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 - Archive ouverte HAL
Article Dans Une Revue Journal of Medicinal Chemistry Année : 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

Javier Egea
  • Fonction : Auteur
Rafael Leon
  • Fonction : Auteur
Patrycja Michalska
  • Fonction : Auteur
Izaskun Buendia
  • Fonction : Auteur
Maria Luisa Jimeno
  • Fonction : Auteur
Daniel Jun
Jana Janockova
Vendula Sepsova
  • Fonction : Auteur
Ondrej Soukup
Oscar M. Bautista-Aguilera
  • Fonction : Auteur
Jose Marco-Contelles
  • Fonction : Auteur

Résumé

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.
Fichier non déposé

Dates et versions

hal-01460668 , version 1 (07-02-2017)

Identifiants

Citer

Mohamed Benchekroun, Alejandro Romero, Javier Egea, Rafael Leon, Patrycja Michalska, et al.. 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, 2016, 59 (21), pp.9967--9973. ⟨10.1021/acs.jmedchem.6b01178⟩. ⟨hal-01460668⟩
153 Consultations
0 Téléchargements

Altmetric

Partager

More