名称:
                                Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors
                             
                            
                                摘要:
                                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 IC50 < 0.1 mu M with excellent selectivity over MMP-1 and TACE. (C) 2009 Elsevier Ltd. All rights reserved.
                             
                                                            
                                    DOI:
                                    10.1016/j.bmcl.2009.02.024