Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement

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• 作者：Neil Moss ; ^{Neil.Moss@comcast.com} ; Zhaoming Xiong ; ^{zhaoming.xiong@boehringer-ingelheim.com} ; Mike Burke ; Derek Cogan ; Donghong A. Gao ; Kathleen Haverty ; Alexander Heim-Riether ; Eugene R. Hickey ; Raj Nagaraja ; Matthew Netherton ; Kathy O’ ; Shea ; Philip Ramsden ; Racheline Schwartz ; Daw-Tsun Shih ; Yancey Ward ; Erick Young ; Qing Zhang
• 关键词：Cathepsin S ; Reversible covalent inhibitors ; Triazole ; SAR ; Metabolic stability
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：1 December, 2012
• 年：2012
• 卷：22
• 期：23
• 页码：7189-7193
• 全文大小：1908 K

文摘

This paper details exploration of a class of triazole-based cathepsin S inhibitors originally reported by Ellman and co-workers. SAR studies involving modifications across the whole inhibitor provide a perspective on the strengths and weaknesses of this class of inhibitors. In addition, we put the unique characteristics of this class of compounds into perspective with other classes of cathepsin S inhibitors.