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吲哚美辛衍生物的合成及其抗炎活性
Synthesis of indomethacin derivatives and their anti-inflammatory activities
【摘要】 目的:合成吲哚美辛衍生物,以寻找新的对胃肠道毒不良反应更小的非甾体抗炎药。方法:吲哚美辛 与卤代烃、硝基苄醇、硝基苄基氯等化合物进行缩合以及硝酸酯化反应,制备相应结构的衍生物。结果与结论:合 成的6个化合物中,化合物3a,3c和5b的抗炎活性明显高于吲哚美辛。
【Abstract】 Objective:To search for new NSAIDs with higher efficacy and lower toxicity. Methods : Indomethacin derivatives were prepared from halohydrocarbons, nitrobenzyl alcohol and netroben zychloride by reactions of condensation and esterfication. Results and Conclusion: 6 new compounds have been synthesized,among them compound 3a,3c and 5b had an anti-inflammatory activity comparable to or higher than indornethathcin.
【关键词】 非甾体抗炎药;
吲哚美辛衍生物;
抗炎活性;
【Key words】 NSAIDs; indomethacin derivatives; anti-inflammatory activity;
【Key words】 NSAIDs; indomethacin derivatives; anti-inflammatory activity;
- 【文献出处】 中国新药杂志 ,Chinese New Drugs Journal , 编辑部邮箱 ,2004年09期
- 【分类号】R914;R96
- 【被引频次】9
- 【下载频次】723