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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.
A monomer compound, artesunate, was isolated from Artemisia anguillarum. Thirteen species of artesunate were synthesized by the coupling of DCC and HOBt / DMAP using artemisiac acid and organic amine as starting materials A artemisinic acid amide derivatives 2a ~ 2m. The synthesized compounds were characterized by IR, 1HNMR, ESI-MS and other analysis methods, and compounds 2a ~ 2m preliminary in vitro anti-A3, B influenza virus and simple I , And herpes simplex virus type II activity.The preliminary test results show that compound 2a has both anti-influenza A3 and anti-influenza B virus activity and anti-influenza B virus activity is higher than the parent compound activity.Compound 2d anti-influenza B virus activity ratio 16 times higher than the parent compound, while compound 2e also has strong anti-herpes simplex virus I and II activity.