Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives
Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives
复制标题
新型苯并咪唑和咪唑并吡啶衍生物的合成及抗炎评价
DOI：
10.1021/ml300282t
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发表时间：
2013-01-01
影响因子：
4.2
通讯作者：
Liang, Guang
中科院分区：
文献类型：
--
作者：
Chen, Gaozhi;Liu, Zhiguo;Liang, Guang
脓毒症是一种急性炎症性疾病，仍然是重症监护病房最常见的死亡原因。合成了一系列苯并咪唑和咪唑并吡啶衍生物并进行了抗炎活性筛选，咪唑并吡啶系列显示出优异的抑制LPS刺激的巨噬细胞中炎性细胞因子的表达。化合物X10、X12、X13、X14和X15以剂量依赖性方式抑制TNF-α和IL-6的释放，并且X12在肝细胞中没有显示出细胞毒性。此外，X12在小鼠模型中对脂多糖诱导的脓毒性死亡表现出显着的保护作用。总之，这些数据提出了一系列新的咪唑并吡啶类化合物，在急性炎症性疾病中具有潜在的治疗作用。
Sepsis, an acute inflammatory disease, remains the most common cause of death in intensive care units. A series of benzimidazole and imidazopyridine derivatives were synthesized and screened for anti-inflammatory activities, and the imidazopyridine series showed excellent inhibition of the expression of inflammatory cytokines in LPS-stimulated macrophages. Compounds X10, X12, X13, X14, and X15 inhibited TNF-alpha and IL-6 release in a dose-dependent manner, and X12 showed no cytotoxicity in hepatic cells. Furthermore, X12 exhibited a significant protection against LPS-induced septic death in mouse models. Together, these data present a series of new imidazopyridines with potential therapeutic effects in acute inflammatory diseases.