This review is focused on the design, synthesis, bio-pharmacological evaluation, and data analysis of a large number of coumarin derivatives, mainly developed in our group, as monoamine oxidase (MAO), cholinesterase (ChE), and aromatase (AR) inhibitors, and as multitarget agents addressing neurodegenerative diseases (NDs). The gene discussed is BCHE; the disease is neurodegenerative disease.