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Bioorg Med Chem Lett. 2011 Nov 15;21(22):6800-3. doi: 10.1016/j.bmcl.2011.09.036. Epub 2011 Sep 18.

Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.

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  • 1Worldwide Medicinal Chemistry, Pfizer Global Research and Development, 200 CambridgePark Drive, Cambridge, MA 02140, USA.


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%.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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