摘要
从新疆一枝蒿中分离得到了单体化合物一枝蒿酮酸,然后以一枝蒿酮酸和有机胺为原料,在偶联剂DCC,HOBt/DMAP的作用下,合成了13种未见文献报道的一枝蒿酮酸酰胺衍生物2a～2m.所合成的化合物经过IR,1HNMR,ESI-MS等分析方法进行了表征,并对化合物2a～2m进行初步的体外抗A3,B型流感病毒和单纯I,II型疱疹病毒活性研究.初步试验结果表明化合物2a同时具有抗A3,B型流感病毒活性,而且抗B型流感病毒活性比母体化合物的活性较高.化合物2d的抗B型流感病毒活性比母体化合物高16倍,化合物2e同时具有较强的抗单纯I,II型疱疹病毒活性.
The rupestonic acid （compound 1） was isolated from the Chinese herbal medicine Artemisia rupestris L. （its Chinese name being Yizhihao）. Then, 13 rupestonic acid amide derivatives 2a-2m were synthesized using rupestonic acid and organic amines in the presence of DCC, HOBt/DMAP and their structures were comfirmed by the methods of IR, 1HNMR, and ESI-MS. All compounds were preliminarily assayed in vitro against influenza A3, B, herpes simplex Ⅰ（HSV-Ⅰ） and herpes simplex Ⅱ （HSV-Ⅱ） viruses, showing that 2a was inhibitive to both influenza A3 and B viruses, and had the higher inhibition against influenza B virus than the parent compound 1. The inhibition of 2d against influenza B virus was 16-fold higher than that of the parent compound and 2e was more active both to HSV-Ⅰ and HSV-Ⅱ viruses.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2008年第10期1807-1812,共6页
Chinese Journal of Organic Chemistry
基金
新疆自治区高技术研究发展计划(No.200515123)
中国科学院知识创新工程重点方向(No.KSCX2-YW-R-132)
国家自然科学基金(No.20872174)资助项目.
关键词
合成
一枝蒿酮酸酰胺衍生物
流感病毒
单纯疱疹病毒
活性研究
synthesis
rupestonic acid amide derivative
influenza A3, B virus
herpes simplex virus
biological activity
