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dc.contributor.authorBenchekroun, M.-
dc.contributor.authorRomero, A.-
dc.contributor.authorEgea, Javier-
dc.contributor.authorLeón, Rafael-
dc.contributor.authorMichalska, P.-
dc.contributor.authorBuendía, I.-
dc.contributor.authorJimeno, M. Luisa-
dc.contributor.authorJun, D.-
dc.contributor.authorJanockova, J.-
dc.contributor.authorSepsova, V.-
dc.contributor.authorSoukup, O.-
dc.contributor.authorBautista-Aguilera, Óscar M.-
dc.contributor.authorRefouvelet, B.-
dc.contributor.authorOuari, O.-
dc.contributor.authorMarco-Contelles, José-
dc.contributor.authorIsmaili, L.-
dc.identifierdoi: 10.1021/acs.jmedchem.6b01178-
dc.identifierissn: 0022-2623-
dc.identifiere-issn: 1520-4804-
dc.identifier.citationJournal of Medicinal Chemistry 59: 9967-9973 (2016)-
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.sponsorshipB.R. and L.I. thank the Regional Council of Franche-Comté (France) for financial support, and M.-J. Henriot (PHV Pharma) for support in the HPLC analyses. M.B. thanks the Regional Council of Franche-Comté(France) for a Ph.D. grant. J.E. has a grant from ISCIII (Programa Miguel Servet, CP14/00008). D.J., J.J., V.S., and O.S. thank Jitka Pichova for a skillful technical assistance. This work was supported by the project MH CZ-DRO (UHHK, 00179906) and by Long Term Development Plan-1011 of Faculty of Military Health Sciences, University of Defence (Czech Republic). R.L. thanks ISCIII (Programa Miguel Servet, CP11/00165; grant PI14/00372), Bayer AG “From targets to novel drugs” (grant 2015-03-1282) and Fundación FIPSE (grant 12-00001344-15). P.M. thanks MECD for a FPU fellowship (FPU13/03737).-
dc.publisherAmerican Chemical Society-
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.description.versionPeer Reviewed-
dc.contributor.funderMinistry of Health of the Czech Republic-
dc.contributor.funderInstituto de Salud Carlos III-
dc.contributor.funderFundación para la Investigación y la Prevención del Sida en España-
dc.contributor.funderMinisterio de Educación, Cultura y Deporte (España)-
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