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.
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