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

被引：148
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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