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Wiley-VCH Verlag, ChemInform, 30(39), 2008

DOI: 10.1002/chin.200830142

Elsevier, European Journal of Medicinal Chemistry, 3(43), p. 668-674

DOI: 10.1016/j.ejmech.2007.06.001

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Synthesis of 6-amino-1,4-dihydropyridines that prevent calcium overload and neuronal death

This paper is available in a repository.
This paper is available in a repository.

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Abstract

The synthesis and pharmacology of 6-amino-1,4-dihydropyridines, such as ethyl 6-amino-4-aryl-5-cyano-1,4-dihydro-2-methyl-3-pyridinecarboxylic acids (3-16) and 2-amino-4-aryl-7,7-dimethyl-5-oxo-1,4,5,6,7,8-hexahydro-3-quinolinenitriles (17-21) are described. Compounds 18 and 21, at the concentration of 0.3 microM, proved to be the best blockers of the [Ca(2+)] overload induced by depolarization with high [K(+)] of SH-SY5Y neuroblastoma cells, with values of 63.8% and 50.4%, respectively. Most of the compounds induced a remarkable neuroprotective effect against toxicity caused by high [K(+)]-elicited [Ca(2+)] overload, and against H(2)O(2)-generated free radicals, in SH-SY5Y cells.