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Curcumin-1,2,3-Triazole Conjugation for Targeting the Cancer Apoptosis Machinery
Open AccessArticle

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

Laboratory of Research in Medicinal Chemistry (PeQuiM), Federal University of Alfenas, Jovino Fernandes Sales Avenue, 2600, Alfenas 37130000, MG, Brazil
Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d’Augusto 237, 47921 Rimini, Italy
Laboratory of Molecular Pharmacology, Federal University of Rio de Janeiro, Avenida Carlos Chagas Filho, 373, Rio de Janeiro 21941590, RJ, Brazil
Laboratory of Molecular Diversity and Medicinal Chemistry (LaDMol-QM), Federal Rural University of Rio de Janeiro—UFRRJ, BR-465, Km 7 Seropédica-Rio de Janeiro 23890000, RJ, Brazil
Grupo de Modelagem Molecular em Sistemas Biológicos (GMMSB), National Laboratory for Scientific Computing—LNCC, Avenida Getúlio Vargas, 333, Petrópolis 25651-076, RJ, Brazil
Authors to whom correspondence should be addressed.
Academic Editor: Federica Belluti
Molecules 2020, 25(14), 3165;
Received: 5 June 2020 / Revised: 6 July 2020 / Accepted: 9 July 2020 / Published: 10 July 2020
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. View Full-Text
Keywords: molecular hybridization; Alzheimer’s disease; curcumin; resveratrol molecular hybridization; Alzheimer’s disease; curcumin; resveratrol
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de Freitas Silva, M.; Tardelli Lima, E.; Pruccoli, L.; Castro, N.G.; Guimarães, M.J.R.; da Silva, F.M.R.; Fonseca Nadur, N.; de Azevedo, L.L.; Kümmerle, A.E.; Guedes, I.A.; Dardenne, L.E.; Gontijo, V.S.; Tarozzi, A.; Viegas, C. Design, Synthesis and Biological Evaluation of Novel Triazole N-acylhydrazone Hybrids for Alzheimer’s Disease. Molecules 2020, 25, 3165.

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