Multi-target 1,4-dihydropyridines showing calcium channel blockade and antioxidant capacity for Alzheimer's disease therapy.

Bioorg Chem

Neurosciences Intégratives et Cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Univ. Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, F-25000 Besançon, France. Electronic address:

Published: October 2019

AI Article Synopsis

  • The study focuses on synthesizing new compounds called 1,4-dihydropyridines (DHPs) that combine features of melatonin and nimodipine to address multiple targets.
  • One of the compounds, DHP 7, showed significant calcium channel blocking ability at 55% and strong antioxidant properties equivalent to 8.78 Trolox equivalents.
  • DHP 7 is highlighted as a promising candidate for potential Alzheimer's disease therapy due to its balanced profile of effects.

Article Abstract

In this work we describe the synthesis, Ca channel blockade capacity and antioxidant power of N,N-bis(2-(5-methoxy-1H-indol-3-yl)ethyl)-2,6-dimethyl-4-aryl-1,4-dihydropyridine-3,5-dicarboxamides 1-9, a number of multi-target small 1,4-dihydropyridines (DHP), designed by juxtaposition of melatonin and nimodipine. As a result, we have identified antioxidant DHP 7 (Ca channel blockade: 55%, and 8.78 Trolox/Equivalents), the most balanced DHP analyzed here, for potential Alzheimer's disease therapy.

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Source
http://dx.doi.org/10.1016/j.bioorg.2019.103205DOI Listing

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