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Design, Synthesis and Biological Evaluation of Novel Triazole N-acylhydrazone Hybrids for Alzheimer’s Disease

2020; Multidisciplinary Digital Publishing Institute; Volume: 25; Issue: 14 Linguagem: Inglês

10.3390/molecules25143165

1433-1373

Matheus de Freitas Silva, Ellen Tardelli Faleiros Lima, Letizia Pruccoli, Newton G. Castro, Marcos Jorge R. Guimarães, Fernanda da Silva, Nathália Fonseca Nadur, Luciana de Azevedo, Arthur Eugen Kümmerle, Isabella Alvim Guedes, Laurent E. Dardenne, Vanessa Silva Gontijo, Andrea Tarozzi, Cláudio Viegas,

Alzheimer's disease research and treatments

Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder that involves different pathogenic mechanisms. In this regard, the goal of this study was the design and synthesis of new compounds with multifunctional pharmacological activity by molecular hybridization of structural fragments of curcumin and resveratrol connected by an N-acyl-hydrazone function linked to a 1,4-disubstituted triazole system. Among these hybrid compounds, derivative 3e showed the ability to inhibit acetylcholinesterase activity, the intracellular formation of reactive oxygen species as well as the neurotoxicity elicited by Aβ42 oligomers in neuronal SH-SY5Y cells. In parallel, compound 3e showed a good profile of safety and ADME parameters. Taken together, these results suggest that 3e could be considered a lead compound for the further development of AD therapeutics.