The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors

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• 作者：Cheryl A. Grice ; Kevin Tays ; Haripada Khatuya ; Darin J. Gustin ; Christopher R. Butler ; Jianmei Wei ; Clark A. Sehon ; Siquan Sun ; Yin Gu ; Wen Jiang et al.
• 关键词：Cathepsin S ; Cysteine protease inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：15 April 2006
• 年：2006
• 卷：16
• 期：8
• 页码：2209-2212
• 全文大小：124 K

文摘

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.