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Synthesis of Novel Hybrids of 1,2,3-Triazoles-Hydrazone: Targeting Cholinesterases and Alzheimer's Related Genes Publisher Pubmed



D Shareghiboroujeni DIBA ; A Iraji AIDA ; M Dara MAHINTAJ ; Mh Hashempur Mohammad HASHEM ; S Zare SHAHROKH ; R Hariri ROSHANAK ; T Akbarzadeh TAHMINEH ; M Saeedi MINA
Authors

Source: Future Medicinal Chemistry Published:2024


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. © 2024 Elsevier B.V., All rights reserved.
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