论文部分内容阅读
目的以环维黄杨星D为先导化合物进行结构修饰,以寻求更好的耐缺氧活性的衍生物。方法将能改变药物活性和水溶性的含氮杂环化合物用于环维黄杨星D的结构修饰,合成目标化合物Ⅱa~Ⅱg。结果合成了7个未见报道的环维黄杨星D衍生物,其结构经1HNMR、13CNMR、MS和IR表征;同时进行了小鼠耐缺氧活性的研究。结论合成的新化合物具有一定的生物活性,其中,含吗啉基、咪唑基、哌嗪基取代的衍生物具有较好的生物活性。
OBJECTIVE To structurally modify cyclovirobuxine D as a lead compound in order to search for better hypoxia-tolerant derivatives. Methods The title compounds Ⅱa ~ Ⅱg were synthesized by modifying the structure of cyclovirobuxium D with the nitrogen-containing heterocyclic compounds which can change the drug activity and water solubility. Results Seven unreported cyclopinin D derivatives were synthesized and their structures were characterized by 1HNMR, 13CNMR, MS and IR. At the same time, the hypoxia tolerance of mice was studied. Conclusion The new compounds have certain biological activity. Among them, morpholino, imidazolyl and piperazinyl substituted derivatives have good biological activity.