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Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents.
|Title||Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents.|
|Publication Type||Journal Article|
|Year of Publication||2013|
|Authors||Hu J, Wang Y, Wei X, Wu X, Chen G, Cao G, Shen X, Zhang X, Tang Q, Liang G, Li X|
|Journal||European journal of medicinal chemistry|
|Date Published||2013 Jun|
The modulation of pro-inflammatory cytokines provides a target for controlling inflammatory diseases and attracts much attention in current anti-inflammatory drug development. Here, four series of thiazolidinone derivatives were synthesized and screened for anti-inflammatory activities. A majority of these compounds showed excellent inhibition on the expression of TNF-α and IL-6 in LPS-stimulated macrophages. Discussions are given regarding the structure-activity relationships. Compounds 12d and 12h inhibited LPS-induced TNF-α and IL-6 release in a dose-dependent manner. Furthermore, 12d exhibited a significant protection against LPS-induced septic death in mouse model. Together, these data present a series of new thiazolidinones with potential therapeutic effects in acute inflammatory diseases and they could be important leads in the continuing anti-inflammatory drug research.
|Alternate Journal||Eur J Med Chem|