Discovery of talmapimod analogues as polypharmacological anti-inflammatory agents

Twenty novel talmapimod analogues were designed, synthesised and evaluated for the in vivo anti-inflammatory activities. Among them, compound 6n, the most potent one, was selected for exploring the mechanisms underlying its anti-inflammatory efficacy. In RAW264.7 cells, it effectively suppressed lip...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2020-01, Vol.35 (1), p.187-198
Hauptverfasser:	Liu, Wandong, Hou, Caiyun, Li, Jiaming, Ma, Xiaodong, Zhang, Yanchun, Hu, Mengqi, Huang, Yuanzheng
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals anti-inflammation Anti-inflammatory agents Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology COXs Cyclooxygenase 2 - metabolism Cyclooxygenase-2 Disease Models, Animal Dose-Response Relationship, Drug Drug Discovery Inflammation Inflammatory diseases Kinases Lipopolysaccharides Lipopolysaccharides - antagonists & inhibitors Lipopolysaccharides - pharmacology Male MAP kinase Mice Mice, Inbred ICR Molecular Structure NF-kappa B - antagonists & inhibitors NF-kappa B - metabolism NF-κB protein Nitric Oxide Synthase Type II - antagonists & inhibitors Nitric Oxide Synthase Type II - metabolism Nitric-oxide synthase p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors p38 Mitogen-Activated Protein Kinases - metabolism p38α MAPK Pharmaceutical sciences Pharmacy Phosphorylation Polypharmacological agent RAW 264.7 Cells Research Paper Signal transduction Signal Transduction - drug effects Structure-Activity Relationship talmapimod analogues
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