POTENT CARBOXYLATE INHIBITORS OF STROMELYSIN CONTAINING P2' PIPERAZICACIDS AND P1' BIARYL MOEITIES

Authors
CHERNEY RJ DECICCO CP NELSON DJ WANG L MEYER DT HARDMAN KD COPELAND RA ARNER EC
Citation
Rj. Cherney et al., POTENT CARBOXYLATE INHIBITORS OF STROMELYSIN CONTAINING P2' PIPERAZICACIDS AND P1' BIARYL MOEITIES, Bioorganic & medicinal chemistry letters, 7(13), 1997, pp. 1757-1762
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
13
Year of publication
1997
Pages
1757 - 1762
Database
ISI
SICI code
0960-894X(1997)7:13<1757:PCIOSC>2.0.ZU;2-Y
Abstract
Several carboxylate derivatives with variation at the P1' residue were synthesized and evaluated as stromelysin (MMP-3) inhibitors. Compound s containing a biphenyl moiety at P1' were found to be potent inhibito rs of MMP-3. An X-ray crystal structure of the most potent compound, c arboxylate 19, revealed an important interaction between the inhibitor 's biphenyl and histidine 224 in the S1' pocket of MMP-3. (C) 1997 Els evier Science Ltd.