| Literature DB >> 17210252 |
Adam M Gilbert1, Matthew G Bursavich, Sabrina Lombardi, Katy E Georgiadis, Erica Reifenberg, Carl R Flannery, Elisabeth A Morris.
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 microM 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 microM and shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).Entities:
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Year: 2006 PMID： 17210252 DOI： 10.1016/j.bmcl.2006.12.020
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823