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
- Benchekroun, Mohamed
- Romero, Alejandro
- Egea, Javier
- Leon, Rafael
- Michalska, Patrycja
- Buendia, Izaskun
- Jimeno, Maria Luisa
- Jun, Daniel
- Janockova, Jana
- Sepsova, Vendula
- Soukup, Ondrej
- Bautista-Aguilera, Oscar M.
- Refouvelet, Bernard
- Ouari, Olivier
- Marco-Contelles, Jose
- Ismaili, Lhassane
Publication date
November 2016
DOI Publisher
American Chemical Society (ACS)Abstract
International audienceNovel 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
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