| 1位芳基取代的青藤碱衍生物的合成和抗炎活性研究 |
| 投稿时间：2018-01-26 修订日期：2018-05-03 点此下载全文 |
| 引用本文：李修政,赵庆杰,董家潇,姜云云,叶光明.1位芳基取代的青藤碱衍生物的合成和抗炎活性研究[J].药学实践杂志,2018,36(5):417~421 |
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| 中文摘要:目的 进行1位取代芳基的青藤碱衍生物的合成及体外抗炎活性研究。方法 以青藤碱为先导化合物，首先1位溴取代反应，然后通过Suzuki偶联反应对A环1位进行修饰，制得一系列取代芳基的青藤碱衍生物，所有化合物均经1H-NMR、13C-NMR、MS结构确认；采用报告基因法研究青藤碱衍生物对NF-κB转录活性的影响。结果 Suzuki偶联反应得到的一系列化合物活性均优于对照药青藤碱。结论 筛选到的4f和4g可作为候选药物进行深入研究，对研发治疗风湿性关节炎药物具有重要意义。 |
| 中文关键词:青藤碱 结构修饰 衍生物 |
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| Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives |
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| Abstract:Objective To synthesize position 1 substituted sinomenine derivatives and study their anti-inflammatory activity in vitro. Methods A series of substituted sinomenine derivatives were prepared by bromination of sinomenine and Suzuki coupling reaction on the A ring 1. All compounds were confirmed by 1H-NMR,13C-NMR and MS. The reporter gene method was used to study the effect of sinomenine derivatives on NF-κB transcriptional activity. Results All the compounds obtained with Suzuki coupling reaction exhibited better anti-inflammatory activity than the parent compound,sinomenine. Conclusion Two top performers, 4f and 4g,can be used as drug candidates. A further study on those compounds will have significant implication for the development of rheumatoid arthritis drugs. |
| keywords:sinomenine structural modification derivatives |
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