European Journal of Medicinal Chemistry p. 292 - 301 (2013)
Update date:2022-08-05
Topics:
Hu, Jie
Wang, Yi
Wei, Xiaoyan
Wu, Xixi
Chen, Gaozhi
Cao, Gaozhong
Shen, Xueqian
Zhang, Xiuhua
Tang, Qinqin
Liang, Guang
Li, Xiaokun
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.
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