The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors

Citation
Fm. Martin et al., The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors, BIOORG MED, 9(19), 1999, pp. 2887-2892
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
19
Year of publication
1999
Pages
2887 - 2892
Database
ISI
SICI code
0960-894X(19991004)9:19<2887:TSABEO>2.0.ZU;2-2
Abstract
Novel sulfonamide matrix metalloproteinase inhibitors of general formula (9 ) were synthesised by a route involving a stereoselective conjugate additio n reaction. Enzyme selectivity was found to be dependant on the nature of t he sulfonamide substituents. Compounds (9f, 9q) are potent selective collag enase inhibitors with good oral bioavailability. (C) 1999 Elsevier Science Ltd. All rights reserved.