Publications [#330222] of Michael J. Therien

Papers Published

1. Isabel, E; Mellon, C; Boyd, MJ; Chauret, N; Deschênes, D; Desmarais, S; Falgueyret, J-P; Gauthier, JY; Khougaz, K; Lau, CK; Léger, S; Levorse, DA; Li, CS; Massé, F; Percival, MD; Roy, B; Scheigetz, J; Thérien, M; Truong, VL; Wesolowski, G; Young, RN; Zamboni, R; Black, WC, Difluoroethylamines as an amide isostere in inhibitors of cathepsin K., Bioorganic & medicinal chemistry letters, vol. 21 no. 3 (February, 2011), pp. 920-923 [doi]
   (last updated on 2026/01/15)

   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.