Design and synthesis of thiol containing inhibitors of matrix metalloproteinases

Authors
Fink, CA Carlson, JE Boehm, C McTaggart, P Qiao, Y Doughty, J Ganu, V Melton, R Goldberg, R
Citation
Ca. Fink et al., Design and synthesis of thiol containing inhibitors of matrix metalloproteinases, BIOORG MED, 9(2), 1999, pp. 195-200
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
2
Year of publication
1999
Pages
195 - 200
Database
ISI
SICI code
0960-894X(19990118)9:2<195:DASOTC>2.0.ZU;2-Y
Abstract
A series of thiol containing derivatives was prepared. Several of these com pounds were found to inhibit matrix metalloproteinases 1, 3, and 9 with sel ectivity towards 3 and 9. Compounds 15, 20, and 22 were administered to rat s orally at 75 mu mol/kg. Drug levels of compounds 20 and 22 in the plasma were found to exceed the IC50 values for MMP 3 and 9 four hours after admin istration. (C) 1999 Elsevier Science Ltd. All rights reserved.