INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE .2. SYNTHESIS AND SAR OF BENZISOTHIAZOLINYLMETHYL ARYL ETHERS

Authors
SUBRAMANYAM C BELL MR FERGUSON E GORDON RG DUNLAP RP FRANKE C MURA AJ
Citation
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
Citations number
14
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
4
Year of publication
1995
Pages
319 - 324
Database
ISI
SICI code
0960-894X(1995)5:4<319:IOHE.S>2.0.ZU;2-9
Abstract
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.