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dc.contributor | Facultad de Veterinaria | es_ES |
dc.contributor.author | Tejería, Ana | |
dc.contributor.author | Pérez Pertejo, Maria Yolanda | |
dc.contributor.author | Reguera Torres, Rosa María | |
dc.contributor.author | Carbajo Andrés, Rubén | |
dc.contributor.author | Balaña Fouce, Rafael | |
dc.contributor.author | Alonso Pérez, Concepción Estíbaliz | |
dc.contributor.author | Martín Encinas, Endika | |
dc.contributor.author | Selas, Asier | |
dc.contributor.author | Rubiales, Gloria | |
dc.contributor.author | Palacios, Francisco | |
dc.contributor.other | Toxicologia | es_ES |
dc.date | 2019-01-15 | |
dc.date.accessioned | 2024-01-25T08:53:49Z | |
dc.date.available | 2024-01-25T08:53:49Z | |
dc.identifier.citation | Tejería, A., Pérez-Pertejo, Y., Reguera, R. M., Carbajo-Andrés, R., Balaña-Fouce, R., Alonso, C., Martin-Encinas, E., Selas, A., Rubiales, G., & Palacios, F. (2019). Antileishmanial activity of new hybrid tetrahydroquinoline and quinoline derivatives with phosphorus substituents. European Journal of Medicinal Chemistry, 162, 18-31. https://doi.org/10.1016/J.EJMECH.2018.10.065 | es_ES |
dc.identifier.issn | 0223-5234 | |
dc.identifier.other | https://www.sciencedirect.com/science/article/pii/S0223523418309425?via%3Dihub | es_ES |
dc.identifier.uri | https://hdl.handle.net/10612/17795 | |
dc.description.abstract | [EN] Heterocyclic compounds, such as hybrid tetrahydroquinoline and quinoline derivatives with phosphorated groups, have been prepared by multicomponent cycloaddition reaction between phosphorus-substituted anilines, aldehydes and styrenes. The antileishmanial activity of these compounds has been evaluated on both promastigotes and intramacrophagic amastigotes of Leishmania infantum. Good antileishmanial activity of functionalized tetrahydroquinolines 4a, 5a, 6b and quinoline 8b has been observed with similar activity than the standard drug amphotericin B and close selective index (SI between 43 and 57) towards L. infantum amastigotes to amphotericin B. Special interest shows tetrahydroquinolylphosphine sulfide 5a with an EC50 value (0.61 ± 0.18 μM) similar to the standard drug amphotericin B (0.32 ± 0.05 μM) and selective index (SI = 56.87). In addition, compound 4c shows remarkable inhibition on Leishmania topoisomerase IB. Parallel theoretical study of stereoelectronic properties, application of docking-based virtual screening methods, along with molecular electrostatic potential and predictive druggability analyses are also reported. | es_ES |
dc.language | eng | es_ES |
dc.publisher | Elsevier | es_ES |
dc.subject | Farmacología | es_ES |
dc.subject.other | Leishmania | es_ES |
dc.subject.other | Phosphorus substituted quinoline derivatives | es_ES |
dc.subject.other | DNA-Topoisomerase | es_ES |
dc.title | Antileishmanial activity of new hybrid tetrahydroquinoline and quinoline derivatives with phosphorus substituents | es_ES |
dc.title.alternative | Actividad frente a Leishmania de nuevos derivados híbridos de tetrahidroquinolina y quinolina con sustituyentes de fósforo | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.identifier.doi | 10.1016/j.ejmech.2018.10.065 | |
dc.description.peerreviewed | SI | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/AEI/ Programa Estatal de I+D+i Orientada a los Retos de la Sociedad / SAF2017-83575-R /ES/ AUTOVIA A LOS LISOSOMAS: DIRIGIENDO A MACROFAGOS INFECTADOS / | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/MINECO/ Programa Estatal de I+D+I Orientada a los Retos de la Sociedad / CTQ2015-67871-R /ES/ NUEVAS HERRAMIENTAS SINTETICAS BASADAS EN ORGANOCATALISIS, REACCIONES UMPOLUNG Y FORMACION SELECTIVA DE HETEROCICLOS NITROGENADOS PARA PREPARACION DE INHIBIDORES ENZIMATICOS // | es_ES |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es_ES |
dc.journal.title | European Journal of Medicinal Chemistry | es_ES |
dc.volume.number | 162 | es_ES |
dc.page.initial | 18 | es_ES |
dc.page.final | 31 | es_ES |
dc.type.hasVersion | info:eu-repo/semantics/draft | es_ES |
dc.subject.unesco | 32 Ciencias Médicas | es_ES |
dc.subject.unesco | 3214 Toxicología | es_ES |
dc.description.project | Financial support from the Ministerio de Economía y Competitividad (MINECO, AEI, FEDER, UE) [MINECO: AGL2016-79813-C2-1R, SAF2017-83575-R and CTQ2015-67871-R], Gobierno Vasco (GV, IT 992-16) and the Junta de Castilla y León cofinanced by FEDER, UE [LE020P17] is gratefully acknowledged. Technical and human support provided by IZO-SGI, SGIker (UPV/EHU, MICINN, GV/EJ, ERDF and ESF) is gratefully acknowledged. | es_ES |
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