Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane Carboxylates As Selective ADAMTS-5 (Aggrecanase-2) Inhibitors

A series of N-substituted sulfonylamino-alkanecarboxylate ADAMTS-5 (Aggrecanase-2) inhibitors has been synthesized and the in vitro enzyme SAR is discussed. This report is the first example of carboxylate-based ADAMTS-5 inhibitors which show strong potency of IC(50)<0.1muM with excellent selectivity over MMP-1 and TACE.