Ring-substituted histaprodifen analogues as partial agonists for histamine H 1 receptors: synthesis and structure–activity relationships

S Elz, K Kramer, C Leschke, W Schunack

文献索引：Elz, Sigurd; Kramer, Kai; Leschke, Christian; Schunack, Walter European Journal of Medicinal Chemistry, 2000 , vol. 35, # 1 p. 41 - 52

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被引用次数: 24

摘要

Thirteen racemic benzene ring-substituted analogues of histaprodifen (8a; 2-[2-(3, 3- diphenylpropyl)-1H-imidazol-4-yl] ethanamine), a novel lead for potent and selective histamine H1-receptor agonists, have been prepared from substituted 4, 4- diphenylbutyronitriles 5 via cyclization of the corresponding methyl butyrimidates 6 with 2- oxo-4-phthalimido-1-butyl acetate in liquid ammonia, followed by deprotection. Nitriles 5 ...