318233-98-6Relevant articles and documents
5-((1H-Pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
Gilbert, Adam M.,Bursavich, Matthew G.,Lombardi, Sabrina,Georgiadis, Katy E.,Reifenberg, Erica,Flannery, Carl R.,Morris, Elisabeth A.
, p. 1189 - 1192 (2007/10/03)
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).