目的合成5种酮洛芬酯类化合物,并研究其抗炎活性和胃肠道不良反应。方法以丹皮酚及结构类似物和酮洛芬为原料,通过碳二亚胺法合成5种化合物;采用二甲苯致小鼠耳廓肿胀模型和角叉菜胶致大鼠足趾肿胀试验对化合物抗炎活性做了初步的药理学筛选;同时考察化合物对胃肠道不良反应的影响。结果化合物的结构经1H-NMR及MS得到确证;5个目标化合物均能显著地减轻小鼠的耳肿胀和大鼠的足趾肿胀程度,与其相应的阳性和阴性对照组相比,都具有良好的抗炎效果;同时,5个目标化合物对胃肠损伤面积明显小于阳性组和阴性组,能够明显地减轻胃肠道的不良反应。结论合成了5种酮洛芬酯类化合物;抗炎活性均明显强于酮洛芬;且对胃肠道的不良反应明显地减轻。 OBJECTIVE To synthesize five ketoprofen esters and study their anti-inflammatory activity and gastrointestinal adverse reactions. Methods Five compounds were synthesized by carbodiimide method using paeonol and its structural analogues and ketoprofen as raw materials. The model of auricle swelling induced by xylene in mice and carrageenan induced rat toe swelling The anti-inflammatory activity of the compound has been preliminary pharmacologically screened; meanwhile, the effects of the compound on adverse reactions of the gastrointestinal tract have been investigated. Results The structures of the compounds were confirmed by 1H-NMR and MS. All of the five target compounds could significantly alleviate the ear swelling in mice and the degree of toe swelling in rats, which were all good compared with the corresponding positive and negative control groups Of the anti-inflammatory effect; the same time, the five target compounds of gastrointestinal lesion area was significantly less than the positive group and negative group, can significantly reduce gastrointestinal adverse reactions. Conclusion Five ketoprofen esters were synthesized. Their anti-inflammatory activity was significantly stronger than that of ketoprofen. The adverse reactions to gastrointestinal tract were relieved.