Articles

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 Lu ,
  • JIANG Xiang-Min ,
  • HE Guang-Wei ,
  • XU Wen-Ting ,
  • GONG Guo-Qing ,
  • XU Yun-Gen
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  • 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 date: 2011-08-05

  Revised date: 2011-10-22

  Online published: 2012-03-09

Supported by

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

Abstract

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.

Cite this article

JIN Lu , JIANG Xiang-Min , HE Guang-Wei , XU Wen-Ting , GONG Guo-Qing , XU Yun-Gen . Synthesis and Na+/H+ Exchanger-1-Inhibitory Activity of 4(6)-{2-[4-(2,3,4-Trimethoxybenzyl)piperazin-1-yl]-2-oxoethoxy}-aroylguanidine Derivatives[J]. Chinese Journal of Organic Chemistry, 2012 , 32(02) : 326 -332 . DOI: 10.6023/cjoc1108051

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