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

Abstract

A group of N-phenylacetamide derivatives bearing five
\nmembered heterocyclic rings, pyrazole or 1,2,4-triazole,
\nwere synthesized to investigate their cholinesterase
\ninhibitory activities. Acetylcholinesterase (AChE) and
\nbutyrylcholinesterase (BuChE) inhibitory activities were
\nevaluated by using Ellman’s spectroscopic method. Results
\nindicated that all of the compounds displayed moderate and
\nselective AChE inhibitory activity and the most active compound
\nwas 2-(1H-1,2,4-triazole-1-yl)-N-(3-methoxyphenyl)acetamide
\nwith an IC50 value of 6.68 mM. Docking studies were also carried
\nout for the most active compound