Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives.
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-α 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.
['Chen|Gaozhi|G|', 'Liu|Zhiguo|Z|', 'Zhang|Yali|Y|', 'Shan|Xiaoou|X|', 'Jiang|Lili|L|', 'Zhao|Yunjie|Y|', 'He|Wenfei|W|', 'Feng|Zhiguo|Z|', 'Yang|Shulin|S|', 'Liang|Guang|G|']
benzimidazoles imidazopyridines sepsis macrophages anti-inflammation