Coumarin versus Chromone Monoamine Oxidase B Inhibitors: Quo Vadis?

Because of the lack of significant
disease-modifying drugs for
neurodegenerative disorders, a pressing need for new chemical entities
endowed with IMAO-B still exists. Within this framework, and for the
first time, a study was performed to compare coumarin- and chomone-3-phenylcarboxamide
scaffolds. Compounds 10a and 10b were the
most potent, selective, and reversible noncompetitive IMAO-B. The
benzopyrone sp2 oxygen atom was found to be position independent
and a productive contributor for the ligand–enzyme complex
stability.