Title of article
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K
Author/Authors
W. Cameron Black، نويسنده , , Christopher I. Bayly، نويسنده , , Dana E. Davis، نويسنده , , Sylvie Desmarais، نويسنده , , Jean-Pierre Falgueyret، نويسنده , , Serge Léger، نويسنده , , Chun-Sing Li، نويسنده , , Frédéric Massé، نويسنده , , Daniel J. McKay، نويسنده , , James T. Palmer، نويسنده , , M. David Percival، نويسنده , , Joël Robichaud، نويسنده , , Nancy Tsou، نويسنده , , Robert Zamboni، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
4741
To page
4744
Abstract
The P2-P3 amide of dipeptide cathepsin K inhibitors can be replaced by the metabolically stable trifluoroethylamine group. The non-basic nature of the nitrogen allows the important hydrogen bond to Gly66 to be made. The resulting compounds are 10- to 20-fold more potent than the corresponding amide derivatives. Compound 8 is a 5 pM inhibitor of human cathepsin K with >10,000-fold selectivity over other cathepsins.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796067
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