Evaluation of phosphorus-containing inhibitors of γ-Glutamyl Hydrolase

被引：5

作者：

Rodriguez, CE ^{[1
]}

Holmes, HM ^{[1
]}

Mlodnosky, KL ^{[1
]}

Lam, VQ ^{[1
]}

Berkman, CE ^{[1
]}

机构：

[1] San Francisco State Univ, Dept Chem & Biochem, San Francisco, CA 94132 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(98)00253-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several putative, phosphorus-containing inhibitors of gamma-glutamyl hydrolase were synthesized and evaluated for inhibitory activity. The phosphonamidoic acids were shown to be weak competitive inhibitors while both a phosphoramidate diester and a phosphonamidate ester were shown to be potent time-dependent inactivators, presumably through irreversible phosphorylation of an active site nucleophile. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1521 / 1524

页数：4

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