C. Subramanyam et al., INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE .3. INHIBITION BY TETRAHYDROBENZISOTHIAZOLINYLMETHYL ARYL CARBOXYLATES, Bioorganic & medicinal chemistry letters, 5(4), 1995, pp. 325-330
Potent mechanism based inhibition of human leukocyte elastase (HLE) by
tetrahydrobenzisothiazolones (2) is described. Structure activity rel
ationships studies led to the identification of WIN 62816 (2c), the mo
st potent inhibitor in this series with a K-i() = 0.7 nM.