Alzheimer's disease (AD) is a prevalent neurodegenerative disorder among the elderly, and there are currently no effective treatment options available. Selective inhibition of butyrylcholinesterase (BuChE) has emerged as a promising strategy for AD therapeutics. In this study, we identified compound 6a as a lead candidate derived from the structural modification of rivastigmine. Our findings indicated that 6a acts as a potent selective BuChE inhibitor, demonstrating an IC