Bioorganic & Medicinal Chemistry Letters 2006-01-15

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

Wayne D Vaccaro, Rosy Sher, Michael Berlin, Neng-Yang Shih, Robert Aslanian, John H Schwerdt, Kevin D McCormick, John J Piwinski, Robert E West, John C Anthes, Shirley M Williams, Ren-Long Wu, H Susan She, Maria A Rivelli, Jennifer C Mutter, Michel R Corboz, John A Hey, Leonard Favreau

Index: Bioorg. Med. Chem. Lett. 16 , 395, (2006)

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Abstract

We report the discovery of novel histamine H(3) 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.