A structural screening approach to ketoamide-based inhibitors of cathepsin K.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA.

Published: May 2005

Several novel ketoamide-based inhibitors of cathepsin K have been identified. Starting from a modestly potent inhibitor, structural screening of P2 elements led to 100-fold enhancements in inhibitory activity. Modifications to one of these leads resulted in an orally bioavailable cathepsin K inhibitor.

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http://dx.doi.org/10.1016/j.bmcl.2005.03.023DOI Listing

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