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A series of novel polar benzimidazoles were synthesized in a 4-step reaction starting from basic compound 4-fluoro-3-nitrobenzoic acid in good to excellent yield. The compounds generally fulfill the Lipinski’s rule of five to show their potential as drug lead compounds. The compounds were screened for their acetylcholinesterase (AChE) inhibitory activities and the most potent compound was found to be 5e which gave IC50 value of 31.04 μM. The structure of the novel polar benzimidazoles were characterized and confirmed by elemental and mass spectral analyses as well as 1H and 13C NMR spectroscopic data. All the compounds were found to be non-toxic when tested with VERO cells at 50 μM.