Structural variations in keto-glutamines for improved inhibition against hepatitis A virus 3C proteinase

被引：149

作者：

Jain, RP ^{[1
]}

Vederas, JC ^{[1
]}

机构：

[1] Univ Alberta, Dept Chem, Edmonton, AB T6G 2G2, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 14期

基金：

加拿大自然科学与工程研究理事会;

关键词：

cysteine protease; hepatitis A virus; inhibitors; glutamine analogs; phthalhydrazides;

D O I：

10.1016/j.bmcl.2004.05.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of keto-glutamine tetrapeptide analogs containing a 2-oxo-pyrrolidine ring as a glutamine side chain mimic were synthesized with both R and S configuration at the beta-carbon. Compounds bearing a phthalhydrazide moiety show improved reversible inhibition of HAV 3C proteinase in the low micromolar range. (C) 2004 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3655 / 3658

页数：4

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