N α-Imidazolylalkyl and pyridylalkyl derivatives of histaprodifen: synthesis and in vitro evaluation of highly potent histamine H1-receptor agonists

S Menghin, HH Pertz, K Kramer, R Seifert…

文献索引：Menghin, Sonja; Pertz, Heinz H.; Kramer, Kai; Seifert, Roland; Schunack, Walter; Elz, Sigurd Journal of Medicinal Chemistry, 2003 , vol. 46, # 25 p. 5458 - 5470

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被引用次数: 27

摘要

A novel series of N α-imidazolylalkyl and pyridylalkyl derivatives of histaprodifen (6, 2-[2-(3, 3-diphenylpropyl) imidazol-4-yl] ethanamine) was synthesized and evaluated as histamine H1-receptor agonists. The title compounds displayed partial agonism at contractile H1- receptors of guinea pig ileum and were at least equipotent with histamine. Agonist effects of the new derivatives were susceptible to blockade by the H1-receptor antagonist ...