| Title : Design, Synthesis and Biological Evaluation of Novel Triazole N-acylhydrazone Hybrids for Alzheimer's Disease - de Freitas Silva_2020_Molecules_25_ |
| Author(s) : de Freitas Silva M , Tardelli Lima E , Pruccoli L , Castro NG , Guimares MJR , F MRdS , Fonseca Nadur N , de Azevedo LL , Kummerle AE , Guedes IA , Dardenne LE , Gontijo VS , Tarozzi A , Viegas C |
| Ref : Molecules , 25 : , 2020 |
|
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 Abeta(42) 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. |
| PubMedSearch : de Freitas Silva_2020_Molecules_25_ |
| PubMedID: 32664425 |
de Freitas Silva M, Tardelli Lima E, Pruccoli L, Castro NG, Guimares MJR, F MRdS, Fonseca Nadur N, de Azevedo LL, Kummerle AE, Guedes IA, Dardenne LE, Gontijo VS, Tarozzi A, Viegas C (2020)
Design, Synthesis and Biological Evaluation of Novel Triazole N-acylhydrazone Hybrids for Alzheimer's Disease
Molecules
25 :
de Freitas Silva M, Tardelli Lima E, Pruccoli L, Castro NG, Guimares MJR, F MRdS, Fonseca Nadur N, de Azevedo LL, Kummerle AE, Guedes IA, Dardenne LE, Gontijo VS, Tarozzi A, Viegas C (2020)
Molecules
25 :