| Literature DB >> 16413777 |
Chun Sing Li1, Denis Deschenes, Sylvie Desmarais, Jean-Pierre Falgueyret, Jacques Yves Gauthier, Donald B Kimmel, Serge Léger, Frédéric Massé, Mary E McGrath, Daniel J McKay, M David Percival, Denis Riendeau, Sevgi B Rodan, Michel Thérien, Vouy-Linh Truong, Gregg Wesolowski, Robert Zamboni, W Cameron Black.
Abstract
Based on our previous study with trifluoroethylamine as a P2-P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound showed excellent pharmacokinetics and efficacy in an ovariectomized (OVX) rhesus monkey model. The volumes of distribution close to unity were consistent with this compound not being lysosomotropic, which is a characteristic of basic cathepsin K inhibitors.Entities:
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Year: 2006 PMID： 16413777 DOI： 10.1016/j.bmcl.2005.12.071
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823