Investigation of the monoamine oxidase inhibition properties of benzoxathiolone derivatives

Abstract The treatment of neuropsychiatric and neurodegenerative disorders such as depression Parkinson’s disease represent significant challenges in healthcare. Enzymes that metabolise neurotransmitter amines are important drug targets for these inhibitors enzymes have played key roles therapeutic agents. For example, monoamine oxidase (MAO) A been used decades antidepressant agents act by inhibiting the central metabolism serotonin noradrenaline, while MAO-B conserve dopamine supply to treat disease. Literature reports benzoxathiolone derivatives potent MAO with specificity isoform. To expand on findings, present study synthesised series investigated their human inhibition properties. results showed were inhibitors, most compounds exhibiting IC 50 values 0.083 0.086 µM ( 4d 5e ) 0.0069 0.0066 3a 3b MAO-A MAO-B, respectively. Compounds significantly more compared those reported previously. It may be concluded derived future leads development new treatments Graphical