摘要
目的研究(2H)-2-环己基-3,4-二氢吡咯[1,2-a]吡嗪-1-酮衍生物抗炎镇痛作用的构效关系。方法以2-吡咯甲酸甲酯为原料,经取代、环合,制备(2H)-2-环己基-3,4-二氢吡咯[1,2-a]吡嗪-1-酮(3);通过Friedel-Crafts酰基化反应,制得其6-酰基衍生物4a^4j。用小鼠测试了所合成化合物的抗炎和镇痛活性。结果与结论合成了10个未见文献报道的新化合物4a^4j,其结构经MS1、H-NMR分析确证。抗炎镇痛试验表明,有些化合物具有明显的抗炎和/或镇痛作用,其中化合物4d的活性与对照药布洛芬相当。
Aim To study the structure-activity relationships of 6-aryl derivatives of （2H）-2-cyclohexyl-3, 4- dihydropyrrolo[1,2-a]pyrazin-l-one and to search for new anti-inflammatory and analgesic agents. Method （2H）-2-cyclohexyl-3, 4-dihydropyrrolo [ 1, 2-a] pyrazin-l-one was synthesized from methyl pyrrole-2-car- boxylate via substitution and cyclization, and the target compounds 6-aryl derivatives were obtained by Friedel-Crafts reaction. Their anti-inflammatory and analgesic activities were tested in xylene-induced mice ear edema and acetic acid-induced mice writhing. Results and conclusion Ten new 6-aryl derivatives were synthesized and their structures were confirmed by MS, ^1H-NMR. Most of the compounds show remarkable anti-inflammatory and/or analgesic activities in mice, and the activities of compound 4d is comparable to ibuprofen.
出处
《中国药物化学杂志》
CAS
CSCD
2006年第1期23-26,共4页
Chinese Journal of Medicinal Chemistry
