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The Antioxidant Additive Approach for Alzheimer’s Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators

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dc.contributor.authorBenchekroun, Mohamed
dc.contributor.authorRomero Hernández, Alejandro
dc.contributor.authorEgea, Javier
dc.contributor.authorLeón Martínez, Rafael
dc.contributor.authorMichalska Dziama, Patrycja
dc.contributor.authorBuendía, Izaskun
dc.contributor.authorJimeno, María Luisa
dc.contributor.authorJun, Daniel
dc.contributor.authorJanockova, Jana
dc.contributor.authorSepsova, Vendula
dc.contributor.authorSoukup, Ondrej
dc.contributor.authorBautista-Aguilera, Oscar
dc.contributor.authorRefouvelet, Bernard
dc.contributor.authorOuari, Olivier
dc.contributor.authorMarco Contelles, José Luis
dc.contributor.authorIsmaili, Lhassane
dc.date.accessioned2024-01-31T12:44:37Z
dc.date.available2024-01-31T12:44:37Z
dc.date.issued2016
dc.description.abstractNovel multifunctional tacrines for Alzheimer’s disease were obtained by Ugi-reaction between ferulic (or lipoic acid), a melatonin-like isocyanide, formaldehyde, and tacrine derivatives, according to the antioxidant additive approach in order to modulate the oxidative stress as therapeutic strategy. Compound 5c has been identified as a promising permeable agent showing excellent antioxidant properties, strong cholinesterase inhibitory activity, less hepatotoxicity than tacrine, and the best neuroprotective capacity, being able to significantly activate the Nrf2 transcriptional pathway.
dc.description.departmentDepto. de Química en Ciencias Farmacéuticas
dc.description.facultyFac. de Farmacia
dc.description.refereedTRUE
dc.description.sponsorshipConseil régional de Franche-Comté (France)
dc.description.sponsorshipInstituto de Salud Carlos III
dc.description.sponsorshipFaculty of Military Health Sciences, University of Defence (Czech Republic)
dc.description.sponsorshipBayer AG
dc.description.sponsorshipFundación FIPSE
dc.description.sponsorshipMinisterio de Educación, Cultura y Deporte (España)
dc.description.statuspub
dc.identifier.citationBenchekroun, Mohamed, et al. «The Antioxidant Additive Approach for Alzheimer’s Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators». Journal of Medicinal Chemistry, vol. 59, n.o 21, noviembre de 2016, pp. 9967-73. https://doi.org/10.1021/acs.jmedchem.6b01178.
dc.identifier.doi10.1021/acs.jmedchem.6b01178
dc.identifier.issn0022-2623
dc.identifier.officialurlhttps://doi.org/10.1021/acs.jmedchem.6b01178
dc.identifier.urihttps://hdl.handle.net/20.500.14352/97148
dc.issue.number21
dc.journal.titleJournal of Medicinal Chemistry
dc.language.isoeng
dc.page.final9973
dc.page.initial9967
dc.relation.projectIDinfo:eu-repo/grantAgreement/CP14/00008
dc.relation.projectIDinfo:eu-repo/grantAgreement/00179906
dc.relation.projectIDinfo:eu-repo/grantAgreement/PI14/00372
dc.relation.projectIDinfo:eu-repo/grantAgreement/2015-03-1282
dc.relation.projectIDinfo:eu-repo/grantAgreement/12-00001344-15
dc.relation.projectIDinfo:eu-repo/grantAgreement/FPU13/03737
dc.rights.accessRightsrestricted access
dc.subject.keywordMultitarget ligand
dc.subject.keywordNrf2 pathway
dc.subject.keywordAlzheimer´s disease
dc.subject.keywordDrug discovery
dc.subject.ucmCiencias Biomédicas
dc.subject.unesco23 Química
dc.titleThe Antioxidant Additive Approach for Alzheimer’s Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators
dc.typejournal article
dc.type.hasVersionVoR
dc.volume.number59
dspace.entity.typePublication
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relation.isAuthorOfPublication7093c6ce-e368-44f0-a993-8f7212cb1c2a
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relation.isAuthorOfPublication20877297-0870-49ef-a0fb-9fc4cba06794
relation.isAuthorOfPublication.latestForDiscovery7093c6ce-e368-44f0-a993-8f7212cb1c2a

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