EXAMINATION OF PEPTIDIC ALPHA',BETA-DIAMINO-ALPHA,ALPHA-DIFLUOROKETONES AS INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE

被引：13

作者：

BERNSTEIN, PR ^{[1
]}

KOSMIDER, BJ ^{[1
]}

VACEK, EP ^{[1
]}

VEALE, CA ^{[1
]}

GOMES, BC ^{[1
]}

机构：

[1] ZENECA PHARMACEUT GRP,DEPT PHARMACOL,WILMINGTON,DE 19897

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)80066-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The preparation and in vitro evaluation of a series of peptidic alpha',beta-diamino-alpha,alpha-difluoroketones are described. Comparison of the efficacy of these compounds to both their corresponding trifluoromethylketone and alpha-carboxamido-alpha,alpha-difluoroketone inhibitors reveals a divergent set of structure-activity relationships. This divergence indicates that the inhibitor's P-l'-amino group is strongly interacting with the enzyme's S-l'-subsite.

引用

页码：2175 / 2178

页数：4

共 14 条

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