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, León, Rafael, Michalska, Patrycja, Buendía, Izaskun, Jimeno, María Luisa, Jun, Daniel, Janockova, Jana, Sepsova, Vendula, Soukup, Ondrej, Bautista-Aguilera, Oscar M, Refouvelet, Bernard, Ouari, Olivier, Marco-Contelles, José and Ismaili, Lhassane (2016) 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, 59 (21). pp. 9967-9973. ISSN 0022-2623

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Abstract

Novel 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.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Research Centres and Groups: Sussex Drug Discovery Centre
Subjects: R Medicine > RS Pharmacy and materia medica > RS0153 Materia medica > RS0400 Pharmaceutical chemistry
Depositing User: Mohamed Benchekroun
Date Deposited: 14 Nov 2016 10:35
Last Modified: 14 Nov 2016 15:06
URI: http://sro.sussex.ac.uk/id/eprint/65413
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