Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377315 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors.
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Authors
Jacques Yves Gauthier, Nathalie Chauret, Wanda Cromlish, Sylvie Desmarais, Le T. Duong, Jean-Pierre Falgueyret, Donald B. Kimmel, Sonia Lamontagne, Serge Léger, Tammy LeRiche, Chun Sing Li, Frédéric Massé, Daniel J. McKay, Deborah A. Nicoll-Griffith,