Synthesis of novel hybrids of 1,2,3-triazoles-hydrazone: targeting cholinesterases and Alzheimer's related genes.
Future Med Chem
; 16(15): 1519-1535, 2024 Aug 02.
Article
em En
| MEDLINE
| ID: mdl-38864182
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-3ß, 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-3ß and CDK5.Conclusion:
The target compounds could be considered in developing anti-Alzheimer's disease agents.
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Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Inibidores da Colinesterase
/
Quinase 5 Dependente de Ciclina
/
Doença de Alzheimer
/
Hidrazonas
Limite:
Humans
Idioma:
En
Revista:
Future Med Chem
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Irã