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
Pages
4
From page
1185
To page
1188
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
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797814
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