摘要
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 design and synthesiz seven novel cyclovirobuxine D derivatives with better anti - anoxia activity. METHODS Using cyclovirobuxine D as the starting materials, the target compounds we synthesized. RESULTS The structures of the derivations were characterized by IR, 1 HNMR , 13 CNMR and MS. The anti - anoxia activities of the compounds were also investiga- ted. CONCLUSION The result indicates that these compounds display different degrees of activity. The compounds with morpholinyl, or imidazolyl piperazinyl exhibit higher anti - anoxia activity than that of cyclovirobuxine D.
出处
《华西药学杂志》
CAS
CSCD
2016年第6期553-555,共3页
West China Journal of Pharmaceutical Sciences
基金
西南民族大学研究生创新型科研项目(CX2016SZ057)
四川省教育厅项目(15ZB0487)
关键词
环维黄杨星D
含氮杂环化合物
合成
耐缺氧活性
结构修饰
衍生物
Cyclovirobuxine D
Nitrogen heterocycles compounds
Synthesis
Anti - anoxia activity
Structural modification
Derivatives
