Identification of a potent and selective non-basic cathepsin K inhibitor.
Publication
, Journal Article
Li, CS; Deschenes, D; Desmarais, S; Falgueyret, J-P; Gauthier, JY; Kimmel, DB; Léger, S; Massé, F; McGrath, ME; McKay, DJ; Percival, MD ...
Published in: Bioorganic & medicinal chemistry letters
April 2006
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.
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Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
April 2006
Volume
16
Issue
7
Start / End Page
1985 / 1989
Related Subject Headings
- Ovariectomy
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Macaca mulatta
- Female
- Cysteine Proteinase Inhibitors
- Crystallography, X-Ray
- Cathepsins
- Cathepsin K
- Animals
Citation
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Li, C. S., Deschenes, D., Desmarais, S., Falgueyret, J.-P., Gauthier, J. Y., Kimmel, D. B., … Black, W. C. (2006). Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorganic & Medicinal Chemistry Letters, 16(7), 1985–1989. https://doi.org/10.1016/j.bmcl.2005.12.071
Li, Chun Sing, Denis Deschenes, Sylvie Desmarais, Jean-Pierre Falgueyret, Jacques Yves Gauthier, Donald B. Kimmel, Serge Léger, et al. “Identification of a potent and selective non-basic cathepsin K inhibitor.” Bioorganic & Medicinal Chemistry Letters 16, no. 7 (April 2006): 1985–89. https://doi.org/10.1016/j.bmcl.2005.12.071.
Li CS, Deschenes D, Desmarais S, Falgueyret J-P, Gauthier JY, Kimmel DB, et al. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorganic & medicinal chemistry letters. 2006 Apr;16(7):1985–9.
Li, Chun Sing, et al. “Identification of a potent and selective non-basic cathepsin K inhibitor.” Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 7, Apr. 2006, pp. 1985–89. Epmc, doi:10.1016/j.bmcl.2005.12.071.
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. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorganic & medicinal chemistry letters. 2006 Apr;16(7):1985–1989.
Published In
Bioorganic & medicinal chemistry letters
DOI
EISSN
1464-3405
ISSN
0960-894X
Publication Date
April 2006
Volume
16
Issue
7
Start / End Page
1985 / 1989
Related Subject Headings
- Ovariectomy
- Models, Molecular
- Medicinal & Biomolecular Chemistry
- Macaca mulatta
- Female
- Cysteine Proteinase Inhibitors
- Crystallography, X-Ray
- Cathepsins
- Cathepsin K
- Animals