Author | dc.contributor.author | Pessoa Mahana, Hernán | |
Author | dc.contributor.author | Recabarren Gajardo, Gonzalo Iván | es_CL |
Author | dc.contributor.author | Fiedler Temer, Jenny | es_CL |
Author | dc.contributor.author | Zapata Torres, Gerald Amilcar | es_CL |
Author | dc.contributor.author | Pessoa Mahana, Carlos David | es_CL |
Author | dc.contributor.author | Saitz Barría, Claudio | es_CL |
Author | dc.contributor.author | Araya Maturana, Ramiro | es_CL |
Admission date | dc.date.accessioned | 2012-06-27T16:50:50Z | |
Available date | dc.date.available | 2012-06-27T16:50:50Z | |
Publication date | dc.date.issued | 2012 | |
Cita de ítem | dc.identifier.citation | Molecules 2012, 17, 1388-1407 | es_CL |
Identifier | dc.identifier.issn | 1420-3049 | |
Identifier | dc.identifier.other | doi:10.3390/molecules17021388 | |
Identifier | dc.identifier.uri | https://repositorio.uchile.cl/handle/2250/121667 | |
General note | dc.description | Artículo de publicación ISI | es_CL |
Abstract | dc.description.abstract | A series of novel benzobthiophen-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-HT1A receptors. The influence of arylpiperazine
moiety and benzobthiophene 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 (Ki = 2.30 μM) toward 5-HT1A sites. Docking
studies shed light on the relevant electrostatic interactions which could explain the
observed affinity for this compound. | es_CL |
Patrocinador | dc.description.sponsorship | Fondo Nacional de Ciencia y Tecnología FONDECYT Research Projects
Nº 1050289 and 1090169 | es_CL |
Lenguage | dc.language.iso | en | es_CL |
Keywords | dc.subject | arylpiperazines | es_CL |
Título | dc.title | Synthesis, Docking Studies and Biological Evaluation of Benzobthiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one Derivatives on 5-HT1A Serotonin Receptors | es_CL |
Document type | dc.type | Artículo de revista | |