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MDPI, Molecules, 1(28), p. 71, 2022

DOI: 10.3390/molecules28010071

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

Journal article published in 2022 by Rim Malek, Alexey Simakov, Audrey Davis ORCID, Maciej Maj, Paul J. Bernard, Artur Wnorowski ORCID, Helene Martin ORCID, José Marco-Contelles, Fakher Chabchoub, Patrick Dallemagne ORCID, Christophe Rochais ORCID, Krzysztof Jozwiak ORCID, Lhassane Ismaili ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

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.