A series of pyridine-linked indanone derivatives were designed and synthesized to discover new small molecules for the treatment of inflammatory bowel disease (IBD). Compounds 5b and 5d exhibited strongest inhibitory activity against TNF-α-induced monocyte adhesion to colon epithelial cells (an in vitro model of colitis). In TNBS (2,4,6-trinitrobenzenesulfonic acid)-induced rat colitis model, oral administration of the compounds 5b and 5d ameliorated colitis with significant recovery in altered expressions of E-cadherin, TNF-α and IL-1β expressions, indicating 5b and 5d as potential agents for therapeutics development against IBD.

中文翻译：

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吡啶连接的茚满酮衍生物的合成和生物学评估：炎症性肠病的潜在药物

设计并合成了一系列吡啶连接的茚满酮衍生物，以发现治疗炎症性肠病（IBD）的新小分子。化合物5b和5d对TNF-α诱导的单核细胞粘附于结肠上皮细胞表现出最强的抑制活性（结肠炎的体外模型）。在TNBS（2,4,6-三硝基苯磺酸）诱导的大鼠结肠炎模型中，口服给予化合物5b和5d改善了结肠炎，E-钙黏着蛋白，TNF-α和IL-1β表达的改变明显恢复，表明5b和5d作为针对IBD的治疗药物开发的潜在药物。