In this paper, we reported the synthesis of bifendate derivatives and evaluation of anti-inflammatory activity by detecting the production of the Nitric Oxide (NO) in the lipopolysaccharide(LPS)-stimulated RAW 264.7 cell lines. Among the newly derivatives, compound 7k was the most potent one and two other compounds (7e and 7f) also exhibited greater anti-inflammatory activity than bifendate. Further in vivo studies confirmed that 7k significantly and dose-dependently inhibited carrageenan-induced paw edema and decreased the serum levels of alanine aminotransaminase, and aspartate aminotransaminase in concanavalin A-induced hepatitis model. Histopathological evaluation demonstrated that 7k has better hepatoprotective effect on acute liver injury induced by concanavalin A than bifendate, suggesting that 7k is a potential drug candidate for the treatment of hepatic injuries.

在本文中，我们通过检测脂多糖（LPS）刺激的RAW 264.7细胞系中一氧化氮（NO）的产生，报告了联苯二酸酯衍生物的合成和抗炎活性的评估。在新衍生物中，化合物7k是最有效的一种，另外两种化合物（7e和7f）也显示出比联苯菊酯更大的抗炎活性。进一步的体内研究证实，在刀豆球蛋白A诱导的肝炎模型中，7k能够显着且剂量依赖性地抑制角叉菜胶诱导的爪水肿，并降低血清丙氨酸氨基转氨酶和天冬氨酸氨基转氨酶的水平。组织病理学评估表明7k在伴刀豆球蛋白A引起的急性肝损伤中比联苯双酯具有更好的肝保护作用，表明7k是治疗肝损伤的潜在药物候选物。