco, GD ^{[1
]}

Yang, YJ ^{[1
]}

Petersen, PJ ^{[1
]}

Lenoy, E ^{[1
]}

Lin, YI ^{[1
]}

机构：

[1] Wyeth Ayerst Res, Chem Sci & Infect Dis, Pearl River, NY 10965 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(99)00107-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two stereoselective processes for the synthesis of novel 3,6-disubstituted penam sulfone derivatives were developed. One 6 beta-(l-hydroxyethyl) and four 6 beta-hydroxymethyl penam sulfone derivatives were synthesized. All four 6 beta-(hydroxymethyl)penam sulfone derivatives demonstrated good IC50 against both TEM-1 and AmpC beta-lactamases. of these, 6 beta-hydroxymethyl penam sulfone derivative 25 was the most active inhibitor which was able to restore the activity of piperacillin in vitro and in vivo against both TEM-1 and AmpC beta-lactamases producing organisms. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：997 / 1002

页数：6

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