Biological activity evaluation of novel monoamine oxidase inhibitory compounds targeting Parkinson disease

Abstract

Aim: Design of 5-methoxy benzofuran hybrids with 2-carbohydrazide and 2-(1,3,4-oxadiazol-2-yl) as potential inhibitors of monoamine oxidase (MAO)-B targeting Parkinson disease. Materials and methods: 12 compounds were synthesized and analyzed via high-resolution mass spectrometry, H-1 nuclear magnetic resonance and C-13 nuclear magnetic resonance techniques. In vitro fluorometric assay was used to investigate the activity of the synthesized compounds on both MAO-A and MAO-B isozymes. Results: Three compounds - 3a, 3c and 3e - displayed half maximal inhibitory concentration values of 0.051 +/- 0.002, 0.038 +/- 0.001 and 0.077 +/- 0.003 mu M in the inhibition of MAO-A and 0.048 +/- 0.002, 0.040 +/- 0.001 and 0.072 +/- 0.002 mu M for MAO-B, respectively. A molecular dynamics simulation study showed that compound 3c has poor stability as a complex with MAO-A. Conclusion: Compound 3c may be a potential candidate for the treatment of Parkinson disease.