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

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.

Graphical abstractA novel series of potent and selective inhibitors of cysteine protease cathepsin K is described.Figure optionsDownload full-size imageDownload as PowerPoint slide