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Published on: August 20, 2016
Identification of potent and selective MMP-13 inhibitors
Junjun Wu1, Thomas S Rush, Rajeev Hotchandani
1Department of Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA.
Bioorganic & Medicinal Chemistry Letters
|July 12, 2005
Abstract:
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.
