Research Article
Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme
Abstract
Alzheimer's disease is a neurological disease characterized by the destruction of brain cells. In this disease,
which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In
this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic
hypothesis, was studied. New 3(2H)pyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR,
HRMS analysis and their IC50 and Ki values were studied. The inhibition constants (Ki) of the compounds against
the AChE enzyme ranged from 2.35 ± 0.18 to 5.15 ± 0.46 μM. The compound with the best inhibitory properties was
compound 6d with a Ki value of 2.35 ± 0.18 μM. In addition, to support the experimental data, molecular docking studies
were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure (PDB ID:4M0E).
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There are 26 citations in total.
Details
| Primary Language | English |
|---|---|
| Subjects | Pharmaceutical Biochemistry, Pharmaceutical Chemistry |
| Journal Section | Articles |
| Authors | |
| Publication Date | June 28, 2025 |
| Published in Issue | Year 2022 Volume: 26 Issue: 5 |