1.
Am J Public Health
; 89(9): 1442, 1999 Sep.
Article
in English
| MEDLINE
| ID: mdl-10474571
2.
J Med Chem
; 38(9): 1571-4, 1995 Apr 28.
Article
in English
| MEDLINE
| ID: mdl-7739015
ABSTRACT
A novel class of alkyl and aryl phosphonate and phosphinate acid-based leaving groups has been developed for utilization in the synthesis of benzoisothiazolone (BIT) inhibitors of human leukocyte elastase (HLE). A number of BITs were synthesized with phosphonate and phosphinate acid-based leaving groups and were found to be potent inhibitors of HLE. Compound 3c with a diethyl phosphonate leaving group is the most potent inhibitor synthesized in this series with Ki* = 0.035 nM and ED50 = 2.0 mg/kg.