Anilide derivatives as monoamine oxidase inhibitors
Lesetja J. Legoabe
North-West University Unit for Drug Research and Development
Abstract:
A series of anilide derivatives were synthesized and evaluated as inhibitors of recombinant human monoamine oxidase B (MAO-B). The most potent inhibitors were (2E)-N-(3-chlorophenyl)-3-phenylprop-2-enamide and (2E)-N-(3-bromophenyl)-3-phenylprop-2-enamide with IC50 values of 0.53 µM and 0.45 µM, respectively. These derivatives exhibited reversible and selective inhibition of MAO-B with binding affinities 37 fold higher for MAO-B than for recombinant human MAO-A. Based on modeling studies, phenolic and benzonitrile H-bond acceptors were introduced into the structure and their effects on MOA inhibition were evaluated.
