Journal
MOLECULES
Volume 25, Issue 6, Pages -Publisher
MDPI
DOI: 10.3390/molecules25061329
Keywords
Alzheimer's disease; Ca2+ channel antagonists; Hantzsch reaction; multitarget directed ligands; neuroprotection; oxidative stress
Funding
- Regional Council of Franche-Comte [2016YC-04540, 04560]
- Foundation for Science and Technology (FCT)
- FEDER/COMPETE [UID/QUI/00081/2020, PTDC/MED-QUI/29164/2017, SFRH/BPD/114945/2016]
- Fundação para a Ciência e a Tecnologia [PTDC/MED-QUI/29164/2017, SFRH/BPD/114945/2016] Funding Source: FCT
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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 mu M), showing significant neuroprotection (38%) against H2O2 at 10 mu M, being considered thus a hit-compound for further investigation in our search for anti-Alzheimer's disease agents.
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