Title of article :
5-((1H-Pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
Author/Authors :
Adam M. Gilbert، نويسنده , , Matthew G. Bursavich، 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 :
A series of 5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5 (aggrecanase-2) is described. These compounds show μM functional inhibition of ADAMTS-5, and represent a new class of agents with the potential of inhibiting degradation of aggrecan, a major component of cartilage which is lost in osteoporosis. Compound 12 is noteworthy in that it has an ADAMTS-5 IC50: 1.1 μM and shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).
Keywords :
Thioxothiazolidin-4-ones , Aggrecanase-2 , ADAMTS-5 , osteoporosis
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
