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| 3,4-二氢吡咯[1,2-a]吡嗪-1-酮衍生物的合成及抗炎镇痛作用 | |
| 引用本文： | 付德才,周鸿娟,狄蕊,张守芳.3,4-二氢吡咯[1,2-a]吡嗪-1-酮衍生物的合成及抗炎镇痛作用[J].中国药物化学杂志,2006,16(1):23-26. |
| 作者姓名： | 付德才 周鸿娟 狄蕊 张守芳 |
| 作者单位： | 1. 河北科技大学,化学与制药工程学院,河北,石家庄,050018 2. 河北师范大学,实验中心,河北,石家庄,050016 3. 沈阳药科大学,制药工程学院,辽宁,沈阳,110016 |
| 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。 |
| 关 键 词： | 药物化学 构效关系 化学合成 (2H)-2-环己基-3 4-二氢吡咯[1 2-a]吡嗪-1-酮 6-酰基衍生物 抗炎 镇痛 |
| 文章编号： | 1005-0108（2006）01-0023-04 |
| 收稿时间： | 2005-10-17 |
| 修稿时间： | 2005年10月17 |
Synthesis,anti-inflammatory and analgesic activities of (2H)-2-cyclohexyl-3,4-dihydropyrrolo[1,2-a] pyrazin-1-one derivatives |
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| FU De-cai,ZHOU Hong-juan,DI Rui,ZHANG Shou-fang.Synthesis,anti-inflammatory and analgesic activities of (2H)-2-cyclohexyl-3,4-dihydropyrrolo[1,2-a] pyrazin-1-one derivatives[J].Chinese Journal of Medicinal Chemistry,2006,16(1):23-26. | |
| Authors: | FU De-cai ZHOU Hong-juan DI Rui ZHANG Shou-fang |
| Institution: | 1. College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, China ; 2. Experimental Center, Hebei Normal University, Shijiazhuang 050016, China ; 3. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
| Abstract: | Aim To study the structure-activity relationships of 6-aryl derivatives of(2H)-2-cyclohexyl-3,4-dihydropyrrolo1,2-a]pyrazin-1-one and to search for new anti-inflammatory and analgesic agents.Method (2H)-2-cyclohexyl-3,4-dihydropyrrolo1,2-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. |
| Keywords: | medicinal chemistry structure-activity relationships chemical synthesis (2H)-2-cyclohexyl-3 4-dihydropyrrolo[1 2-a]pyrazin-1-one 6-aryl derivatives anti-inflammatory analgesic |
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