环维黄杨星D的结构改造及生物活性

Structural modification and bioactivity of cyclovirobuxine D

目的 通过对植物活性单体环维黄杨星D的结构改造 ,以寻求疗效更好、治疗安全范围更宽的心血管药物。方法 根据合理药物设计原理 ,设计合成目标化合物 ,并研究其生物活性。结果 获得 1 0个环维黄杨星D新衍生物 ,经光谱证明了结构。结论 选取部分环维黄杨星D新衍生物进行耐缺氧、抗心律失常药理实验 ,结果表明部分化合物药理活性优于环维黄杨星D。

Aim To search for new compounds for the treatment of cardiovascular diseases by structural modification of cyclovirobuxine D. Methods According to rational drug design principle, a series of cyclovirobuxine D analogues were prepared, and their bioactivities were tested. Results Ten new compounds were syntheized and confirmed by spectra. Conclusion Endurance lacking oxygen activity and antiarrhythmia effects of some analogues of cyclovirobuxine D were tested. Some compounds showed better activity than cyclovirobuxine D.