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 2

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

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 2

Bioorg Med Chem Lett. 2002 Jan 21;12(2):249-53.

Authors

J Ignacio Andrés¹, Jesús Alcázar, José M Alonso, Adolfo Díaz, Javier Fernández, Pilar Gil, Laura Iturrino, Encarna Matesanz, Theo F Meert, Anton Megens, Victor K Sipido

Affiliation

¹ Janssen-Cilag, Basic Research Centre, Jarama s/n, 45007 Toledo, Spain. jandres@jaces.jnj.com

PMID: 11755365

Abstract

Following the programme started at Janssen Research Foundation searching for 5-HT(2A/2C) antagonists, we now report on the synthesis of a series of substituted 2-(Dimethylaminomethyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives. The 5-HT(2A), 5-HT(2C) and H(1) receptor affinities as well as the mCPP antagonistic activity of the compounds synthesised is described.

MeSH terms

Azepines / chemical synthesis*
Azepines / chemistry
Azepines / pharmacology*
Receptor, Serotonin, 5-HT2A
Receptor, Serotonin, 5-HT2C
Receptors, Serotonin / drug effects*
Serotonin Antagonists / chemical synthesis*
Serotonin Antagonists / chemistry
Serotonin Antagonists / pharmacology*
Structure-Activity Relationship

Substances

Azepines
Receptor, Serotonin, 5-HT2A
Receptor, Serotonin, 5-HT2C
Receptors, Serotonin
Serotonin Antagonists