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还原青蒿素羧酸酯的合成

The Synthesis of Carboxylic Esters of Dihydroartemisinine

  • 摘要: 抗疟新药青蒿素有速效、低毒的优点,但在临床上存在杀灭疟原虫不彻底、近期复发率高的缺陷。为了克服这种缺陷,自1979年以来,我们合成了九个还原青蒿素羧酸酯,拟增强其脂溶性,以期达到延长药效而克服近期复发的目的。实验结果,化合物Ⅰ、Ⅱ、Ⅲ、Ⅸ的疗效优于青蒿素。

     

    Abstract: Artemisinine is a new type of fast-acting suppresive antimalarial drug. Dihydroar-temisinine is its reduced product. We have prepared nine oarboxylio esters of dihvdroartemisinine for evaluation of their antimalarial potency. All the new compounds have been tested for suppressive antimalarial activity against p. herghei in mice, four Ⅰ、Ⅱ、Ⅲ、Ⅸ,) of them are superior to artemisinine.

     

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