تجاوز إلى المحتوى الرئيسي

[3 + 2] Cycloaddition Synthesis of New (Chromene-1,3,4-Oxadiazole) Hybrids Linked to Pyrazole Units as Potential Acetylcholinesterase Inhibitors

Author name : AHMED ABDELHAMID MOHAMED AHMED
Publication Date : 2025-01-15
Journal Name : ChemistrySelect

Abstract

A lot of interest has been gained recently in developing novel acetylcholinesterase (AChE) inhibitors that can alleviate Alzheimer's symptoms. In the current study, we aimed to explore AChE inhibitory activity of new chromenes attached to 1,3,4-oxadiazole and/or pyrazole units. The new hybrids were obtained via [3 + 2] cycloaddition reaction between the appropriate chromene-based enaminones and hydrazonyl chlorides. The inhibition percentages of the new products against AChE were recorded at tested concentrations of 15 and 25 µM compared to donepezil. 3-(3-Acetyl-1-(4-methoxyphenyl)-1H-pyrazole-4-carbonyl)-6-(((5-phenyl-1,3,4-oxadiazol-2-yl)thio)methyl)-2H-chromen-2-one displayed promising activity with inhibition percentages of 73.2 and 87.3, respectively, at the aforementioned concentrations. Moreover, the previous hybrid gave promising 2,2-diphenylpicrylhydrazyl (DPPH) inhibitory activity using the reference ascorbic acid. It had an inhibition percentage of 86.6 at a tested concentration of 25 µM.

Keywords

acetylcholinesterase (AChE) inhibitors- Alzheimer's symptoms- [3 + 2] cycloaddition reaction

Publication Link

https://doi.org/10.1002/slct.202404804

Block_researches_list_suggestions

Suggestions to read

HIDS-IoMT: A Deep Learning-Based Intelligent Intrusion Detection System for the Internet of Medical Things
Ahlem . Harchy Ep Berguiga
Generalized first approximation Matsumoto metric
AMR SOLIMAN MAHMOUD HASSAN
Structure–Performance Relationship of Novel Azo-Salicylaldehyde Disperse Dyes: Dyeing Optimization and Theoretical Insights
EBTSAM KHALEFAH H ALENEZY
“Synthesis and Characterization of SnO₂/α-Fe₂O₃, In₂O₃/α-Fe₂O₃, and ZnO/α-Fe₂O₃ Thin Films: Photocatalytic and Antibacterial Applications”
Asma Arfaoui
تواصل معنا