【作者】 吴丽颖；

【导师】 宋宏锐；

【作者基本信息】 沈阳药科大学 ， 药物化学， 2007， 硕士

【摘要】 本论文是关于吡咯并[1，2-a]吡嗪-1-酮类化合物的合成及其抗炎镇痛活性的研究。有机合成实验室在对吡咯里嗪酮类抗炎镇痛剂的研究过程中发现，吡里酮的结构类似物吡嗪酮具有显著的抗炎镇痛作用，一些已合成的吡嗪酮衍生物具有明显的抗炎镇痛活性，预示着该类化合物抗炎镇痛作用的构效关系具有广阔的研究前景。本课题是在吡嗪酮类化合物已有的研究基础上，设计合成二十一个未见文献报道的新型吡嗪酮类化合物，从而进行深入的抗炎镇痛构效关系研究，其结构经~1H-NMR，MS确证。以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试验，结果表明，以200mg／kg的剂量灌胃给药，WLY-113，WLY-115，WLY-119具有一定的镇痛作用；WLY-103，WLY-114，WLY-119具有一定的抗炎作用，并总结了一些初步的构效关系规律。更多还原

【Abstract】 The synthesis and structure-activity relationship(SAR) of the novel nonsteroidal anti -inflammatory agents,pyrrolo[l,2-a]pyrazine-l-one derivatives were reported in this dissertation.In the research of pyrrolizinones of nonsteroidal anti-inflammatory drugs(NSAIDs),it has been proved that pyrazinones showed remarkable anti-inflammatory and analgesic activities. Based on the SAR of pyrazinones and their analogues reported in our laboratory, twenty-one new pyrazinone derivatives were designed and synthesized for further study of the SAR, which structures have been confirmed by ~1H-NMR and MS. They have not been found in literatures.Anti-inflammatory and analgesic activities were evaluated with xylene-induced ear edema and acetic acid-induced writhing in mice, respectively. The results of pharmacological tests show that some synthesized compounds have anti-inflammatory and/or analgesic activities. Some new SAR of these compounds is discussed from the studies above.更多还原