INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE .3. INHIBITION BY TETRAHYDROBENZISOTHIAZOLINYLMETHYL ARYL CARBOXYLATES

Authors
SUBRAMANYAM C BELL MR GHOSE AK KUMAR V DUNLAP RP FRANKE C MURA AJ
Citation
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
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
325 - 330
Database
ISI
SICI code
0960-894X(1995)5:4<325:IOHE.I>2.0.ZU;2-3
Abstract
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.