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有机化学 ›› 2012, Vol. 32 ›› Issue (02): 326-332 .DOI: 10.6023/cjoc1108051 上一篇    下一篇

研究论文

4(6)-{2-[4-(2,3,4-三甲氧基苄基)哌嗪-1-基]-2-氧代乙氧基}芳甲酰胍类化合物的合成及其Na+/H+交换器1 抑制活性

靳璐a, 姜向敏a, 何广卫b, 徐文婷a, 龚国清c, 徐云根a   

  1. a 中国药科大学药物化学教研室 南京 210009;
    b 合肥医工医药有限公司 合肥 230088;
    c 中国药科大学药理学教研室 南京 210009
  • 收稿日期:2011-08-05 修回日期:2011-10-22 发布日期:2012-03-09
  • 通讯作者: 何广卫; 徐云根 E-mail:xyg64@126.com
  • 基金资助:

    国家自然科学基金(No. 30672512)资助项目.

Synthesis and Na+/H+ Exchanger-1-Inhibitory Activity of 4(6)-{2-[4-(2,3,4-Trimethoxybenzyl)piperazin-1-yl]-2-oxoethoxy}-aroylguanidine Derivatives

Jin Lua, Jiang Xiangmina, He Guangweib, Xu Wentinga, Gong Guoqingc, Xu Yungena   

  1. a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009;
    b Hefei Yi Gong Medicine Technology Company Limited, Hefei 230088;
    c Department of Pharmacology, China Pharmaceutical University, Nanjing 210009
  • Received:2011-08-05 Revised:2011-10-22 Published:2012-03-09
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 30672512).

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NHE1 (Na+/H+交换器1)抑制剂对于心肌缺血再灌注损伤具有较好的保护作用. 以苯(或吡啶)甲酰胍为母核, 利用拼合原理, 在苯(或吡啶)甲酰胍母环上引入4-(2,3,4-三甲氧基苄基)哌嗪-1-甲基, 设计并合成了8 个未见文献报道的目标化合物. 其结构经MS, IR, 1H NMR 和元素分析确证. 体外血小板肿胀模型(PSA)试验结果表明, 大部分目标化合物显示出较好的NHE1 抑制活性.

关键词: NHE1 抑制剂, 缺血再灌注损伤, 苯(或吡啶)甲酰胍, 合成

Na+/H+ exchanger 1 (NHE1) inhibitors have a protective effect against myocardial ischemic-reperfusion injury. By choseing benzoyl (or pyridine-3-carbonyl) guanidine as main structure, and introducing 4-(2,3,4-trimethoxybenzyl)piperazine- 1-yl to its benzene (or pyridine) ring, eight compounds were designed and synthesized. All the target compounds have not been reported and their structures have been confirmed by IR, 1H NMR, MS and elemental analysis. The rat platelet swelling assay (PSA) results showed that most of the tested compounds exhibited potent NHE1 inhibitory effects.

Key words: NHE1 inhibitor, ischemia-reperfusion injury, benzoyl (or pyridine-3-carbonyl) guanidine, synthesis