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Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor

dc.contributor.authorPessoa-Mahana H.
dc.contributor.authorGonzález-Lira C.
dc.contributor.authorFierro A.
dc.contributor.authorZapata-Torres G.
dc.contributor.authorPessoa-Mahana C.D.
dc.contributor.authorOrtiz-Severin J.
dc.contributor.authorIturriaga-Vásquez P.
dc.contributor.authorReyes-Parada M.
dc.contributor.authorSilva-Matus P.
dc.contributor.authorSaitz-Barría C.
dc.contributor.authorAraya-Maturana R.
dc.date.accessioned2020-09-02T22:25:48Z
dc.date.available2020-09-02T22:25:48Z
dc.date.issued2013
dc.identifier10.1016/j.bmc.2013.10.036
dc.identifier.citation21, 24, 7604-7611
dc.identifier.issn09680896
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5786
dc.descriptionA 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. © 2013 Elsevier Ltd. All rights reserved.
dc.language.isoen
dc.subject5-Hydroxytryptamine 1A receptor
dc.subjectBivalent ligands
dc.subjectDocking
dc.subjectPiperazinylpropylindole derivatives
dc.subjectSerotonin transporter
dc.subject1,4 bis[3 (1h 3 indolyl)propyl]piperazine
dc.subject1,4 bis[3 (5 bromo 1h 3 indolyl)propyl]piperazine
dc.subject1,4 bis[3 (5 fluoro 1h 3 indolyl]propyl)piperazine
dc.subject1,4 bis[3 (5 methoxy 1h 3 indolyl]propyl)piperazine
dc.subject3 [3 [4 [3 (1h 3 indolyl)propyl] 1 piperazinyl]propyl] 5 bromo 1h indol
dc.subject3 [3 [4 [3 (1h 3 indolyl)propyl] 1 piperazinyl]propyl] 5 fluoro 1h indol
dc.subject3 [3 [4 [3 (1h 3 indolyl)propyl] 1 piperazinyl]propyl] 5 methoxy 1h indol
dc.subject3 [3 [4 [3 (1h indol 3 yl)propyl]piperazin 1 yl]propyl] 1h indole derivative
dc.subject5 bromo 3 [3 [4 [3 (5 fluoro 1h 3 indolyl)propyl]piperazinyl]propyl] 1h indol
dc.subject5 bromo 3 [3 [4 [3 (5 methoxy 1h 3 indolyl)propyl]piperazinyl]propyl] 1h indol
dc.subject5 fluoro 3 [3 [4 [3 (5 methoxy 1h 3 indolyl)propyl]piperazinyl]propyl] 1h indol
dc.subjectcitalopram
dc.subjectindole derivative
dc.subjectserotonin 1A receptor
dc.subjectserotonin transporter
dc.subjectunclassified drug
dc.subjectanimal tissue
dc.subjectarticle
dc.subjectbinding affinity
dc.subjectcontrolled study
dc.subjectdrug structure
dc.subjectdrug synthesis
dc.subjecthuman
dc.subjecthuman cell
dc.subjectin vitro study
dc.subjectmolecular docking
dc.subjectnonhuman
dc.subjectrat
dc.subject5-Hydroxytryptamine 1A receptor
dc.subjectBivalent ligands
dc.subjectDocking
dc.subjectPiperazinylpropylindole derivatives
dc.subjectSerotonin transporter
dc.subjectDose-Response Relationship, Drug
dc.subjectHumans
dc.subjectIndoles
dc.subjectModels, Molecular
dc.subjectMolecular Docking Simulation
dc.subjectMolecular Structure
dc.subjectPiperazines
dc.subjectReceptor, Serotonin, 5-HT1A
dc.subjectSerotonin Plasma Membrane Transport Proteins
dc.subjectStructure-Activity Relationship
dc.titleSynthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor
dc.typeArticle


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