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2-(2, 6-二氯苯胺基)苯乙酸(3-硝氧甲基)苯酯的合成及抗炎镇痛活性[J]. 中国药科大学学报, 2003, (1): 15-18.
引用本文: 2-(2, 6-二氯苯胺基)苯乙酸(3-硝氧甲基)苯酯的合成及抗炎镇痛活性[J]. 中国药科大学学报, 2003, (1): 15-18.
Synthesis and Anti-inflammatory Analgesic Activities of 2-(2,6-dichlorophenylamino)-benzeneacetic Acid(3-nitroxymethyl) Phenyl Ester[J]. Journal of China Pharmaceutical University, 2003, (1): 15-18.
Citation: Synthesis and Anti-inflammatory Analgesic Activities of 2-(2,6-dichlorophenylamino)-benzeneacetic Acid(3-nitroxymethyl) Phenyl Ester[J]. Journal of China Pharmaceutical University, 2003, (1): 15-18.

2-(2, 6-二氯苯胺基)苯乙酸(3-硝氧甲基)苯酯的合成及抗炎镇痛活性

Synthesis and Anti-inflammatory Analgesic Activities of 2-(2,6-dichlorophenylamino)-benzeneacetic Acid(3-nitroxymethyl) Phenyl Ester

  • 摘要: 目的:获得抗炎活性强、胃肠道副作用小的新型非甾体抗炎药。方法:以间羟基苯甲醛为原料,经还原、溴代和硝氧化,最后与双氯芬酸进行酯化反应,制备2-(2,6-二氯苯胺基)苯乙酸(3-硝氧甲基)苯酯(ZLR-9);观察ZLR-9对二甲苯致炎小鼠和角叉菜胶致炎大鼠的抗炎活性,对热板法实验和扭体实验小鼠的镇痛活性及致大鼠胃肠道反应,研究体内外ZLR-9的NO释放。结果:ZLR-9结构经MS、IR、^1HNMR确证,它的抗炎镇痛活性强于DC-Na,胃肠道副作用显著小于DC-Na,并小于文献报道的硝酸酯类DO-DC,体内有明显的NO释放。结论:ZLR-9值得深入研究。

     

    Abstract: AIM:To obtain novel nonsteroidal anti inflammatory drug with higher potency and lower undesirable effects. METHOD:Synthesizing 2 (2, 6 dichlorophenylamino)benzeneacetic acid (3 nitroxy methyl) phenyl ester (ZLR 9) from m hydroxybenzaldehyde through

     

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