| 19329309 |
Hopper DW, Vera MD, How D, Sabatini J, Xiang JS, Ipek M, Thomason J, Hu Y, Feyfant E, Wang Q, Georgiadis KE, Reifenberg E, Sheldon RT, Keohan CC, Majumdar MK, Morris EA, Skotnicki J, Sum PE: Synthesis and biological evaluation of ((4-keto)-phenoxy) methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors. Bioorg Med Chem Lett. 2009 May 1;19(9):2487-91. Epub 2009 Mar 18.
The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation in osteoarthritis. The evaluation of a series of biphenylsulfonamides resulted in the identification of the ((4-keto)-phenoxy) methyl biphenyl-4-sulfonamides analogs (19-21 and 24) with improved Agg-1 inhibition and MMP-2, MMP-13 activity. |
81(1,1,1,1) |