Synthesis and biological assessment of 2-hydroxyiminoethanones as anti-inflammatory and β-amyloid aggregation inhibitors


Valipour M., Davaji I., Abedi N., Rajabi M., Kucukkilinc T. T. , AYAZGÖK B. , ...Daha Fazla

Iranian Journal of Pharmaceutical Research, cilt.18, ss.1288-1298, 2019 (SCI Expanded İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 18 Konu: 3
  • Basım Tarihi: 2019
  • Doi Numarası: 10.22037/ijpr.2019.15567.13181
  • Dergi Adı: Iranian Journal of Pharmaceutical Research
  • Sayfa Sayıları: ss.1288-1298

Özet

Alzheimer's disease (AD) is a neuroinflammatory based pathologic state in which beta-amyloid aggregates are major devastating agents. In this study, a series of 2-hydroxyiminoethanones were synthesized and evaluated as anti-inflammatory in carrageenan and formalin tests and inhibitors of beta-amyloid aggregation. Compounds 1-10b were synthesized through a two-step reaction. Results: Compounds 1-5b showed more beta-amyloid disaggregation ability than reference drugs rifampicin and donepezil and compound 2b was the best compound in this series and could reduce the extent of amyloid aggregation to 50.9%. Interestingly, compounds 1b and 3b showed significant anti-inflammatory activity in carrageenan-induced paw edema compared to control group and equivalent to the reference drug indomethacin. 2-Hydeoxyiminoethanones are privileged scaffold for further drug research and development as anti-neuroinflammatory and neuroprotective agents.