Synthesis and serotonergic activity of 5-(oxadiazolyl) tryptamines: potent agonists for 5-HT1D receptors

…, R Baker, JL Castro, MS Chambers…

文献索引：Street, Leslie J.; Baker, Raymond; Castro, Jose L.; Chambers, Mark S.; Guiblin, Alexander R.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 11 p. 1529 - 1538

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被引用次数: 84

摘要

The synthesis and~-HT~ D receptor activity of a novel series of 5-(oxadiazolyl) tryptamines is described. Modifications of the oxadiazole 3-substituent, length of the linking chain (n), and the amine substituents are explored and reveal a large binding pocket in the~-HT~ D receptor domain. Osadiazole Substituents such as benzyl are accommodated without loss of agonist potency or efficacy. The incorporation of polar functionality on a phenyl or benzyl ...