Exploring the Potential of Sulfonamide-Dihydropyridine Hybrids as Multitargeted Ligands for Alzheimer's Disease Treatment.
Fiche publication
Date publication
juin 2023
Journal
International journal of molecular sciences
Auteurs
Membres identifiés du Cancéropôle Est :
Pr BEDUNEAU Arnaud
Tous les auteurs :
Dakhlaoui I, Bernard PJ, Pietrzak D, Simakov A, Maj M, Refouvelet B, Béduneau A, Cornu R, Jozwiak K, Chabchoub F, Iriepa I, Martin H, Marco-Contelles J, Ismaili L
Lien Pubmed
Résumé
Alzheimer's disease (AD) is a multifactorial neurodegenerative disease that has a heavy social and economic impact on all societies and for which there is still no cure. Multitarget-directed ligands (MTDLs) seem to be a promising therapeutic strategy for finding an effective treatment for this disease. For this purpose, new MTDLs were designed and synthesized in three steps by simple and cost-efficient procedures targeting calcium channel blockade, cholinesterase inhibition, and antioxidant activity. The biological and physicochemical results collected in this study allowed us the identification two sulfonamide-dihydropyridine hybrids showing simultaneous cholinesterase inhibition, calcium channel blockade, antioxidant capacity and Nrf2-ARE activating effect, that deserve to be further investigated for AD therapy.
Mots clés
Hantzsch reaction, Nrf2, calcium channel antagonism, cholinesterase inhibition, multitarget directed ligands
Référence
Int J Mol Sci. 2023 06 4;24(11):