| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377983 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
Abstract
A series of 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5 (aggrecanase-2) is described. These compounds show μM functional inhibition of ADAMTS-5, and represent a new class of agents with the potential of inhibiting degradation of aggrecan, a major component of cartilage which is lost in osteoporosis. Compound 12 is noteworthy in that it has an ADAMTS-5 IC50: 1.1 μM and shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Adam M. Gilbert, Matthew G. Bursavich, Sabrina Lombardi, Katy E. Georgiadis, Erica Reifenberg, Carl R. Flannery, Elisabeth A. Morris,