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ID: ALA1144597

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).

Authors: Bursavich MG, Gilbert AM, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.

Abstract: 5-Benzylidene-2-thioxo-thiazolidin-4-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. The identified compounds show micromolar ADAMTS-5 potency and demonstrate SAR trends for both the aryl group and thioxothiazolidinone zinc chelator. This series of compounds represents steps toward a metalloprotease inhibitor as a disease-modifying osteoarthritis drug.

CiteXplore: 17210251

DOI: 10.1016/j.bmcl.2006.12.027