【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。更多还原

【Abstract】 Aim To study the structure-activity relationships of 6-aryl derivatives of(2H)-2-cyclohexyl-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one and to search for new anti-inflammatory and analgesic agents.Method (2H)-2-cyclohexyl-3,4-dihydropyrrolo[1,2-a]pyrazin-1-one was synthesized from methyl pyrrole-2-carboxylate 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.更多还原