Synthesis and cholinesterase inhibitory activity of some phenylacetamide derivatives bearing 1H-pyrazole or 1H-1,2,4-triazole

Abstract

A group of N-phenylacetamide derivatives bearing five membered heterocyclic rings, pyrazole or 1,2,4-triazole, were synthesized to investigate their cholinesterase inhibitory activities. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities were evaluated by using Ellman’s spectroscopic method. Results indicated that all of the compounds displayed moderate and selective AChE inhibitory activity and the most active compound was 2-(1H-1,2,4-triazole-1-yl)-N-(3-methoxyphenyl)acetamide with an IC50 value of 6.68 mM. Docking studies were also carried out for the most active compound.

Keywords

• Alzheimer’s disease
• pyrazole
• 1
• 2
• 4-triazole
• acetamide
• cholinesterase inhibitory activity

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