2. Academic Validation
  3. Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists

Identification of novel indanylsulfonamide guanylhydrazones as potent 5-HT6 serotonin receptor antagonists

  • J Med Chem. 2009 Oct 8;52(19):6153-7. doi: 10.1021/jm900796p.
Neus Mesquida 1,  Sara López-Pérez,  Immaculada Dinarès,  Jordi Frigola,  Ramon Mercè,  Jörg Holenz,  Raquel Pérez,  Javier Burgueño,  Ermitas Alcalde
Affiliations

Affiliation

  • 1 Departament de Farmacologia i Química Terapeutica, Facultat de Farmàcia, Universitat de Barcelona, Barcelona, Spain. neusmesquida@ub.edu
PMID: 19739674 DOI: 10.1021/jm900796p
Abstract

Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT(6) 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-HT(6) receptor, with K(i) and IC(50) values in the nanomolar range (K(i) >or= 1.2 nM, IC(50) >or= 47 nM, and I(max) <or= 173%).

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