Cyclopropyl‐tryptamine Analogues: Synthesis and Biological Evaluation as 5‐HT6 Receptor Ligands. Issue 1 (5th November 2012)

• Record Type: Journal Article
• Authors: Szalata, Claude; Szymoniak, Jan; Fabis, Frédéric; Butt‐Gueulle, Sabrina; Rault, Sylvain; Bertus, Philippe; Gérard, Stéphane; Sapi, Janos
• Is Part Of: ChemMedChem. Volume 8:Issue 1(2013:Jan.)
• Page Start: 70
• Page End: 73
• Publication Date: 2012-11-05
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201200396
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>Conformational restrictions:</bold> 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. <italic>N</italic>, <italic>N</italic>‐Dimethyl‐1‐arylsulfonyltryptamine derivatives exhibited promising selectivity for 5‐HT₆ over 5‐HT_1a and 5‐HT₄ receptors and interesting activity against 5‐HT₆ (<italic>K</italic>_i=∼0.15 μ<sc>M</sc>; IC₅₀=∼0.20 μ<sc>M</sc>).<boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgg1p89bf2x" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>