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- Title
Design, Synthesis and Biological Evaluation of New Antioxidant and Neuroprotective Multitarget Directed Ligands Able to Block Calcium Channels.
- Authors
Pachòn Angona, Irene; Daniel, Solene; Martin, Helene; Bonet, Alexandre; Wnorowski, Artur; Maj, Maciej; Jóźwiak, Krzysztof; Silva, Tiago Barros; Refouvelet, Bernard; Borges, Fernanda; Marco-Contelles, José; Ismaili, Lhassane; Romanelli, Maria Novella; Dei, Silvia
- Abstract
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.
- Subjects
BIOSYNTHESIS; CALCIUM channels; LIGANDS (Biochemistry); TELLURIUM compounds; SODIUM channels; ANTIOXIDANTS
- Publication
Molecules, 2020, Vol 25, Issue 6, p1329
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules25061329