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

以中药益母草中有效成分益母草碱为先导化合物,按生物电子等排原理,设计合成了18个益母草碱类似物.通过MS,1H NMR,13C NMR对化合物结构进行表征.初步的药效研究结果表明部分化合物具有Na+/H+交换器-1(NHE-1)抑制活性,其中化合物1a和1e的活性显著强于阳性对照药Cariporide.

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.