Review of β‐carboline and its derivatives as selective MAO‐A inhibitors

As flavin adenine dinucleotide (FAD)‐dependent enzymes, monoamine oxidases (MAOs) catalyze the oxidative deamination of various endogenous and exogenous amines. MAO‐A inhibitors are thought to be effective therapeutic agents for treating neurological diseases including depression and anxiety. Due to the academic challenge of developing new human (h) MAO‐A inhibitors and the potential for discovering substances with remarkable properties compared to existing MAO‐A inhibitors, numerous research groups are looking into novel classes of chemical compounds that may function as selective hMAO‐A inhibitors. β‐Carbolines are reported to be a prominent class of bioactive molecules exhibiting MAO‐A inhibition. Chemically, β‐carboline is a tricyclic pyrido‐3,4‐indole ring. It has only recently been discovered that this chemotype has highly effective and specific MAO‐A inhibitory activity. In this review, structure–activity relationship studies included in particular research publications from the 1960s to the present are discussed with regard to β‐carboline and its analogs. This comprehensive information helps to design and develop a new family of MAO‐A inhibitors for the management of depressive disorders. As flavin adenine dinucleotide‐dependent enzymes, monoamine oxidases (MAOs) catalyze the oxidative deamination of various endogenous and exogenous amines. This review discusses the structure–activity relationship studies reported in research publications from the 1960s to the present with regard to β‐carboline and its analogs. The provided information will help to design new MAO‐A inhibitors for the management of depressive disorders.