| Literature DB >> 20061146 |
Elise Isabel1, Kevin P Bateman, Nathalie Chauret, Wanda Cromlish, Sylvie Desmarais, Le T Duong, Jean-Pierre Falgueyret, Jacques Yves Gauthier, Sonia Lamontagne, Cheuk K Lau, Serge Léger, Tammy LeRiche, Jean-François Lévesque, Chun Sing Li, Frédéric Massé, Daniel J McKay, Christophe Mellon, Deborah A Nicoll-Griffith, Renata M Oballa, M David Percival, Denis Riendeau, Joël Robichaud, Gideon A Rodan, Sevgi B Rodan, Carmai Seto, Michel Thérien, Vouy Linh Truong, Gregg Wesolowski, Robert N Young, Robert Zamboni, W Cameron Black.
Abstract
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo studies using deuterated MK-0674 show stereoselective epimerization of the alcohol stereocenter via an oxidation/reduction cycle. From in vitro incubations, two metabolites could be identified: the hydroxyleucine and the glucuronide conjugate which were confirmed using authentic synthetic standards. Copyright (c) 2009. Published by Elsevier Ltd.Entities:
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Year: 2009 PMID： 20061146 DOI： 10.1016/j.bmcl.2009.12.083
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823