| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370908 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The trifluoroethylamine group found in cathepsin K inhibitors like odanacatib can be replaced by a difluoroethylamine group. This change increased the basicity of the nitrogen which positively impacted the log D. This translated into an improved oral bioavailability in pre-clinical species. Difluoroethylamine compounds exhibit a similar potency against cathepsin K and selectivity profile against other cathepsins when compared to trifluoroethylamine analogs.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Elise Isabel, Christophe Mellon, Michael J. Boyd, Nathalie Chauret, Denis Deschênes, Sylvie Desmarais, Jean-Pierre Falgueyret, Jacques Yves Gauthier, Karine Khougaz, Cheuk K. Lau, Serge Léger, Dorothy A. Levorse, Chun Sing Li, Frédéric Massé,