| Literature DB >> 17804234 |
Matthew G Bursavich1, Adam M Gilbert, Sabrina Lombardi, Katy E Georgiadis, Erica Reifenberg, Carl R Flannery, Elisabeth A Morris.
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.Entities:
Mesh：
Substances：
Year: 2007 PMID： 17804234 DOI： 10.1016/j.bmcl.2007.07.048
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823