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

Dawbaa S., Evren A. E., Sağlık B. N., Gündoğdu-Karaburun N., Karaburun A. Ç.

FUTURE MEDICINAL CHEMISTRY, vol.14, no.22, pp.1663-1679, 2022 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 14 Issue: 22
  • Publication Date: 2022
  • Doi Number: 10.4155/fmc-2022-0167
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Chemical Abstracts Core, EMBASE, MEDLINE
  • Page Numbers: pp.1663-1679
  • Keywords: benzofuran, carbohydrazide, molecular docking, molecular dynamics simulation, monoamine oxidase inhibitors, oxadiazol, Parkinson disease, DYNAMICS
  • Anadolu University Affiliated: Yes


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.