Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT<sub>1A</sub> receptor

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dc.contributor.authorPessoa-Mahana, Hernan
dc.contributor.authorGonzalez-Lira, Christian
dc.contributor.authorFierro, Angelica
dc.contributor.authorZapata-Torres, Gerald
dc.contributor.authorDavid Pessoa-Mahana, C.
dc.contributor.authorOrtiz-Severin, Javiera
dc.contributor.authorIturriaga-Vasquez, Patricio
dc.contributor.authorReyes-Parada, Miguel
dc.contributor.authorSilva-Matus, Paul
dc.contributor.authorSaitz-Barria, Claudio
dc.contributor.authorAraya-Maturana, Ramiro
dc.date.accessioned2025-01-24T00:07:27Z
dc.date.available2025-01-24T00:07:27Z
dc.date.issued2013
dc.description.abstractA series of 3-(3-(4-(3-(1H-indol-3-yl)propyl)piperazin-1-yl)propyl)-1H-indole derivatives (3a-d and 5a-f) as homo-and hetero-bis-ligands, were synthesized and evaluated for in vitro affinity at the serotonin transporter (SERT) and the 5-HT1A receptor. Compounds 5b and 5f showed nanomolar affinities for both targets. The experimental data were rationalized according to results obtained from docking experiments. These findings are in agreement with our proposal that bis-indole derivatives can bind both targets, and might serve as leads in the quest of ligands endowed with a dual mechanism of action. (C) 2013 Elsevier Ltd. All rights reserved.
dc.description.funderFONDECYT
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.bmc.2013.10.036
dc.identifier.eissn1464-3391
dc.identifier.issn0968-0896
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2013.10.036
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/101914
dc.identifier.wosidWOS:000327766200007
dc.issue.numero24
dc.language.isoen
dc.pagina.final7611
dc.pagina.inicio7604
dc.revistaBioorganic & medicinal chemistry
dc.rightsacceso restringido
dc.subjectPiperazinylpropylindole derivatives
dc.subjectSerotonin transporter
dc.subject5-Hydroxytryptamine 1A receptor
dc.subjectBivalent ligands
dc.subjectDocking
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleSynthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT<sub>1A</sub> receptor
dc.typeartículo
dc.volumen21
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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