Identification of a potent and selective non-basic cathepsin K inhibitor.
Published
Journal Article
Based on our previous study with trifluoroethylamine as a P2-P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound showed excellent pharmacokinetics and efficacy in an ovariectomized (OVX) rhesus monkey model. The volumes of distribution close to unity were consistent with this compound not being lysosomotropic, which is a characteristic of basic cathepsin K inhibitors.
Full Text
Duke Authors
Cited Authors
- Li, CS; Deschenes, D; Desmarais, S; Falgueyret, J-P; Gauthier, JY; Kimmel, DB; Léger, S; Massé, F; McGrath, ME; McKay, DJ; Percival, MD; Riendeau, D; Rodan, SB; Thérien, M; Truong, V-L; Wesolowski, G; Zamboni, R; Black, WC
Published Date
- April 2006
Published In
Volume / Issue
- 16 / 7
Start / End Page
- 1985 - 1989
PubMed ID
- 16413777
Pubmed Central ID
- 16413777
Electronic International Standard Serial Number (EISSN)
- 1464-3405
International Standard Serial Number (ISSN)
- 0960-894X
Digital Object Identifier (DOI)
- 10.1016/j.bmcl.2005.12.071
Language
- eng