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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
journal contribution
posted on 2023-06-09, 03:59 authored by Mohamed Benchekroun, Alejandro Romero, Javier Egea, Rafael León, Patrycja Michalska, Izaskun Buendía, María Luisa Jimeno, Daniel Jun, Jana Janockova, Vendula Sepsova, Ondrej Soukup, Oscar M Bautista-Aguilera, Bernard Refouvelet, Olivier Ouari, José Marco-Contelles, Lhassane IsmailiNovel 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.
History
Publication status
- Published
Journal
Journal of Medicinal ChemistryISSN
0022-2623Publisher
American Chemical SocietyExternal DOI
Issue
21Volume
59Page range
9967-9973Department affiliated with
- Chemistry Publications
Research groups affiliated with
- Sussex Drug Discovery Centre Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2016-11-14Usage metrics
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