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- Title
Design, Synthesis and Biological Evaluation of Novel Triazole N-acylhydrazone Hybrids for Alzheimer's Disease.
- Authors
de Freitas Silva, Matheus; Tardelli Lima, Ellen; Pruccoli, Letizia; Castro, Newton G.; Guimarães, Marcos Jorge R.; da Silva, Fernanda M. R.; Fonseca Nadur, Nathalia; de Azevedo, Luciana Luiz; Kümmerle, Arthur Eugen; Guedes, Isabella Alvim; Dardenne, Laurent Emmanuel; Gontijo, Vanessa Silva; Tarozzi, Andrea; Viegas, Claudio; Belluti, Federica
- Abstract
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.
- Subjects
BIOSYNTHESIS; ALZHEIMER'S disease; TACRINE; REACTIVE oxygen species; TRIAZOLES; MOLECULAR hybridization
- Publication
Molecules, 2020, Vol 25, Issue 14, p3165
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules25143165