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dc.contributor.authorAutorEspinosa-Saez, Roger
dc.contributor.authorAutorRobledo, Sara M.
dc.contributor.authorAutorPineda, Tatiana
dc.contributor.authorAutorMurillo, Javier
dc.contributor.authorAutorZúñiga, César
dc.contributor.authorAutorYáñez, Osvaldo
dc.contributor.authorAutorCantero-López, Plinio
dc.contributor.authorAutorSaez-Vega, Alex
dc.contributor.authorAutorGuzmán-Teran, Camilo
dc.date.accessionedFecha ingreso2024-09-03T19:17:37Z
dc.date.availableFecha disponible2024-09-03T19:17:37Z
dc.date.issuedFecha publicación2023
dc.identifier.citationReferencia BibliográficaScientific Reports, 13(1), 16 p.
dc.identifier.issnISSN2045-2322
dc.identifier.uriURLhttp://repositorio.udla.cl/xmlui/handle/udla/1333
dc.identifier.uriURLhttps://www.nature.com/srep/
dc.description.abstractResumenIn this study, six analogs of 2-arylquinoline were synthesized and evaluated for their in vitro and in vivo antiplasmodial and leishmanicidal activity. At a later stage, hemolytic activity and druggability were tested in vitro and in silico, respectively, observing as a result: firstly, compounds showed half-maximal effective concentration (EC50) values between 3.6 and 19.3 µM. Likewise, a treatment using the compounds 4a–f caused improvement in most of the treated hamsters and cured some of them. Regarding the antiplasmodial activity, the compounds showed moderate to high activity, although they did not show hemolytic activity. Furthermore, 4e and 4f compounds were not able to control P. berghei infection when administered to animal models. Molecular dynamic simulations, molecular docking and ligand binding affinity indicate good characteristics of the studied compounds, which are expected to be active. And lastly, the compounds are absorbable at the hematoencephalic barrier but not in the gastrointestinal tract. In summary, ADMET properties suggest that these molecules may be used as a safe treatment against Leishmania.
dc.format.extentdc.format.extent16 páginas
dc.format.extentdc.format.extent1.455Mb
dc.format.mimetypedc.format.mimetypePDF
dc.language.isoLenguaje ISOeng
dc.publisherEditorNature Research
dc.rightsDerechosCreative Commons Attribution License (CC BY)
dc.sourceFuentesScientific Reports
dc.subject.lcshdc.subject.lcshAnimales
dc.subject.lcshdc.subject.lcshAntimaláricos
dc.subject.lcshdc.subject.lcshAgentes antiprotozoarios
dc.subject.lcshdc.subject.lcshLeishmania
dc.titleTítuloScreening of the antileishmanial and antiplasmodial potential of synthetic 2-arylquinoline analogs
dc.typeTipo de DocumentoArtículo
dc.udla.catalogadordc.udla.catalogadorCBM
dc.udla.indexdc.udla.indexScience Citation Index Expanded
dc.udla.indexdc.udla.indexScopus
dc.udla.indexdc.udla.indexAcademic Search Ultimate
dc.udla.indexdc.udla.indexNatural Science Collection
dc.udla.indexdc.udla.indexDOAJ
dc.udla.indexdc.udla.indexBiological Science Database
dc.udla.indexdc.udla.indexBiomedical Reference Collection
dc.udla.indexdc.udla.indexBIOSIS
dc.udla.indexdc.udla.indexCAB Abstracts
dc.udla.indexdc.udla.indexEMBASE
dc.udla.indexdc.udla.indexHealth Research Premium Collection
dc.udla.indexdc.udla.indexMEDLINE
dc.identifier.doidc.identifier.doi10.1038/s41598-023-43805-4
dc.facultaddc.facultadFacultad de Ingeniería y Negocios


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