{Reference Type}: Journal Article
{Title}: Synthesis of novel hybrids of 1,2,3-triazoles-hydrazone: targeting cholinesterases and Alzheimer's related genes.
{Author}: Shareghi-Boroujeni D;Iraji A;Dara M;Hashempur MH;Zare S;Hariri R;Akbarzadeh T;Saeedi M;
{Journal}: Future Med Chem
{Volume}: 0
{Issue}: 0
{Year}: 2024 Jun 12
{Factor}: 4.767
{DOI}: 10.1080/17568919.2024.2359894
{Abstract}: Aim: A new series of 1,2,3-triazole-hydrazone derivatives were developed to evaluate their anti-Alzheimer's activity. Materials & methods: All compounds were screened toward cholinesterases via the modified Ellman's method. The toxicity assay on SH-SY5Y cells was performed using the MTT assay, and the expression levels of GSK-3α, GSK-3β, DYRK1 and CDK5 were assessed in the presence of compounds 6m and 6p. Results: 6m and 6p; acting as mixed-type inhibitors, exhibited promising acetylcholinesterase and butyrylcholinesterase inhibitory activity, respectively. 6m demonstrated no toxicity under tested concentrations on the SH-SY5Y cells and positively impacted neurodegenerative pathways. Notably, 6m displayed a significant downregulation in mRNA levels of GSK-3α, GSK-3β and CDK5. Conclusion: The target compounds could be considered in developing anti-Alzheimer's disease agents.<BR>[Box: see text].