新型抗心绞痛药物的设计、合成及生物活性评价

Design,Synthesis and Biological Evaluation of the Novel Anti-angina Drugs

以雷诺嗪为模板,设计合成了3个雷诺嗪类似物,其结构经^1HNMR、^13CNMR、ESI-MS确证。考察所合成化合物对大鼠心绞痛模型ST-T波、CK-MB、MDA、LDH的影响。结果显示,所合成化合物能显著抑制大鼠心绞痛模型ST-T波抬高,并能降低大鼠心绞痛模型MDA、LDH、CK-MB的含量,优于阳性对照物雷诺嗪。所合成化合物具有显著的抗心绞痛、心肌损伤保护作用,具有较好的开发前景。

Using Ranolazine as the template,three Ranolazine analogues were designed and synthesized,and the structures were confirmed by ^1HNMR,^13CNMR and ESI-MS.Detecting the effects of synthetic compounds on ST-T wave,CK-MB,MDA and LDH in rat angina pectoris model.The results showed that,synthetic compounds can significantly inhibit the elevation of ST-T wave and decrease the content of MDA,LDH and CK-MB in rats with angina pectoris,which is superior to that of Ranolazine.The synthetic compounds have significant anti-angina pectoris,myocardial injury protection,with good prospects for development.