Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl) methyl] piperidine series of histamine H 3 receptor antagonists

…, JJ Piwinski, NY Shih, L Duguma, DM Solomon…

文献索引：Berlin, Michael; Ting, Pauline C.; Vaccaro, Wayne D.; Aslanian, Robert; McCormick, Kevin D.; Lee, Joe F.; Albanese, Margaret M.; Mutahi, Mwangi W.; Piwinski, John J.; Shih, Neng-Yang; Duguma, Luli; Solomon, Daniel M.; Zhou, Wei; Sher, Rosy; Favreau, Leonard; Bryant, Matthew; Korfmacher, Walter A.; Nardo, Cymbelene; West Jr., Robert E.; Anthes, John C.; Williams, Shirley M.; Wu, Ren-Long; Susan She; Rivelli, Maria A.; Corboz, Michel R.; Hey, John A. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 4 p. 989 - 994

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被引用次数: 18

摘要

A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl) methyl] piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.