Novel histamine H₃ receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold

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• 作者：Wayne D. Vaccaro ; Rosy Sher ; Michael Berlin ; Neng-Yang Shih ; Robert Aslanian ; John H. Schwerdt ; Kevin D. McCormick ; John J. Piwinski ; Robert E. West ; Jr. et al.
• 关键词：Histamine ; H₃ antagonists ; Imidazole series ; 4-[ ; (1H-Imidazol-4-yl)methyl] ; piperidine ; Norepinephrine ; Allergic rhinitis ; Decongestion
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 January 2006
• 卷：16
• 期：2
• 页码：395-399
• 文件大小：161 K

摘要

We report the discovery of novel histamine H₃ receptor antagonists based on 4-[(1H-imidazol-4-yl)methyl]piperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.