| 非甾体抗炎药ML4000的合成及生物活性研究 |
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| 引用本文： | 郑志超,梅林雨,高晶,罗振福,孙有光.非甾体抗炎药ML4000的合成及生物活性研究[J].中国新药杂志,2011(2). |
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| 作者姓名： | 郑志超 梅林雨 高晶 罗振福 孙有光 |
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| 作者单位： | 天津理工大学化学化工学院;天津药物研究院; |
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| 基金项目： | 天津市2008年度科技计划项目(08ZCKFSH00700) |
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| 摘 要： | 目的:合成非甾体抗炎药ML4000并研究其生物活性。方法:ML4000以环氧合酶(COX)和5-脂氧合酶(5-LOX)双重抑制剂利克飞龙(licofelone,ML3000)为先导化合物,结构上链接了1个一氧化氮(NO)供体;通过灌胃给药,观察ML4000在动物体内的初步代谢、抗炎活性、胃肠道作用以及血清和胃黏膜NO水平。结果:ML4000经IR,MS,1H NMR,13C NMR以及元素分析等确证结构;大鼠灌胃ML4000(10 mg.kg-1)0.25 h后,即可测到ML4000代谢为ML3000;ML4000抗炎活性与ML3000相当;连续14 d灌胃(60mg.kg-1,qd),未见大鼠胃肠道出血;灌胃给药(60 mg.kg-1)1 h后大鼠血清和胃黏膜NO量显著增加。结论:合成的ML4000具有较强的抗炎作用,胃肠道耐受性好,并能够释放出NO。
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| 关 键 词： | 非甾体抗炎药 一氧化氮供体 利克飞龙 合成 生物活性 |
Synthesis and biological activity of the non-steroidal anti-inflammatory drug ML4000 |
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| ZHENG Zhi-chao,MEI Lin-yu,GAO Jing,LUO Zhen-fu,SUN You-guang.Synthesis and biological activity of the non-steroidal anti-inflammatory drug ML4000[J].Chinese Journal of New Drugs,2011(2). |
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| Authors: | ZHENG Zhi-chao MEI Lin-yu GAO Jing LUO Zhen-fu SUN You-guang |
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| Institution: | ZHENG Zhi-chao1,MEI Lin-yu2,GAO Jing2,LUO Zhen-fu2,SUN You-guang1(1 College of Chemistry and Chemical Engineering,Tianjin University of Technology,Tianjin 300191,China,2 Tianjin Institute of Pharmaceutical Research,Tianjin 300193,China) |
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| Abstract: | Objective: To synthesize the non-steroidal anti-inflammatory drug(NSAID) ML4000 and evaluate its biological activity.Methods: Licofelone,a balanced inhibitor of cyclooxygenase(COX) and 5-lipoxygenase(5-LOX),covalently bound to one NO-donating moiety to produce ML4000.The metabolism of ML4000 in vivo,the anti-inflammatory activity,and the effects on gastrointestinal tract(GI),and NO level in the serum and gastric mucosa were determineed.Results: ML4000 structure was confirmed by IR,MS,1H NMR,13C NMR and elem... |
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| Keywords: | non-steroidal anti-inflammatory drugs(NSAIDs) NO donor licofelone synthesis biological activity |
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