Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors
| Author | Mehdi Valipour | en |
| Author | Issa Davaji | en |
| Author | Niusha Abedi | en |
| Author | Mahsa Rajabi | en |
| Author | Tuba Tüylü Küçükkılınç | en |
| Author | Beyza Ayazgök | en |
| Author | Hamid Irannejad | en |
| Issued Date | 2019-07-31 | en |
| Abstract | Alzheimer’s disease (AD) is a neuroinflammatory based pathologic state in which β-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 β-amyloid aggregation. Compounds 1-10b were synthesized through a two-step reaction. Results: Compounds 1-5b showed more β-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. | en |
| DOI | https://doi.org/10.22037/ijpr.2019.15567.13181 | en |
| Keyword | Synthesis | en |
| Keyword | Anti- inflammatory | en |
| Keyword | Alzheimer′s disease | en |
| Keyword | hydroxyiminoethanone | en |
| Keyword | β-amyloid aggregation | en |
| Publisher | Brieflands | en |
| Title | Synthesis and Biological Assessment of 2-Hydroxyiminoethanones as Anti-Inflammatory and β-Amyloid Aggregation Inhibitors | en |
| Type | Original Article | en |
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