Cyclopropyl-tryptamine analogues: synthesis and biological evaluation as 5-HT(6) receptor ligands.

Claude Szalata, Jan Szymoniak, Frédéric Fabis, Sabrina Butt-Gueulle, Sylvain Rault, Philippe Bertus, Stéphane Gérard, Janos Sapi

Institut de Chimie Moléculaire de Reims, UMR CNRS 7312 (ex 6229), Faculté de Pharmacie, Université de Reims-Champagne-Ardenne, 51096 Reims Cedex and UFR Sciences, 51687, Reims Cedex 2, France.

ChemMedChem 2013 Jan

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Conformational restrictions: Based on the pharmacophore model for 5-HT(6) receptor ligands (shown), tryptamine analogues bearing a cyclopropyl ring on the α-position of the tryptamine side chain were synthesized and evaluated against 5-HT receptors. N,N-Dimethyl-1-arylsulfonyltryptamine derivatives exhibited promising selectivity for 5-HT(6) over 5-HT(1a) and 5-HT(4) receptors and interesting activity against 5-HT(6) (K(i) =∼0.15 μM; IC(50) =∼0.20 μM). Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Citation

Claude Szalata, Jan Szymoniak, Frédéric Fabis, Sabrina Butt-Gueulle, Sylvain Rault, Philippe Bertus, Stéphane Gérard, Janos Sapi. Cyclopropyl-tryptamine analogues: synthesis and biological evaluation as 5-HT(6) receptor ligands. ChemMedChem. 2013 Jan;8(1):70-3