《Design, synthesis and biological evaluation of novel triazole N-acylhydrazone hybrids for alzheimer’s disease》 was written by de Freitas Silva, Mathesus; Lima, Ellen Tardelli; Pruccoli, Letizia; Castro, Newton G.; Guimaraes, Marcos Jorge R.; da Silva, Fernanda M. R.; Nadur, Nathalia Fonseca; Luiz de Azevedo, Luciana; Kummerle, Arthur Eugen; Guedes, Isabella Alvim; Dardenne, Laurent Emmanuel; Gontijo, Vanessa Silva; Tarozzi, Andrea; Viegas, Claudio Jr.. COA of Formula: C7H6O3This research focused ontriazole acylhydrazone hybrid preparation diastereoselective antialzheimer cholinesterase inhibitor docking; pharmacokinetic antioxidant neurotoxicity triazole acylhydrazone hybrid; Alzheimer’s disease; curcumin; molecular hybridization; resveratrol. The article conveys some information:
The goal of this study was the design and synthesis of novel triazole N-acylhydrazone hybrids I [R1 = H, OH, OMe; R2 = H, F, 1-piperidyl, etc.; R3 = H, OH, OMe, F, Cl; R4 = H, F, Cl] with multifunctional pharmacol. activity by mol. 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, compound I [R1 = OMe, R2 = OH, R3 = R4 = H (II)] 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 II showed a good profile of safety and ADME parameters. Taken together, these results suggested that compound II could be considered a lead compound for the further development of AD therapeutics. The results came from multiple reactions, including the reaction of 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8COA of Formula: C7H6O3)
3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is a building block. It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities.COA of Formula: C7H6O3
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