摘要
为了提高一枝蒿酮酸的生物活性,以一枝蒿酮酸和3-取代苯基-5-氨甲基-异噁唑为原料,在偶合试剂DCC,HOBt/DMAP的作用下,合成了6个未见文献报道的含异噁唑的一枝蒿酮酸酰胺衍生物3a～3f.所合成的化合物均经过IR,1H NMR,13C NMR,ESI-MS等分析方法表征及初步体外抗A(H3N2,H1N1)型和B型流感病毒活性研究.初步实验结果表明:化合物3c同时具有抗A(H3N2)型和B型流感病毒活性,化合物3c和3e表现出比母体化合物强的抗B型流感病毒活性.
To improve biological activity of rupestonic acid,six rupestonic acid amide derivatives containing isoxazole were synthesized in the presence of DCC,HOBt/DMAP using the rupestonic acid and 3-aryl-5-isoxazole-methylamine as the start-ing materials.The synthesized compounds 3a～3f were confirmed by the methods of 1H NMR,13C NMR,IR,ESI-MS tech-niques and preliminarily assayed in vitro against influenza viruses A and B.The results showed that compound 3c showed better activity against both influenza viruses A（H3N2） and B,and compounds 3c and 3e had the higher inhibition against in-fluenza B virus than the parent compound 1.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2012年第2期333-337,共5页
Chinese Journal of Organic Chemistry
基金
新疆自治区高技术研究发展计划(No.200910105)
国家自然科学基金(No.20872174)
国家杰出青年基金科学(No.30925045)资助项目~~
关键词
一枝蒿酮酸
异噁唑衍生物
流感病毒
活性研究
rupestonic acid
isoxazole derivative
influenza virus
inhibitory activity
