1位芳基取代的青藤碱衍生物的合成和抗炎活性研究

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1位芳基取代的青藤碱衍生物的合成和抗炎活性研究

李修政, 赵庆杰, 董家潇, 姜云云, 叶光明

文章导航 > 药学实践与服务 > 2018 > 36(5): 417-421

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]. 药学实践与服务, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

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]. 药学实践与服务, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

LI Xiuzheng, ZHAO Qingjie, DONG Jiaxiao, JIANG Yunyun, YE Guangming. Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

Citation:

LI Xiuzheng, ZHAO Qingjie, DONG Jiaxiao, JIANG Yunyun, YE Guangming. Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

1位芳基取代的青藤碱衍生物的合成和抗炎活性研究

doi: 10.3969/j.issn.1006-0111.2018.05.007

1.
安徽医科大学解放军98临床学院, 浙江湖州 230032
2.
第二军医大学药学院, 上海 200433
3.
解放军101医院, 江苏无锡 214044

Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives

1.
Huzhou Clinical College of Anhui Medical University, No. 98 Hospital of PLA, Huzhou 230032, China
2.
School of Pharmacy, Second Military Medical University, Shanghai 200433, China
3.
No. 101 Hospital of PLA, Wuxi 214044, China

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。
- 青藤碱 /
- 结构修饰 /
- 衍生物
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.
- sinomenine /
- structural modification /
- derivatives

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[2]	高晨鑫,张湛明,陈继红,等. 青藤碱对类风湿关节炎细胞因子影响的研究进展[J]. 风湿病与关节炎,2017,6(2):72-75.
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1位芳基取代的青藤碱衍生物的合成和抗炎活性研究

doi: 10.3969/j.issn.1006-0111.2018.05.007

1. 安徽医科大学解放军98临床学院, 浙江湖州 230032

2. 第二军医大学药学院, 上海 200433

3. 解放军101医院, 江苏无锡 214044

收稿日期: 2018-01-26
修回日期: 2018-05-03

关键词:

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。

English Abstract

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]. 药学实践与服务, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

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]. 药学实践与服务, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

LI Xiuzheng, ZHAO Qingjie, DONG Jiaxiao, JIANG Yunyun, YE Guangming. Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

Citation:

LI Xiuzheng, ZHAO Qingjie, DONG Jiaxiao, JIANG Yunyun, YE Guangming. Synthesis and anti-inflammatory activity of position 1 substituted sinomenine derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(5): 417-421. doi: 10.3969/j.issn.1006-0111.2018.05.007

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