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QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy

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dc.contributor.authorRamos Alonso, Eva
dc.contributor.authorPalomino-Antolín, Alejandra
dc.contributor.authorBartolini, Manuela
dc.contributor.authorIriepa, Isabel
dc.contributor.authorMoraleda, Ignacio
dc.contributor.authorDiez-Iriepa, Daniel
dc.contributor.authorSamadi, Abdelouahid
dc.contributor.authorCortina, Carol V.
dc.contributor.authorChioua, Mourad
dc.contributor.authorEgea, Javier
dc.contributor.authorRomero Martínez, Manuel Alejandro
dc.contributor.authorMarco-Contelles, José
dc.date.accessioned2023-06-17T12:34:24Z
dc.date.available2023-06-17T12:34:24Z
dc.date.issued2019-04-17
dc.description.abstractWe report the synthesis and relevant pharmacological properties of the quinoxalinetacrine (QT) hybrid QT78 in a project targeted to identify new non-hepatotoxic tacrine derivatives for Alzheimer’s disease therapy. We have found that QT78 is less toxic than tacrine at high concentrations (from 100 μM to 1 mM), less potent than tacrine as a ChE inhibitor, but shows selective BuChE inhibition (IC50 (hAChE) = 22.0 ± 1.3 μM; IC50 (hBuChE) = 6.79 ± 0.33 μM). Moreover, QT78 showed effective and strong neuroprotection against diverse toxic stimuli, such as rotenone plus oligomycin-A or okadaic acid, of biological significance for Alzheimer’s disease.
dc.description.departmentSección Deptal. de Farmacología y Toxicología (Veterinaria)
dc.description.facultyFac. de Veterinaria
dc.description.refereedTRUE
dc.description.sponsorshipMinisterio de Ciencia e Innovación (MICINN)
dc.description.sponsorshipInstituto de Salud Carlos III/FEDER (European Regional Development Fund)
dc.description.sponsorshipFundación Mutua Madrileña
dc.description.statuspub
dc.eprint.idhttps://eprints.ucm.es/id/eprint/65102
dc.identifier.doi10.3390/molecules24081503
dc.identifier.issn1420-3049
dc.identifier.officialurlhttps://doi.org/10.3390/molecules24081503
dc.identifier.relatedurlhttps://www.mdpi.com/1420-3049/24/8/1503
dc.identifier.urihttps://hdl.handle.net/20.500.14352/12527
dc.issue.number8
dc.journal.titleMolecules
dc.language.isoeng
dc.page.initial1503
dc.publisherMDPI
dc.relation.projectID(SAF2006-08764-C02-01 and ISCIII [RED RENEVAS (RD06/0026/1002))
dc.relation.projectIDMIguel Servet CP14/00008;PI16/00735)
dc.rightsAtribución 3.0 España
dc.rights.accessRightsopen access
dc.rights.urihttps://creativecommons.org/licenses/by/3.0/es/
dc.subject.keywordAlzheimer’s disease
dc.subject.keywordcholinesterase inhibitor
dc.subject.keywordhepatotoxicity
dc.subject.keywordmolecular modeling
dc.subject.keywordneuroprotection
dc.subject.keywordquinoxalines
dc.subject.keywordquinoxalinetacrines
dc.subject.keywordtacrine
dc.subject.ucmNeurociencias (Medicina)
dc.subject.ucmFarmacología veterinaria
dc.subject.unesco2490 Neurociencias
dc.subject.unesco3109.08 Farmacología
dc.titleQuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy
dc.typejournal article
dc.volume.number24
dspace.entity.typePublication
relation.isAuthorOfPublication5f16335c-a2b9-4244-b00f-215f16e7150c
relation.isAuthorOfPublicationc658be58-bda9-4100-ad65-bac31e1256af
relation.isAuthorOfPublication.latestForDiscovery5f16335c-a2b9-4244-b00f-215f16e7150c

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