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Título: | Design, synthesis and biological evaluation of new antioxidant and neuroprotective multitarget directed ligands able to block calcium channels |
Autor: | Pachòn Angona, Irene; Daniel, Solene; Martin, Hélène; Bonet, Alexandre; Wnorowski, Artur; Maj, Maciej; Jóźwiak, Krzysztof; Silva, Tiago Barros; Refouvelet, Bernard; Borges, Fernanda; Marco-Contelles, José CSIC ORCID; Ismaili, Lhassane | Palabras clave: | Alzheimer’s disease Ca2+ channel antagonists Hantzsch reaction multitarget directed ligands Neuroprotection oxidative stress |
Fecha de publicación: | 14-mar-2020 | Editor: | Multidisciplinary Digital Publishing Institute | Citación: | Molecules 25(6): 1329 (2020) | Resumen: | 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. | Versión del editor: | https://doi.org/10.3390/molecules25061329 | URI: | http://hdl.handle.net/10261/205638 | DOI: | 10.3390/molecules25061329 | E-ISSN: | 1420-3049 |
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antioxidant_neuroprotective_ligands_calcium.pdf | 7,06 MB | Adobe PDF | Visualizar/Abrir |
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