Bioorganic and Medicinal Chemistry Letters p. 923 - 928 (2008)
Update date:2022-08-03
Topics:
Gauthier, Jacques Yves
Chauret, Nathalie
Cromlish, Wanda
Desmarais, Sylvie
Duong, Le T.
Falgueyret, Jean-Pierre
Kimmel, Donald B.
Lamontagne, Sonia
Leger, Serge
LeRiche, Tammy
Li, Chun Sing
Masse, Frederic
McKay, Daniel J.
Nicoll-Griffith, Deborah A.
Oballa, Renata M.
Palmer, James T.
Percival, M. David
Riendeau, Denis
Robichaud, Joel
Rodan, Gideon A.
Rodan, Sevgi B.
Seto, Carmai
Therien, Michel
Truong, Vouy-Linh
Venuti, Michael C.
Wesolowski, Gregg
Young, Robert N.
Zamboni, Robert
Black, W. Cameron
Odanacatib is a potent, selective, and neutral cathepsin K inhibitor which was developed to address the metabolic liabilities of the Cat K inhibitor L-873724. Substituting P1 and modifying the P2 side chain led to a metabolically robust inhibitor with a long half-life in preclinical species. Odanacatib was more selective in whole cell assays than the published Cat K inhibitors balicatib and relacatib. Evaluation in dermal fibroblast culture showed minimal intracellular collagen accumulation relative to less selective Cat K inhibitors.
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