Basic Information
ID: ALA1909576
Journal: Bioorg Med Chem Lett
Title: Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.
Authors: Hu Y, Xing L, Thomason JR, Xiang J, Ipek M, Guler S, Li H, Sabatini J, Chockalingam P, Reifenberg E, Sheldon R, Morris EA, Georgiadis KE, Tam S.
Abstract: Design, synthesis and structure-activity relationship of a series of biphenylsulfonamido-3-methylbutanoic acid based aggrecanase-1 inhibitors are described. In addition to robust aggrecanase-1 inhibition, these compounds also exhibit potent MMP-13 activity. In cell-based cartilage explants assay compound 48 produced 87% inhibition of proteoglycan degradation at 10 μg/mL. Good pharmacokinetic properties were demonstrated by 46 with a half-life of 6h and bioavailability of 23%.
CiteXplore: 21982494
DOI: 10.1016/j.bmcl.2011.09.036
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets