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Identification of Novel Indanylsulfonamide Guanylhydrazones as Potent 5-HT6 Serotonin Receptor Antagonists

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journal contribution
posted on 08.10.2009, 00:00 by Neus Mesquida, Sara López-Pérez, Immaculada Dinarès, Jordi Frigola, Ramon Mercè, Jörg Holenz, Raquel Pérez, Javier Burgueño, Ermitas Alcalde
Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid guanylhydrazone moiety at the indene 3-position led to the identification of the title indanylguanylhydrazones 6, which exhibited excellent binding affinities and an antagonistic response at the 5-HT6 receptor, with Ki and IC50 values in the nanomolar range (Ki ≥ 1.2 nM, IC50 ≥ 47 nM, and Imax ≤ 173%).