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Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: A class of potent aggrecanase-1 inhibitors |
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| Authors: | Darrin W. Hopper Matthew D. Vera David How Joshua Sabatini Jason S. Xiang Manus Ipek Jennifer Thomason Yonghan Hu Eric Feyfant Qin Wang Katy E. Georgiadis Erica Reifenberg Richard T. Sheldon Cristin C. Keohan Manas K. Majumdar Elisabeth A. Morris Jerauld Skotnicki Phaik-Eng Sum |
| Affiliation: | 1. Department of Chemical and Screening Sciences, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, USA;2. Department of Chemical and Screening Sciences, Wyeth Research, 200 CambridgePark Road, Cambridge, MA 02140, USA;3. Department of Women’s Health and Musculoskeletal Biology, Wyeth Research, 200 CambridgePark Road, Cambridge, MA 02140, USA |
| Abstract: | 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. |
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