Chakrapani Subramanyam, Malcolm R. Bell, Edward Ferguson, Robert G. Gordon, Richard P. Dunlap, Catherine Franke, Albert J. Mura

Potent mechanism based inhibition of human leukocyte elastase (HLE) by tetrahydrobenzisothiazolones (2) is described. Structure activity relationships studies led to the identification of WIN 62816 (2c), the most potent inhibitor in this series with a Ki* = 0.7 nM.