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Synthesis, docking studies and biological evaluation of benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives on 5-HT1A serotonin receptors
Authors:Pessoa-Mahana Hernán  Recabarren-Gajardo Gonzalo  Temer Jenny Fiedler  Zapata-Torres Gerald  Pessoa-Mahana C David  Barría Claudio Saitz  Araya-Maturana Ramiro
Institution:Departamento de Química Orgánica y Fisicoquímica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Casilla 233, Santiago 1, Chile. hpessoa@ciq.uchile.cl
Abstract:A series of novel benzob]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 benzob]thiophene ring substitutions on binding affinity was studied. The most promising analogue, 1-(benzob]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.
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