N-Arylsulfonyl-2-vinyltryptamines as new 5-HT₆ serotonin receptor Ligands

Marion Raoul Université de Reims-Champagne-Ardenne, FRE CNRS 2715 “Isolement, Structure, Transformations et Synthèse de Substances Naturelles”, IFR 53 “Biomolécules”, Faculté de Pharmacie, 51 rue Cognacq-Jay, Reims Cedex, F-51096, France

Dominique Patigny Université de Reims-Champagne-Ardenne, FRE CNRS 2715 “Isolement, Structure, Transformations et Synthèse de Substances Naturelles”, IFR 53 “Biomolécules”, Faculté de Pharmacie, 51 rue Cognacq-Jay, Reims Cedex, F-51096, France

Frédréic Fabis UFR des Sciences Pharmaceutiques, Centre d'Etudes et de Recherche sur le Médicament de Normandie, 5 rue Vaubénard, Caen Cedex, 14032, France

FranÇis Dauphin UFR des Sciences Pharmaceutiques, Centre d'Etudes et de Recherche sur le Médicament de Normandie, 5 rue Vaubénard, Caen Cedex, 14032, France

Sylvain Rault UFR des Sciences Pharmaceutiques, Centre d'Etudes et de Recherche sur le Médicament de Normandie, 5 rue Vaubénard, Caen Cedex, 14032, France

Janos Sapi Université de Reims-Champagne-Ardenne, FRE CNRS 2715 “Isolement, Structure, Transformations et Synthèse de Substances Naturelles”, IFR 53 “Biomolécules”, Faculté de Pharmacie, 51 rue Cognacq-Jay, Reims Cedex, F-51096, France

Jean-Yves Laronze Université de Reims-Champagne-Ardenne, FRE CNRS 2715 “Isolement, Structure, Transformations et Synthèse de Substances Naturelles”, IFR 53 “Biomolécules”, Faculté de Pharmacie, 51 rue Cognacq-Jay, Reims Cedex, F-51096, France

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Abstract

Several new 2-vinyl-N_b,N_b-dimethyltryptamines were prepared using Fischer indole synthesis followed by simple functional group transformations and evaluated on 5-HT₄, 5-HT₅, 5-HT₆ and 5-HT₇ serotonin receptors. It was found that 2-vinyl substitution conferred a potent and selective 5-HT₆ binding activity to these molecules which could be enhanced by N_a-arylsulfonyl substituents.

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Acknowledgements

Spectroscopic measurements by P. Sigaut (MS) and C. Petermann (NMR) are gratefully acknowledged.

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N-Arylsulfonyl-2-vinyltryptamines as new 5-HT₆ serotonin receptor Ligands

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N-Arylsulfonyl-2-vinyltryptamines as new 5-HT₆ serotonin receptor Ligands