Identification of a novel, orally bioavailable histamine H 3 receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template

…, X Zhu, SC Wong, SB Rosenblum, Y Jiang…

文献索引：Aslanian, Robert; Mutahi, Mwangi W.; Shih, Neng-Yang; McCormick, Kevin D.; Piwinski, John J.; Ting, Pauline C.; Albanese, Margaret M.; Berlin, Michael Y.; Zhu, Xiaohong; Wong, Shing-Chun; Rosenblum, Stuart B.; Jiang, Yueheng; West, Robert; She, Susan; Williams, Shirley M.; Bryant, Matthew; Hey, John A. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 6 p. 937 - 941

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被引用次数: 37

摘要

A novel series of histamine H3 receptor antagonists, based on the 4-benzyl-(1H-imidazole-4- yl) template, incorporating urea and carbamate linkers has been prepared. Compound 3j is a selective H3 antagonist and demonstrates excellent oral plasma levels in the rat and monkey.