Primary amides as selective inhibitors of cathepsin K

…, S Desmarais, JP Falgueyret, F Massé…

Index: Leger, Serge; Bayly, Christopher I.; Black, W. Cameron; Desmarais, Sylvie; Falgueyret, Jean-Pierre; Masse, Frederic; Percival, M. David; Truchon, Jean-Francois Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4328 - 4332

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Citation Number: 16

Abstract

The nitrile warhead used in a series of cathepsin K inhibitors can be replaced by a less electrophilic primary amide. The accompanying loss of potency can be partially recovered by introducing a substituent α to the amide. The potency gain resulting from this addition is ...

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