Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents
Synthesis and biological evaluation of novel thiazolidinone derivatives as potential anti-inflammatory agents
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作为潜在抗炎剂的新型噻唑烷酮衍生物的合成和生物学评价
DOI：
10.1016/j.ejmech.2013.04.010
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发表时间：
2013-06-01
影响因子：
6.7
通讯作者：
Li, Xiaokun
中科院分区：
文献类型：
--
作者：
Hu, Jie;Wang, Yi;Li, Xiaokun
促炎症细胞因子的调节为控制炎症性疾病提供了一个靶点，在当前的抗炎药物开发中备受关注。本文合成了四个系列的噻唑烷酮类化合物，并对其抗炎活性进行了筛选。其中大部分化合物对脂多糖刺激的巨噬细胞表达的肿瘤坏死因子-α和白介素6有很好的抑制作用。对结构活动关系进行了讨论。化合物12d和12h以剂量依赖方式抑制内毒素诱导的肿瘤坏死因子-α和白介素6的释放。此外，12d对脂多糖诱导的小鼠脓毒症死亡有明显的保护作用。综上所述，这些数据提供了一系列新的噻唑烷酮类化合物，它们对急性炎症性疾病具有潜在的治疗效果，并可能成为持续抗炎药物研究的重要线索。(C)2013年爱思唯尔·马森公司。版权所有。
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-alpha and IL-6 in LPS-stimulated macrophages. Discussions are given regarding the structure activity relationships. Compounds 12d and 12h inhibited LPS-induced TNF-alpha 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. (C) 2013 Elsevier Masson SAS. All rights reserved.