Publication:
Design, synthesis, acetylcholinesterase inhibition and larvicidal activity of girgensohnine analogs on Aedes aegypti, vector of dengue fever

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col.comunidadvinculadaComunidad científica colombianaes_CO
col.contrato0572-2012es_CO
col.date.proyecto2018-01
col.programa.colcienciasProgramas de CT+I Ejecutados por Redes de Conocimientoes_CO
col.tipo.espArtículos de investigaciónes_CO
dc.audienceAdministradores de ciencia y tecnologíaes_CO
dc.audienceInvestigadoreses_CO
dc.coverage.spatialColombiaes_CO
dc.creatorCarreño Otero, Aurora L.
dc.creatorVargas Méndez, Leonor Yamile
dc.creatorDuque L., Jonny Edward
dc.creatorKouznetsov, Vladimir V.
dc.creator.corporativoBio-Red-CO-CENIVAMes_CO
dc.creator.corporativoUniversidad Industrial de Santander, UISes_CO
dc.creator.corporativoUniversidad Santo Tomás, USTA - Seccional Bucaramangaes_CO
dc.creator.mailkouznet@uis.edu.coes_CO
dc.date.accessioned2019-04-01T00:03:10Z
dc.date.available2019-04-01T00:03:10Z
dc.date.embargoEndinfo:eu-repo/date/embargoEnd/2024-01-31es_CO
dc.date.issued2014-03
dc.description.abstractGirgensohnine alkaloid was used as a natural model in the design and generation of new alkaloid-like α-aminonitrilea series that was completed by the use of SSA-catalyzed Strecker reaction between commercial and inexpensive substituted benzaldehydes, piperidine (pyrrolidine, morpholine and N-methylpiperazine) and acetone cyanohydrin. Calculated ADMETox parameters of the designed analogs revealed their good pharmacokinetic profiles indicating lipophilic characteristics. In vitro AChE enzyme test showed that obtained a-aminonitriles could be considered as AChEIs with micromolar IC50 values ranging from 42.0 to 478.0 mM (10.3e124.0 mg/mL). Among this series, the best AChE inhibitor was the pyrrolidine a-aminonitrile 3 (IC50 ¼ 42 mM), followed by the piperidine a-aminonitriles 2 and 6 (IC50 ¼ 45 mM and IC50 ¼ 51 mM, respectively), and the compound 7 (IC50 ¼ 51 mM). In vivo insecticidal activity of more active AChEIs against Aedes aegypti larvae was also performed showing a good larvicidal activity at concentrations less than 140 ppm, highlighting products 2 and 7 that could serve as lead compounds to develop new potent and selective insecticides.es_CO
dc.description.isprojectnoes_CO
dc.description.projectid5507-543-31904es_CO
dc.description.projectnamePrograma: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombianaes_CO
dc.description.sponsorshipDepartamento Administrativo de Ciencia, Tecnología e Innovación [CO] Colcienciases_CO
dc.formatpdfes_CO
dc.format.extent9 páginases_CO
dc.identifier.bibliographicCitationContiene 44 referencias bibliográficas. Véase documento adjuntoes_CO
dc.identifier.doi10.1016/j.ejmech.2014.03.067
dc.identifier.issn0223-5234
dc.identifier.urihttp://repositorio.colciencias.gov.co/handle/11146/34168
dc.language.isoenges_CO
dc.relation.ispartofPrograma: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombiana. La publicación completa está disponible en : <a href="http://repositorio.colciencias.gov.co/handle/11146/34163" target="blank">http://repositorio.colciencias.gov.co/handle/11146/34163</a>es_CO
dc.rightsinfo:eu-repo/semantics/embargoedAccesses_CO
dc.sourceEuropean Journal of Medicinal Chemistry 78 (2014) 392-400es_CO
dc.subject.keywordα-Aminonitriles
dc.subject.keywordStrecker reaction
dc.subject.keywordAChE inhibition
dc.subject.keywordLarvicidal activity
dc.subject.keywordAedes aegypti larvae
dc.subject.lembCromatografía de gaseses_CO
dc.subject.lembAceites vegetaleses_CO
dc.subject.spinesCatalizadoreses_CO
dc.subject.spinesBioquímica vegetales_CO
dc.subject.spinesBiotecnologíaes_CO
dc.subject.spinesQuímica agrícolaes_CO
dc.subject.spinesBiología moleculares_CO
dc.titleDesign, synthesis, acetylcholinesterase inhibition and larvicidal activity of girgensohnine analogs on Aedes aegypti, vector of dengue feveres_CO
dc.typeArtículo científicoes_CO
dc.type.driverinfo:eu-repo/semantics/articlees_CO
dc.type.hasversioninfo:eu-repo/semantics/publishedVersiones_CO
dspace.entity.typePublication

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