Author/Authors :
Ranjit C. Desai، نويسنده , , Richard P. Dunlap، نويسنده , , Robert P. Farrell، نويسنده , , Edward Ferguson، نويسنده , , Catherine A. Franke، نويسنده , , Robert Gordon، نويسنده , , Dennis J. Hlasta، نويسنده , , Timothy G. Talomie، نويسنده ,
Abstract :
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 Ki* = 0.022 nM is the most potent analog synthesized in this series.
