C. Subramanyam et al., INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE .2. SYNTHESIS AND SAR OF BENZISOTHIAZOLINYLMETHYL ARYL ETHERS, Bioorganic & medicinal chemistry letters, 5(4), 1995, pp. 319-324
A series of 4-isopropyl benzisothiazolinylmethyl aryl ethers were prep
ared and evaluated as inhibitors of human leukocyte elastase (HLE). Am
ong the phenols attached as leaving groups onto N-methyl of the 4-isop
ropyl benzisothiazolone nucleus, the sulfonamido phenol 26 was found t
o be the best. Compound 7i with K-i() = 0.8 nM was the most potent in
hibitor in this series.