新型一枝蒿酮酸异噁唑衍生物的合成及其抗A,B型流感病毒活性研究  

Synthesis of Novel Isoxazole Contained Rupestonic Acid Derivatives and in vitro Inhibitory Activity against Influenza Viruses A and B

作　　者：赵江瑜[1,2] 阿吉艾克拜尔·艾萨[1] 

机构地区：[1]中国科学院新疆理化技术研究所、干旱区植物资源化学重点实验室,乌鲁木齐830011 [2]中国科学院研究生院,北京100039

出　　处：《有机化学》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~~

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.

关 键 词：一枝蒿酮酸 异噁唑衍生物 流感病毒 活性研究 

分 类 号：R96[医药卫生—药理学] R914[医药卫生—药学]