Stereoselective synthesis and antibacterial evaluation of 4-amido-isothiazolidinone oxides

被引：21

作者：

Chen, ZL ^{[1
]}

Demuth, TP ^{[1
]}

Wireko, FC ^{[1
]}

机构：

[1] Procter & Gamble Pharmaceut, Mason, OH 45040 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)00409-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two well-defined oxidative chlorination-cyclization processes have been developed for the stereoselective synthesis of a variety of 4-amido-isothiazolidinone oxide derivatives. The stereochemistry of the cyclization products was confirmed by X-ray crystallography. These new compounds were designed as bacterial serine protease inhibitors. In tests. some of them showed weak antibacterial activity. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：2111 / 2115

页数：5

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