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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

AuthorsBenchekroun, M.; Romero, A.; Egea, Javier; León, Rafael ; Michalska, P.; Buendía, I.; Jimeno, M. Luisa CSIC ORCID; Jun, D.; Janockova, J.; Sepsova, V.; Soukup, O.; Bautista-Aguilera, Óscar M.; Refouvelet, B.; Ouari, O.; Marco-Contelles, José CSIC ORCID; Ismaili, L.
Issue Date2016
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 59: 9967-9973 (2016)
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.
Publisher version (URL)
Identifiersdoi: 10.1021/acs.jmedchem.6b01178
issn: 0022-2623
e-issn: 1520-4804
Appears in Collections:(CENQUIOR) Artículos
(IQOG) Artículos

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