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Evaluation of the Antioxidant and Neuroprotectant Activities of New Asymmetrical 1,3-Diketones. | LitMetric

A series of fourteen new asymmetrical 1,3-diketone derivatives have been synthesized and evaluated in the ABTS, FRAP and DPPH assays as a new chemotype with antioxidant and drug-like properties. All the compounds displayed low cytotoxicity in comparison to curcumin against the human neuroblastoma SH-SY5Y cell line. Among them, (3,5)-6-(2,5-difluoro-4-hydroxy-phenyl)-1,1,1-trifluoro-4-hydroxyhexa-3,5-dien-2-one () and (3,5)-6-(2,3-difluoro-4-hydroxy-phenyl)-1,1,1-trifluoro-4-hydroxyhexa-3,5-dien-2-one () with excellent solubility and chemical stability in biorelevant media, have also shown a similar Fe chelation behavior to that of curcumin. Additionally, both derivatives and have afforded good neuroprotection activity against H₂O₂ induced oxidative stress in the same neuronal cell line, with a significant reduction of intracellular ROS levels, in parallel with a good recovery of the Mitochondrial Membrane Potential (ΔΨ). Compounds and with a promising antioxidant and drug-like profile, with low cytotoxic and good neuroprotectant activity, constitute a new interesting chemical class with high potential as new therapeutic agents against neurodegenerative diseases.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222706PMC
http://dx.doi.org/10.3390/molecules23081837DOI Listing

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