Cyclopropyl-tryptamine Analogues: Synthesis and Biological Evaluation as 5-HT6 Receptor Ligands

Conformational restrictions: Based on the pharmacophore model for 5‐HT6 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 ex...

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Bibliographic Details
Published in:ChemMedChem 2013-01, Vol.8 (1), p.70-73
Main Authors: Szalata, Claude, Szymoniak, Jan, Fabis, Frédéric, Butt-Gueulle, Sabrina, Rault, Sylvain, Bertus, Philippe, Gérard, Stéphane, Sapi, Janos
Format: Article
Language:English
Subjects:
Chemical Sciences
conformational restriction
inhibitors
Medicinal Chemistry
serotonin receptors
structure-activity relationships
tryptamines
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Summary:Conformational restrictions: Based on the pharmacophore model for 5‐HT6 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‐HT6 over 5‐HT1a and 5‐HT4 receptors and interesting activity against 5‐HT6 (Ki=∼0.15 μM; IC50=∼0.20 μM).
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201200396