Title of article :
Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)
Author/Authors :
Matthew G. Bursavich، نويسنده , , Adam M. Gilbert، نويسنده , , Sabrina Lombardi، نويسنده , , Katy E. Georgiadis، نويسنده , , Erica Reifenberg، نويسنده , , Carl R. Flannery، نويسنده , , Elisabeth A. Morris، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2007
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.
Keywords :
Aggrecanase , Thioxothiazolidinone , Metalloprotease inhibitor , ADAMTS-5 , Zinc chelator
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
