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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作者单位E-mail
李修政 安徽医科大学解放军98临床学院, 浙江 湖州 230032  
赵庆杰 第二军医大学药学院, 上海 200433  
董家潇 安徽医科大学解放军98临床学院, 浙江 湖州 230032  
姜云云 解放军101医院, 江苏 无锡 214044  
叶光明 安徽医科大学解放军98临床学院, 浙江 湖州 230032 shygm98@163.com 
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4f4g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
 
Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives
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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