Discovery of monoamine oxidase inhibitors by medicinal chemistry approaches.

Neuropsychiatric disorders, such as Alzheimer's disease (AD), Parkinson's disease (PD) and depression, have seriously inconvenienced the lives of patients. Growing evidence indicates that these diseases are closely related to the monoamine oxidase (MAO) enzyme, making it an attractive target for the exploitation of potent MAO inhibitors (MAOIs) with high selectivity and low side effects. Although various MAOIs have been discovered, the discovery of an ideal MAOI is not an easy task. In this review, we discuss the currently available rational design strategies for obtaining ideal MAOIs, including ligand-based and receptor-based design strategies, and these strategies were further illustrated with the aid of specific examples from the recent literature. To better understanding the biological activity of MAO, we also highlight the binding modes of typical inhibitors against MAO. Besides, advanced strategies for finding upcoming potent MAOIs were prospected.