Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors

Pyrazole-based thioether amide inhibitors of cathepsin S: SAR investigations. A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide functional groups were prepared with the goal of improving upon the cellular activity of amidoethylthioethers. This Letter descri...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2379-2382
Main Authors: Wiener, Danielle K., Lee-Dutra, Alice, Bembenek, Scott, Nguyen, Steven, Thurmond, Robin L., Sun, Siquan, Karlsson, Lars, Grice, Cheryl A., Jones, Todd K., Edwards, James P.
Format: Article
Language:English
Subjects:
Acetamides - chemistry
Acetamides - pharmacology
Biological and medical sciences
Cathepsins - antagonists & inhibitors
Cathepsins - chemistry
Cathepsins - metabolism
Cell Line
Humans
Immunomodulators
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
Pyrazoles - chemistry
Pyrazoles - pharmacology
Structure-Activity Relationship
Sulfides - chemistry
Sulfides - pharmacology
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Summary:Pyrazole-based thioether amide inhibitors of cathepsin S: SAR investigations. A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide functional groups were prepared with the goal of improving upon the cellular activity of amidoethylthioethers. This Letter describes altered amide connectivity, in conjunction with changes to other binding elements, resulting in improved potency, as well as increased knowledge of the relationship between this chemotype and human CatS activity.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.103