Indole amide derivatives: synthesis, structure–activity relationships and molecular modelling studies of a new series of histamine H 1-receptor antagonists

S Battaglia, E Boldrini, F Da Settimo, G Dondio…

文献索引：Battaglia, Sandra; Boldrini, Enrico; Da Settimo, Federico; Dondio, Giulio; La Motta, Concettina; Marini, Anna Maria; Primofiore, Giampaolo European Journal of Medicinal Chemistry, 1999 , vol. 34, # 2 p. 93 - 105

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被引用次数: 27

摘要

A number of indole amide derivatives bearing a basic side chain, in which the indole ring replaces the isoster benzimidazole nucleus typical of some well-known antihistamines, were prepared and tested for their H1-antihistaminic activity. The 1-benzyl-3-indolecarboxamides 32–42 showed antihistaminic (H1) activity (pA2 6–8); the 3-indolylglyoxylylamides 7–16 and the 2-indolecarboxamides 48–56 showed little or no activity. Insertion of the basic side ...