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Article Dans Une Revue Molecules Année : 2020

Design, Synthesis and Biological Evaluation of New Antioxidant and Neuroprotective Multitarget Directed Ligands Able to Block Calcium Channels

Irene Pachòn Angona
  • Fonction : Auteur
Solene Daniel
  • Fonction : Auteur
Helene Martin
  • Fonction : Auteur
Alexandre Bonet
  • Fonction : Auteur
Artur Wnorowski
Maciej Maj
Krzysztof Jóźwiak
Tiago Barros Silva
  • Fonction : Auteur
Bernard Refouvelet
  • Fonction : Auteur
Fernanda Borges
José Marco-Contelles

Résumé

We report herein the design, synthesis and biological evaluation of new antioxidant and neuroprotective multitarget directed ligands (MTDLs) able to block Ca2+ channels. New dialkyl 2,6-dimethyl-4-(4-(prop-2-yn-1-yloxy)phenyl)-1,4-dihydropyridine-3,5-dicarboxylate MTDLs 3a–t, resulting from the juxtaposition of nimodipine, a Ca2+ channel antagonist, and rasagiline, a known MAO inhibitor, have been obtained from appropriate and commercially available precursors using a Hantzsch reaction. Pertinent biological analysis has prompted us to identify the MTDL 3,5-dimethyl-2,6–dimethyl–4-[4-(prop–2–yn–1-yloxy)phenyl]-1,4-dihydro- pyridine- 3,5-dicarboxylate (3a), as an attractive antioxidant (1.75 TE), Ca2+ channel antagonist (46.95% at 10 μM), showing significant neuroprotection (38%) against H2O2 at 10 μM, being considered thus a hit-compound for further investigation in our search for anti-Alzheimer’s disease agents.

Dates et versions

hal-03654614 , version 1 (28-04-2022)

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Citer

Irene Pachòn Angona, Solene Daniel, Helene Martin, Alexandre Bonet, Artur Wnorowski, et al.. Design, Synthesis and Biological Evaluation of New Antioxidant and Neuroprotective Multitarget Directed Ligands Able to Block Calcium Channels. Molecules, 2020, 25 (6), pp.1329. ⟨10.3390/molecules25061329⟩. ⟨hal-03654614⟩

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