5-Substituted 3,4-dihydro-3-amino-2H-1-benzopyran derivatives: synthesis and interaction with serotoninergic receptors-Reference-Cited by-同舟云学术

5-Substituted 3,4-dihydro-3-amino-2H-1-benzopyran derivatives: synthesis and interaction with serotoninergic receptors

Published:2001-07 Issue:7 Volume:53 Page:959-968
ISSN:0022-3573
Container-title:Journal of Pharmacy and Pharmacology
language:en
Short-container-title:

Author:

Rezaie R¹,Joseph B¹,Bremner J B²,Delagrange P³,Kopp C⁴,Misslin R⁴,Pfeiffer B⁵,Renard P⁵,Guillaumet G¹

Affiliation:

1. Institut de Chimie Organique et Analytique, UMR-CNRS 6005, Université d'Orléans, BP 6759, 45067 Orleans Cedex 2, France

2. Department of Chemistry, University of Wollongong, Northfields Avenue, Wollongong, NSW 2522, Australia

3. IRI Servier, 6, Place des Pléiades, 92415 Courbevoie Cedex, France

4. Laboratoire de Psychophysiologie, associé au CNRS, Université Louis Pasteur, 7 rue de l'Université, 67000 Strasbourg, France

5. ADIR, 1, rue Carle Hebert, 92415 Courbevoie Cedex, France

Abstract

Abstract A new series of 3,4-dihydro-3-amino-2H-1-benzopyran derivatives (1 and 2) bearing various substituents on the 5-position was successfully prepared via palladium-mediated cross-coupling reactions. Some of the new compounds showed high affinity for 5-HT1A and 5-HT7 receptors. The best affinity for the 5-HT1A and 5-HT7 receptors was obtained for 2b (Ki = 0.3 nM for 5-HT1A and 3.1 nM for 5-HT7). The anxiolytic activity of compound 2b was evaluated.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Link

http://academic.oup.com/jpp/article-pdf/53/7/959/36783277/0022357011776388.pdf

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