Design, Synthesis and Anti-Inflammatory Evaluation of Novel 5-Benzylidene-3,4-Dihalo-Furan-2-One Derivatives

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作者：Wang, F., Sun, J. R., Huang, M. Y., Wang, H. Y., Sun, P. H., Lin, J. & Chen, W. M.
期刊：European journal of medicinal chemistry 72, 35-45 (2014)
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Rosiglitazone has shown promising anti-inflammation effect. To develop preferable anti-inflammatory agents, twenty-two rosiglitazone analogs were synthesized and their anti-inflammatory activity was evaluated. Among these compounds, 6i and 6k displayed excellent inhibitory activities on the production of inflammatory mediators, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Furthermore, 6i and 6k showed suppression effects on the nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways, and this suppression effects could be partially reversed by GW9662, which is a peroxisome proliferator-activated receptor γ (PPARγ) antagonist. Additionally, our docking results exhibited the well combination of 6i and 6k to PPARγ. So the anti-inflammation activity of 6i and 6k was due at least in part, to their interaction with PPARγ.