Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374595 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
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.
Graphical abstractPyrazole-based thioether amide inhibitors of cathepsin S: SAR investigations.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Danielle K. Wiener, Alice Lee-Dutra, Scott Bembenek, Steven Nguyen, Robin L. Thurmond, Siquan Sun, Lars Karlsson, Cheryl A. Grice, Todd K. Jones, James P. Edwards,