Design, Synthesis and Sodium Hydrogen Exchanger Isoform-1 (NHE-1) Inhibitory Activity of Leonurine Analogues

Chin. J. Org. Chem. ›› 2011, Vol. 31 ›› Issue (9): 1445-1451. Previous Articles Next Articles

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益母草碱类似物设计、合成及其Na^＋/H^＋交换器-1抑制活性

钟国琛¹，彭家志¹，李家明*^,1，徐云根²，周鹏¹，盛日正¹

(¹安徽中医学院药学院安徽省现代中药重点实验室合肥 230031)
(²中国药科大学药物化学教研室南京 210009)

收稿日期:2011-01-07 修回日期:2011-03-31 发布日期:2011-04-27
通讯作者: 李家明 E-mail:lijiaming2004@sina.com

Design, Synthesis and Sodium Hydrogen Exchanger Isoform-1 (NHE-1) Inhibitory Activity of Leonurine Analogues

Zhong Guochen¹ Peng Jiazhi¹ Li Jiaming*^,1 Xu Yungen² Zhou Peng¹ Sheng Rizheng¹

(¹Anhui Key Laboratory of Traditional Chinese Medicine, Department of Pharmacy, Anhui College of Traditional Chinese Medicine, Hefei 230031)
(²Department of Medicinal Chem-istry, China Pharmaceutical University, Nanjing 210009)

Received:2011-01-07 Revised:2011-03-31 Published:2011-04-27

Leonurine, a useful compound of Chinese traditional medicine, was used as leading compounds. Eighteen leonurine analogues were designed and synthesized based on the bioisosterism. Their structures were characterized by ¹H NMR, ¹³C NMR and mass spectra. The results of preliminary pharmacological tests showed that some of compounds possess sodium hydrogen exchanger isoform-1 (NHE-1) inhibitory effects, among them, the inhibitory activities of compounds 1a and 1e were stronger than cariporide.

Key words: leonurine, ischemia-reperfusion injury, NHE-1 inhibitory activity, synthesis

Cite this article

ZHONG Guo-Chen, PENG Jia-Zhi, LI Jia-Ming, XU Yun-Gen, ZHOU Peng, SHENG Ri-Zheng. Design, Synthesis and Sodium Hydrogen Exchanger Isoform-1 (NHE-1) Inhibitory Activity of Leonurine Analogues[J]. Chin. J. Org. Chem., 2011, 31(9): 1445-1451.

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益母草碱类似物设计、合成及其Na^＋/H^＋交换器-1抑制活性

Design, Synthesis and Sodium Hydrogen Exchanger Isoform-1 (NHE-1) Inhibitory Activity of Leonurine Analogues

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益母草碱类似物设计、合成及其Na＋/H＋交换器-1抑制活性

Design, Synthesis and Sodium Hydrogen Exchanger Isoform-1 (NHE-1) Inhibitory Activity of Leonurine Analogues

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Cited

Abstract

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Related Articles 15

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益母草碱类似物设计、合成及其Na^＋/H^＋交换器-1抑制活性