Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)
…, S Lombardi, KE Georgiadis, E Reifenberg…
文献索引：Bursavich, Matthew G.; Gilbert, Adam M.; Lombardi, Sabrina; Georgiadis, Katy E.; Reifenberg, Erica; Flannery, Carl R.; Morris, Elisabeth A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1185 - 1188
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.
