吡咯并吡嗪酮类化合物的合成及抗炎镇痛活性研究  

The Study on Synthesis and Anti-inflammatory and Analgesic Activities of Pyrrolepyrazinone

作　　者：吴丽颖[1] 马鹤[1] 王玉玲[1] 宋宏锐[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《河北化工》2007年第9期3-5,共3页Hebei Chemical Industry

摘　　要：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。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。合成了10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。化合物WLY-113、WLY-115的镇痛活性较好,WLY-103、WLY-114的抗炎活性较好,值得进一步研究。To study the structure-activity relationship （SAR） of the title compounds and search for the novel nonsteroidal anti-inflammatory agents in pyrrolepyrazinone. A series of pyrrolepyrazinone derivatives were prepared. Anti-inflammatory and analgesic activities were evaluated with xylene-induced ear edema and acetic acid-induced writhing in mice, respectively. Ten new compounds were synthesized and their structures were confirmed by ＇H-NMR and MS. Some of the target compounds showed anti-inflammatory or analgesic activities. WLY-113.WLY-115 have anti-inflammatory activities, WLY-103.WLY-114 have analgesic activities. They could be regarded as valuable compounds for further study.

关 键 词：药物化学 制备 化学合成 吡咯并[1 2-a]吡嗪酮 抗炎 镇痛 

分 类 号：R971.1[医药卫生—药品]