β-carbonyl substituted glutathione conjugates as inhibitors of O-volvulus GST2

被引：20

作者：

Brophy, PM

Campbell, AM

van Eldik, AJ

Teesdale-Spittle, PH

Liebau, E

Wang, MF

机构：

[1] De Montfort Univ, Dept Chem, Leicester LE1 9BH, Leics, England

[2] Univ Wales, Inst Biol Sci, Aberystwyth SY23 3DA, Dyfed, Wales

[3] Bernhard Nocht Inst Trop Med, Hamburg, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)00142-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of beta-carbonyl substituted glutathione conjugates were prepared and evaluated as inhibitors of OvGST2. Their specificity for the parasite derived protein was assessed through comparison with their inhibition of human pi GST. Inhibition of OvGST2 has been demonstrated at low micromolar concentrations for these conjugates and selectivity for OvGST2 over human pi-GST of greater than 10-fold has been achieved. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：979 / 981

页数：3

共 7 条

[1] GLUTATHIONE S-TRANSFERASES - REACTION-MECHANISM, STRUCTURE, AND FUNCTION [J].