Inhibiting human monoamine oxidase (MAO)-B to increase the availability of monoamine neurotransmitters is a clinically approved strategy for treating Parkinson’s disease, yet available inhibitors lack efficacy or increase risk of adverse events. Researchers at Hefei University of Technology and collaborators started from the clinically improved MAO-B inhibitor safinamide and generated various derivatives, among which [I] and [II] emerged as the most promising.