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Difluoroethylamines as an amide isostere in inhibitors of cathepsin K

Authors
Journal
Bioorganic & Medicinal Chemistry Letters
0960-894X
Publisher
Elsevier
Publication Date
Volume
21
Issue
3
Identifiers
DOI: 10.1016/j.bmcl.2010.12.070
Keywords
  • Cathepsin K
  • Cat K
  • Difluoroethylamine
  • Log D
  • Pka

Abstract

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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