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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.
Based on the principle of bioisosterism, Leonurine, the active ingredient in Chinese traditional medicine Leonurus, was used as the lead compound to synthesize 18 Leonurine analogs.The structures of the compounds were characterized by MS, 1H NMR and 13C NMR.The preliminary results showed that Some compounds have Na + / H + exchanger-1 (NHE-1) inhibitory activity, of which compounds 1a and 1e are significantly more active than the positive control Cariporide.