Exploration of the P1 SAR of aldehyde cathepsin K inhibitors

The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-01, Vol.14 (1), p.275-278
Main Authors: CATALANO, John G, DEATON, David N, FURFINE, Eric S, HASSELL, Annie M, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R, SHEWCHUK, Lisa M, WILLARD, Derril H, WRIGHT, Lois L
Format: Article
Language:English
Subjects:
Aldehydes - chemistry
Aldehydes - pharmacology
Binding Sites - drug effects
Binding Sites - physiology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cathepsin K
Cathepsins - antagonists & inhibitors
Cathepsins - metabolism
Medical sciences
Pharmacology. Drug treatments
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
Structure-Activity Relationship
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Summary:The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.09.088