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青蒿素是新型化学结构的抗疟药。为了克服复燃率高及不溶解于水的缺点,我们以二氢青蒿素为原料与二元酸或酸酐和二环已基碳二亚胺(DCC)在4-二甲氨基吡啶(DMAP)催化下合成一系列的二氢青蒿素二元酸双酯及单酯类衍生物。经鼠疟(Plasmodium berghei)抗氯喹虫株筛选结果表明,化合物3的抗疟效果比青蒿素强9倍。
Artemisinin is a new chemical structure of antimalarial drugs. In order to overcome the shortcomings of high reuptake rate and insolubility in water, we used dihydroartemisinin as the raw material and dibasic acid or anhydride and dicyclohexylcarbodiimide (DCC) in 4-dimethylaminopyridine (DMAP ) Catalyzed synthesis of a series of dihydroartemisinin diacid diester and monoester derivatives. Plasmodium berghei showed that the anti-malarial effect of Compound 3 was 9 times stronger than that of artemisinin.