环维黄杨星D磺酰化衍生物的合成及耐缺氧活性的研究

Synthesis and effects of sulfonamide derivatives of Cyclovirobuxine D on oxygen-deficient endurance in mice

目的寻找更多具有治疗心脑血管疾病的潜在药物。方法通过磺酰化反应将不同取代的磺酰氯中间体连接到环维黄杨星D上,合成得到目标产物,并对其进行耐缺氧活性的研究。结果和结论共合成了7个环维黄杨星D磺酰化衍生物,其结构经IR、MS1、HNMR和高分辨质谱(HRMS)确证,且化合物2 a^2g均具有良好的药理活性,其中化合物2 e、2g作用最强,超过现有临床药物黄杨宁片。

OBJECTIVE To obtain more potential agents for the treatment of cardiovascular diseases. METHODS The target compounds were synthesized from the corresponding sulfonic acid chloride and Cyclovirobuxine D by sulfonamide acylation. RESULTS and CONCLUSION The structures of all compounds synthesized were determined by IR, MS, 1 HNMR and HRMS. Their effects on oxygen - deficient endurance in mice were primarily evaluated. The results indicated that all compounds possess efficiency on oxygen - defecient endurance, especially that compounds 2e, 2g were more active than clinical drug Cyclovirobuxinel tablet. These seven new compounds can promote the treatment capability of cardiovascular diseases.