Title of article
5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one 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
5630
To page
5633
Abstract
5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. Selected compounds 23, 33–35 show sub-micromolar ADAMTS-5 potency and strong SAR trends with selectivity over the related metalloproteases ADAMTS-4 (Aggrecanase-1), MMP12, and MMP13. This series of compounds represents progress toward a selective ADAMTS-5 inhibitor as a disease modifying osteoarthritis drug.
Keywords
ADAMTS-5 , Aggrecanase-2 , Metalloprotease inhibitors , osteoarthritis , Thiadiazoles
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798668
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