论文部分内容阅读
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。
OBJECTIVE: To synthesize indomethacin derivatives to find new NSAIDs with less adverse gastrointestinal toxicity. Methods: Indomethacin was condensed with nitrocarbons by halogenated hydrocarbons, nitrobenzyl alcohol and nitrobenzyl chloride to prepare the corresponding derivatives. RESULTS AND CONCLUSION: Among the 6 compounds synthesized, the anti-inflammatory activity of compounds 3a, 3c and 5b was significantly higher than that of indomethacin.