1.
Bioorg Med Chem Lett
; 15(18): 4105-9, 2005 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16005220
RESUMO
A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 microM) inhibitor that did not bear a zinc chelator. Structure-based drug design strategies were employed to append a Zn-chelating group to one end of the molecule and functionality to enhance selectivity to the other. A compound from this series demonstrated rat oral bioavailability and efficacy in a bovine articular cartilage explant model.