Next Article in Journal
Study on Lavender Essential Oil Chemical Compositions by GC-MS and Improved pGC
Previous Article in Journal
10-Gingerol Targets Lipid Rafts Associated PI3K/Akt Signaling in Radio-Resistant Triple Negative Breast Cancer Cells
Previous Article in Special Issue
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

1
Laboratory of Research in Medicinal Chemistry (PeQuiM), Federal University of Alfenas, Jovino Fernandes Sales Avenue, 2600, Alfenas 37130000, MG, Brazil
2
Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d’Augusto 237, 47921 Rimini, Italy
3
Laboratory of Molecular Pharmacology, Federal University of Rio de Janeiro, Avenida Carlos Chagas Filho, 373, Rio de Janeiro 21941590, RJ, Brazil
4
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
5
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; https://doi.org/10.3390/molecules25143165
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
Show Figures

Figure 1

MDPI and ACS Style

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.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop