2-(3-Aryl-1-phenyl-1H-pyrazol-4-yl) methylene amino) alkanoic acid: Synthesis, anticholinesterase evaluation and molecular modeling studies

Ashwani Kumar*, Sandeep Jain a

Abstract

A new series of 1-phenyl-3-aryl-1H-pyrazole derivatives was synthesized and evaluated as potential acetylcholinesterase (AChE) inhibitors against Alzheimer’s disease (AD). Most of the compounds exhibited moderate to good inhibitory potency. Specifically, the compound 3f was found to be strongest inhibitor at 0.89 μM concentration (IC50 value). Further docking calculations were performed in order to understand the binding mode between the most active compound and the active site of the cholinesterase enzyme.