Keeping in view the biological significance of benzimidazole, pyrrole and piperidine moieties, in this study, we designed and synthesized hybrid scaffolds of benzimidazole-bearing pyrroles and piperidines as potential inhibitors of AChE and BuChE for the treatment of Alzheimer’s disease in the search for lead molecules, and the results obtained corroborated that these compounds could be considered as potential lead molecules for the development of improved AChE and BuChE inhibitors. The gene discussed is ACHE; the disease is early-onset autosomal dominant Alzheimer disease.