Bioorganic & Medicinal Chemistry Letters 2002-01-21

Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.

J Ignacio Andrés, Jesús Alcázar, José M Alonso, Adolfo Díaz, Javier Fernández, Pilar Gil, Laura Iturrino, Encarna Matesanz, Theo F Meert, Anton Megens, Victor K Sipido

文献索引：Bioorg. Med. Chem. Lett. 12(2) , 243-48, (2002)

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摘要

The synthesis of a series of novel 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives as well as their 5-HT(2A/2C) and H(1) receptor binding affinities are described. The in vivo activity as potential anxiolytics of the synthesised compounds was measured in a mCPP challenge test. One of the compounds, 2a, proved to be a potent 5-HT(2A/2C) receptor antagonist showing as well oral activity and therefore could be considered as a potential anxiolytic/antidepressant agent.