| 第 47 卷第 3 期 |  | Vol. 47 No. 3 | | 2017 年 6 月 | Jun 2017 |
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所属栏目：医药及中间体
2-芳基苯并呋喃类化合物的合成与抗心肌缺血活性研究 |
| 李金龙，李永鹏，王少利，吴 浩，金 辄，刘晓平*，胡 春*
（沈阳药科大学，“基于靶点的药物设计与研究”教育部重点实验室，辽宁 沈阳 110016） |
| 摘 要：以丹酚酸C为先导化合物，根据药物设计中简化天然产物活性结构的原则，基于生物电子等排、活性结构优化手段，通过简化丹酚酸C结构，设计合成了一系列新型2-芳基苯并呋喃类化合物。所合成的目标化合物均未见文献报道，其组成和结构经熔点、红外光谱和核磁共振氢谱确证。采用小鼠夹闭气管致心肌缺氧模型测试了目标化合物的抗心肌缺血活性。实验结果表明，目标化合物5c、5e、5f、5h具有抗心肌缺血活性。 |
| 关键词：抗心肌缺血；2-芳基苯并呋喃；构效关系 |
| 中图分类号：O622.2 文献标识码：A 文章编号：1009-9212（2017）03-0016-05 |
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| Synthesis and Anti-myocardial Ischemia Activity of 2-Arylbenzofuran Derivatives |
| LI Jin-long, LI Yong-peng, WANG Shao-li, WU Hao, JIN Zhe, LIU Xiao-ping*, HU Chun*
(Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education; Shenyang Pharmaceutical University, Shenyang 110016, China) |
| Abstract：Salvianolic acid C isolated from Salvia miltiorrhiza has the protective effects on heart cells injured by myocardial ischemia and oxygen re-supply. In order to discover the new 2-arylbenzofuran derivatives with anti-myocardial ischemia activity, the salvianolic acid C was chosen as the lead compound; based on several drug design methods including simplification of active natural products, bioisosterism and active structure optimization, a series of 2-arylbenzofuran derivatives were designed, synthesized and characterized by melting point, IR and proton NMR spectra. The anti-myocardial ischemia activity of the target compounds was studied using the pharmacological model of the duration of electrocardiograph after clamping trachea in mice. The biological screening results showed that some target compounds 5c, 5e, 5f and 5h exhibited anti-myocardial ischemia activity. |
| Key words：anti-myocardial ischemia; 2-arylbenzofuran derivatives; structure-activity relationship |
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基金项目：国家自然科学基金资助项目（21342006）。
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作者简介：李金龙（1992-），男，安徽淮北人，硕士研究生，主要从事新药设计与合成（E-mail：jinlong_li163@163.com）。
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联 系 人：刘晓平，副教授，主要从事新药设计与合成（E-mail：lxp19730107@163.com）；胡春，教授，主要从事新药设计与合成（E-mail：chunhu@syphu.edu.cn）。
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收稿日期：2017-06-17
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