Design, synthesis and in vivo evaluation of 1,4-dioxo-2-butenyl aryl amine derivatives as a promising anti-inflammatory drug prototype

Bioorganic Chemistry(2022)

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摘要
•Virtual screening provided 4 candidates potentially able to strongly inhibit COX isoenzymes in inflammatory process.•Compounds (1–4) reduced pain in the inflammatory phase response.•Compound 4 inhibited the involvement of PGs in the formation of paw edema.•Compounds 2 and 4 reduced the cellular recruitment of PMN to the inflammatory site.•Compounds 1, 3 and 4 reduced the neurogenic phase of pain.
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关键词
1,4-Dioxo-2-butenyl derivatives,Dipyrone,Analgesic effects,Anti-inflammatory effects,Docking
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