alpha-((tetronoyl)oxy)- and alpha-((tetramoyl)oxy)methyl ketone inhibitors of the interleukin-1 beta converting enzyme (ICE)

被引：17

作者：

Graybill, TL ^{[1
]}

Prouty, CP ^{[1
]}

Speier, GJ ^{[1
]}

Hoyer, D ^{[1
]}

Dolle, RE ^{[1
]}

Helaszek, CT ^{[1
]}

Ator, MA ^{[1
]}

Uhl, J ^{[1
]}

Strasters, J ^{[1
]}

机构：

[1] SANOFI WINTHROP INC,MALVERN,PA 19355

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(96)00574-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aryl-substituted tetronic acids, tetramic acids, and cyclic beta-dicarbonyl moieties were evaluated as leaving groups in the peptidyl-COCH2-X type inhibitor iii. Tripeptidyl aspartyl alpha-((tetronoyl)oxy)- and alpha-((tetramoyl)oxy)methyl ketone derivatives demonstrate potent time-dependent inhibition (k(obs)/[T] 100,000-250,000 M(-1)s(-1)) of the cysteine protease ICE. Copyright (C) 1996 Elsevier Science Ltd

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页码：41 / 46

页数：6

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