Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Basic Information
ID: ALA1147767
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Authors: Xiang JS, Hu Y, Rush TS, Thomason JR, Ipek M, Sum PE, Abrous L, Sabatini JJ, Georgiadis K, Reifenberg E, Majumdar M, Morris EA, Tam S.
Abstract: Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of biphenylsulfonamidocarboxylic acid inhibitors of aggrecanase-1 are reported. Compound 24 demonstrated 89% inhibition of proteoglycan degradation at 10 microg/mL and has an oral bioavailability in rat of 35%.
CiteXplore: 16275085
DOI: 10.1016/j.bmcl.2005.10.001
Patent ID: ┄