目的合成甘草次酸酰胺的异噁唑衍生物, 寻找活性好的抗炎药物。方法以甘草次酸为原料, 与3-取代苯基-5-异唑甲胺进行偶联, 合成了6个新型甘草次酸酰胺类衍生物, 采用IR、¹H-NMR、¹³C-NMR、MS等方法确定其化学结构。以二甲苯引起的小鼠耳肿模型和醋酸引起的小鼠腹膜炎模型评价了抗炎活性。结果IR、¹H-NMR、¹³C-NMR、MS等数据表明这些化学结构正确。其中, 化合物具有明显的抗炎活性。结论合成的系列新化合物结构正确, 发现了一个抗炎活性较强的化合物。

Objective To synthesize the novel derivatives of glycyrrhetinic acid containing isoxazole ring with high anti inflammatory activities.Methods Using 18β-glycyrrhetinic acid as a raw material,six novel glycyrrhetinic 30-amide derivatives were synthesized by coupling of 18β-glycyrrhetinic acid with 3-R-Ar-5-isoxazole-methylamine.And the synthesized compounds were analyzed by means of IR,¹H-NMR, ¹³C-NMR.and MS.Their preliminary anti-inflammatory activities were evaluated by two models.They are ear swelling of mice induced by xylene and peritonitis of mice induced by acetic acid.Results The structures of all the novel compounds were identified and proven right.The compound IV showed a significant anti-inflammatory activity in two model tests and compounds I,Ⅱ,andⅢwere active only by inhibiting the ear swelling induced by xylene.Conclusion The modification of glycyrrhetinic acid can produce a series of derivatives with correct structures and various activities,and a compound with significant anti-inflammation has been found.