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目的研究吡咯并吡嗪酮类化合物的抗炎镇痛作用构效关系,寻找具有抗炎镇痛活性的新型吡嗪酮类化合物。方法以2-甲基-3-苯基吡咯并[1,2-a]吡嗪-1(2H)-酮化合物为母体,合成系列化合物。用二甲苯致小鼠耳肿胀法和醋酸致小鼠扭体法对所合成的目标化合物分别进行了抗炎和镇痛活性实验。结果合成了11个目标化合物,经1H-NMR和MS确证其结构。小鼠实验表明,一些所合成的化合物具有一定的抗炎或镇痛作用。结论化合物14抗炎镇痛活性较好,值得进一步研究。
Objective To study the structure-activity relationship of anti-inflammatory and analgesic effects of pyrrolopyrazinones and to find novel pyrazinones with anti-inflammatory and analgesic activity. Methods A series of compounds were synthesized using 2-methyl-3-phenylpyrrolo [1,2-a] pyrazin-1 (2H) -one as the precursor. Anti-inflammatory and analgesic activities of the target compounds were tested respectively by xylene-induced mouse ear swelling and acetic acid writhing in mice. Results Eleven target compounds were synthesized and confirmed by 1H-NMR and MS. Mouse experiments show that some of the compounds synthesized have some anti-inflammatory or analgesic effects. Conclusion The anti-inflammatory and analgesic activity of compound 14 is good and worthy of further study.