Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and ?-Amyloid Aggregation Inhibitors.

ABSTRACT: Alzheimer's disease (AD) is a neuroinflammatory based pathologic state in which ?-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 ?-amyloid aggregation. Compounds 1-10b were synthesized through a two-step reaction. Results: Compounds 1-5b showed more ?-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.

SUBMITTER: Valipour M 

PROVIDER: S-EPMC6934981 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature