INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE .2. SYNTHESIS AND SAR OF BENZISOTHIAZOLINYLMETHYL ARYL ETHERS

被引：12

作者：

SUBRAMANYAM, C

BELL, MR

FERGUSON, E

GORDON, RG

DUNLAP, RP

FRANKE, C

MURA, AJ

机构：

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

[2] EASTMAN KODAK CO, RES LABS, ROCHESTER, NY 14650 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 04期

关键词：

D O I：

10.1016/0960-894X(95)00028-R

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-isopropyl benzisothiazolinylmethyl aryl ethers were prepared and evaluated as inhibitors of human leukocyte elastase (HLE). Among the phenols attached as leaving groups onto N-methyl of the 4-isopropyl benzisothiazolone nucleus, the sulfonamido phenol 26 was found to be the best. Compound 7i with K-i(*) = 0.8 nM was the most potent inhibitor in this series.

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页码：319 / 324

页数：6

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