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Novel 2-Thiouracil-5-Sulfonamide Derivatives: Design, Synthesis, Molecular Docking, and Biological Evaluation as Antioxidants with 15-LOX Inhibition. | LitMetric

New antioxidant agents are urgently required to combat oxidative stress, which is linked to the emergence of serious diseases. In an effort to discover potent antioxidant agents, a novel series of 2-thiouracil-5-sulfonamides (-) were designed and synthesized. In line with this approach, our target new compounds were prepared from methyl ketone derivative , which was used as a blocking unit for further synthesis of a novel series of chalcone derivatives -, thiosemicarbazone derivatives -, pyridine derivatives - and -, bromo acetyl derivative , and thiazole derivatives -. All compounds were evaluated as antioxidants against 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydrogen peroxide (HO), lipid peroxidation, and 15-lipoxygenase (15-LOX) inhibition activity. Compounds , , , , , and demonstrated significant RSA in all three techniques in comparison with ascorbic acid and 15-LOX inhibitory effectiveness using quercetin as a standard. Molecular docking of compound endorsed its proper binding at the active site pocket of the human 15-LOX which explains its potent antioxidant activity in comparison with standard ascorbic acid.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9963659PMC
http://dx.doi.org/10.3390/molecules28041925DOI Listing

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