ALKOXY-SUBSTITUTED BENZISOTHIAZOLONE (BIT) DERIVATIVES - POTENT INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE

被引:13
作者
DESAI, RC
DUNLAP, RP
FARRELL, RP
FERGUSON, E
FRANKE, CA
GORDON, R
HLASTA, DJ
TALOMIE, TG
机构
[1] STERLING WINTHROP INC, DIV PHARMACEUT RES, DEPT BIOCHEM, COLLEGEVILLE, PA 19426 USA
[2] STERLING WINTHROP INC, DIV PHARMACEUT RES, DEPT VASC PHARMACOL, COLLEGEVILLE, PA 19426 USA
[3] EASTMAN KODAK CO, RES LABS, ROCHESTER, NY 14650 USA
关键词
D O I
10.1016/0960-894X(94)00466-S
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Alkoxy substituted benzisothiazolones (BIT) are reported as inhibitors of human leukocyte elastase (HLE). Structure-activity relationship study results are described. The contribution of alkoxy substituents towards improving the stability of BIT derivatives in human blood is discussed. WIN 68769 (12) with a K-i* = 0.022 nM is the most potent analog synthesized in this series.
引用
收藏
页码:105 / 109
页数:5
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