Chile | Artículos de revistas

Synthesis, docking studies and biological evaluation of benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives on 5-HT 1A serotonin receptors

dc.creatorPessoa Mahana, Hernán
dc.creatorRecabarren Gajardo, Gonzalo Iván
dc.creatorTemer, Jenny Fiedler
dc.creatorZapata Torres, Gerald
dc.creatorPessoa Mahana, Carlos David
dc.creatorBarría, Claudio Saitz
dc.creatorAraya Maturana, Ramiro
dc.date.accessioned2018-12-20T15:10:34Z
dc.date.available2018-12-20T15:10:34Z
dc.date.created2018-12-20T15:10:34Z
dc.date.issued2012
dc.identifierMolecules, Volumen 17, Issue 2, 2018, Pages 1388-1407
dc.identifier14203049
dc.identifier10.3390/molecules17021388
dc.identifierhttps://repositorio.uchile.cl/handle/2250/158243
dc.description.abstractA series of novel benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1- one derivatives 6a-f, 7a-f and their corresponding alcohols 8a-f were synthesized and evaluated for their affinity towards 5-HT 1A receptors. The influence of arylpiperazine moiety and benzo[b]thiophene ring substitutions on binding affinity was studied. The most promising analogue, 1-(benzo[b]thiophen-2-yl)-3-(4-(pyridin-2-yl)piperazin-1-yl)propan- 1-one (7e) displayed micromolar affinity (K i = 2.30 μM) toward 5-HT 1A sites. Docking studies shed light on the relevant electrostatic interactions which could explain the observed affinity for this compound.
dc.languageen
dc.rightshttp://creativecommons.org/licenses/by-nc-nd/3.0/cl/
dc.rightsAttribution-NonCommercial-NoDerivs 3.0 Chile
dc.sourceMolecules
dc.subject5-HT1A receptor
dc.subjectArylpiperazines
dc.subjectBenzo[b]thiophene
dc.subjectDepression
dc.subjectDocking
dc.subjectMicrowave Michael addition
dc.titleSynthesis, docking studies and biological evaluation of benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives on 5-HT 1A serotonin receptors
dc.typeArtículos de revistas


Este ítem pertenece a la siguiente institución