Cholinesterase inhibition is the only current validated target in clinics in the treatment of Alzheimer's disease (AD). Therefore, there is continuous interest in the development and discovery of novel cholinesterase inhibitory molecules. Coumarins, beside their employment in other pharmacological groups, have also attracted attention to be utilized in cholinesterase inhibitory molecule discovery and development. Numerous studies so far indicated the natural and synthetic coumarin analogues that have the potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes. Since the pathophysiology of AD is highly complex and, in particular, monoamine oxidase (MAO) inhibitors are also utilized in clinic for disease symptoms, coumarin analogues, either natural or synthetic, that have the potential to inhibit cholinesterase or MAO enzymes are summarized within this review.