ChemInform Abstract: Inhibition of Monoamine Oxidase Types A and B by 2‐Aryl‐4H‐1,3,4‐oxadiazin‐5(6H)‐one Derivatives.

Abstract

ChemInform Abstract Monoamine oxidase (MAO) is responsible for the metabolic inactivation of amine neurotransmitters such as serotonin and dopamine. The title compounds of type (III) and (VI) are tested in vitro for their inhibitory effects on MAO A and MAO B. (IIIa) and (IIIb) with hydrophobic and electron-withdrawing R1 substituent, resp., inhibit MAO B, while (IIIc) are more active on MAO A. Replacement of the (CH2)2-CN moiety in (III) by the substituent R2 leads to the less active derivatives (VI). Introduction of a 6-methyl group into (Ib) decreases the inhibitor potency on MAO B.