INHIBITION OF INTERLEUKIN-1-BETA CONVERTING-ENZYME BY N-ACYL-ASPARTYL ARYLOXYMETHYL KETONES

被引：8

作者：

MJALLI, AMM

ZHAO, JJ

CHAPMAN, KT

THORNBERRY, NA

PETERSON, EP

MACCOSS, M

HAGMANN, WK

机构：

[1] MERCK SHARP & DOHME RES LABS,DEPT MED CHEM,RAHWAY,NJ 07065

[2] MERCK SHARP & DOHME RES LABS,DEPT BIOCHEM,RAHWAY,NJ 07065

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 13期

关键词：

D O I：

10.1016/0960-894X(95)00232-I

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of N-allyloxy-aspartyl aryloxymethyl ketones and their evaluation as inhibitors of interleukin-1 beta converting enzyme (ICE) are described. 3-Substituted 2-naphthyloxymethyl ketones were found to have K-i's of 90-500 nM. The SAR suggests that the substituents on the aryloxy group may have a specific binding interaction in the active site of ICE.

引用

收藏

页码：1409 / 1414

页数：6

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