SYNTHESIS AND EVALUATION OF DIACYLHYDRAZINES AS INHIBITORS OF THE INTERLEUKIN-1-BETA CONVERTING-ENZYME (ICE)

被引：11

作者：

GRAYBILL, TL

DOLLE, RE

HELASZEK, CT

ATOR, MA

STRASTERS, J

机构：

[1] STERLING WINTHROP PHARMACEUT RES DIV,DEPT BIOCHEM,COLLEGEVILLE,PA 19426

[2] STERLING WINTHROP PHARMACEUT RES DIV,DEPT ANALYT CHEM,COLLEGEVILLE,PA 19426

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 11期

关键词：

D O I：

10.1016/0960-894X(95)00194-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Diacylhydrazines ([azaAsp(1)] derivatives) were prepared and shown to inactivate ICE in a time-dependent manner. Inactivation rates for most of these diacylhydrazines were 10-fold slower than their alpha-substituted methylketone congeners. Rates for 6 and 7 (ca. 18,000 M(-1)s(-1)) compared favorably to those reported for Ac-Tyr-Val-Ala-Asp-CH-N-2 and azapeptide inhibitors for other cysteine proteases.

引用

页码：1197 / 1202

页数：6

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