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 |
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Authors: | Pessoa-Mahana Hernán Recabarren-Gajardo Gonzalo Temer Jenny Fiedler Zapata-Torres Gerald Pessoa-Mahana C David Barría Claudio Saitz Araya-Maturana Ramiro |
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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 |
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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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