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Bioorg Med Chem Lett. 2006 Aug 15;16(16):4296-9. Epub 2006 Jun 5.

Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.

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  • 1Celera Genomics, South San Francisco, CA 94080, USA. eduardo.setti@bcglobal.net


The synthesis and biological profile of a novel series of potent and selective inhibitors of cysteine protease cathepsin K (Cat K) are described. Pharmacokinetic evaluation of 12 indicated that some members of this series could be suitable candidates to develop new orally active therapeutic agents for the treatment of osteoporosis.

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