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


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 ?M), showing significant neuroprotection (38%) against H2O2 at 10 ?M, being considered thus a hit-compound for further investigation in our search for anti-Alzheimer's disease agents.

SUBMITTER: Pachon Angona I 

PROVIDER: S-EPMC7144121 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature

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

Pachòn Angona Irene I   Daniel Solene S   Martin Helene H   Bonet Alexandre A   Wnorowski Artur A   Maj Maciej M   Jóźwiak Krzysztof K   Silva Tiago Barros TB   Refouvelet Bernard B   Borges Fernanda F   Marco-Contelles José J   Ismaili Lhassane L  

Molecules (Basel, Switzerland) 20200314 6


We report herein the design, synthesis and biological evaluation of new antioxidant and neuroprotective multitarget directed ligands (MTDLs) able to block Ca<sup>2+</sup> channels. New dialkyl 2,6-dimethyl-4-(4-(prop-2-yn-1-yloxy)phenyl)-1,4-dihydropyridine-3,5-dicarboxylate MTDLs <b>3a</b>-<b>t</b>, resulting from the juxtaposition of nimodipine, a Ca<sup>2+</sup> channel antagonist, and rasagiline, a known MAO inhibitor, have been obtained from appropriate and commercially available precursors  ...[more]

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