| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378131 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 μM) 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.
Graphical abstractA potent, selective series of MMP-13 inhibitors has been derived from a weak inhibitor that did not bear a zinc chelator.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Junjun Wu, Thomas S. Rush III, Rajeev Hotchandani, Xuemei Du, Mary Geck, Elisabeth Collins, Zhang-Bao Xu, Jerry Skotnicki, Jeremy I. Levin, Frank E. Lovering,