Alkoxy-Substituted Benzisothiazolone (Bit) Derivatives - Potent Inhibitors Of Human-Leukocyte Elastase

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.