| 第 47 卷第 3 期 |  | Vol. 47 No. 3 | | 2017 年 6 月 | Jun 2017 |
|
所屬欄目：醫藥及中間體
2-芳基苯并呋喃類(lèi)化合物的合成與抗心肌缺血活性研究 |
| 李金龍，李永鵬，王少利，吳 浩，金 輒，劉曉平*，胡 春*
（沈陽(yáng)藥科大學(xué)，“基于靶點(diǎn)的藥物設計與研究”教育部重點(diǎn)實(shí)驗室，遼寧 沈陽(yáng) 110016） |
| 摘 要：以丹酚酸C為先導化合物，根據藥物設計中簡(jiǎn)化天然產(chǎn)物活性結構的原則，基于生物電子等排、活性結構優(yōu)化手段，通過(guò)簡(jiǎn)化丹酚酸C結構，設計合成了一系列新型2-芳基苯并呋喃類(lèi)化合物。所合成的目標化合物均未見(jiàn)文獻報道，其組成和結構經(jīng)熔點(diǎn)、紅外光譜和核磁共振氫譜確證。采用小鼠夾閉氣管致心肌缺氧模型測試了目標化合物的抗心肌缺血活性。實(shí)驗結果表明，目標化合物5c、5e、5f、5h具有抗心肌缺血活性。 |
| 關(guān)鍵詞：抗心肌缺血；2-芳基苯并呋喃；構效關(guān)系 |
| 中圖分類(lèi)號：O622.2 文獻標識碼：A 文章編號：1009-9212（2017）03-0016-05 |
|
| 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 |
|
基金項目：國家自然科學(xué)基金資助項目（21342006）。
|
作者簡(jiǎn)介：李金龍（1992-），男，安徽淮北人，碩士研究生，主要從事新藥設計與合成（E-mail：jinlong_li163@163.com）。
|
聯(lián) 系 人：劉曉平，副教授，主要從事新藥設計與合成（E-mail：lxp19730107@163.com）；胡春，教授，主要從事新藥設計與合成（E-mail：chunhu@syphu.edu.cn）。
|
收稿日期：2017-06-17
|
|