期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 32, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127720
关键词
Flavone; Fluorine; Neuroprotection; Antioxidant; NMR
资金
- National Institutes of Health (NIH)
- National Institute of General Medical Sciences [P20GM104932, P20GM130460]
- University of Hail, Saudi Arabia
The synthesis of flavones with fluorine substitutions has been reported, and their biological evaluation showed enhanced antioxidant activity and conserved neuroprotective activity compared to their non-fluorinated counterparts. Additionally, 3-fluoro-3',4',5'-trihydroxyflavone can serve as an NMR probe to detect structural changes during its action as a radical scavenger.
Flavones are valuable scaffolds in medicinal chemistry, especially as they display activity as antioxidants and neuroprotective agents. The need to incorporate a fluorine atom on flavones has driven much of the recent synthetic work in this area. We now report a route for the production of 3-fluorinated derivatives of 3',4',5'-trihydroxyflavone and 3',4',5'-trimethoxyflavone. Biological evaluation of these agents, along with their non fluorinated counterparts, demonstrate that antioxidant activity may be enhanced whereas neuroprotective activity is conserved. Also, the 3-fluoro-3',4',5'-trihydroxyflavone can act as an NMR probe to detect structural changes during its action as a radical scavenger.
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