Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca2+ Channel Blocking Ability, Cholinesterase Inhibition, Antioxidant Capacity, and Nrf2 Activation - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Molecules Année : 2023

Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca2+ Channel Blocking Ability, Cholinesterase Inhibition, Antioxidant Capacity, and Nrf2 Activation

Rim Malek
  • Fonction : Auteur
Alexey Simakov
  • Fonction : Auteur
Audrey Davis
Maciej Maj
  • Fonction : Auteur
Paul Bernard
  • Fonction : Auteur
Artur Wnorowski
Helene Martin
José Marco-Contelles
  • Fonction : Auteur
Fakher Chabchoub
  • Fonction : Auteur
Patrick Dallemagne
Krzysztof Jozwiak
Lhassane Ismaili

Résumé

Novel multitarget-directed ligands BIGI 4a-d and BIGI 5a-d were designed and synthesized with a simple and cost-efficient procedure via a one-pot three-component Biginelli reaction targeting acetyl-/butyrylcholinesterases inhibition, calcium channel antagonism, and antioxidant ability. Among these multitarget-directed ligands, BIGI 4b, BIGI 4d, and BIGI 5b were identified as promising new hit compounds showing in vitro balanced activities toward the recognized AD targets. In addition, these compounds showed suitable physicochemical properties and a good druglikeness score predicted by Data Warrior software.

Domaines

Chimie
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Dates et versions

hal-03969932 , version 1 (02-02-2023)

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Citer

Rim Malek, Alexey Simakov, Audrey Davis, Maciej Maj, Paul Bernard, et al.. Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca2+ Channel Blocking Ability, Cholinesterase Inhibition, Antioxidant Capacity, and Nrf2 Activation. Molecules, 2023, 28 (1), pp.71. ⟨10.3390/molecules28010071⟩. ⟨hal-03969932⟩
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