Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374954 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group found in our screening hit. Continued investigation into replacements for the 4-aryl piperazine resulted in the identification of potentially useful CatS inhibitors with enzymatic and cellular activity similar to that of JNJ 10329670 as disclosed in a previous publication.
Graphical abstractNoncovalent, potent, and selective inhibitors of the cysteine protease cathepsin S are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Cheryl A. Grice, Kevin Tays, Haripada Khatuya, Darin J. Gustin, Christopher R. Butler, Jianmei Wei, Clark A. Sehon, Siquan Sun, Yin Gu, Wen Jiang, Robin L. Thurmond, Lars Karlsson, James P. Edwards,