ONYL)OXY]-6-SUBSTITUTED-1H-ISOINDOLE-1,3(2H)-DIONE MECHANISM-BASED INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE

Authors
KERRIGAN JE SHIRLEY JJ
Citation
Je. Kerrigan et Jj. Shirley, ONYL)OXY]-6-SUBSTITUTED-1H-ISOINDOLE-1,3(2H)-DIONE MECHANISM-BASED INHIBITORS OF HUMAN-LEUKOCYTE ELASTASE, Bioorganic & medicinal chemistry letters, 6(4), 1996, pp. 451-456
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
4
Year of publication
1996
Pages
451 - 456
Database
ISI
SICI code
0960-894X(1996)6:4<451:OMI>2.0.ZU;2-S
Abstract
Derivatives of 2-[(alkylsulfonyl)oxy]-1H-isoindole-1,3(2H)-diones (N-( sulfonyloxy)phthalimides) with ring substituents in the 6-position wer e found to exhibit enhanced inhibitory potency and selectivity for HLE . The most potent inhibitor of HLE in this series was 2-[(methylsulfon yl)oxy]-1H-isoindole-1,3(2H)-dione 10 with a k(obs)/[I] of 110,000 M(- 1) s(-1).