李英, 虞佩琳, 陈一心, 李良泉, 盖元珠, 王德生, 郑亚平. 青蒿素类似物的研究——Ⅰ、还原青蒿素的醚类、羧酸酯类及碳酸酯类衍生物的合成J. 药学学报, 1981, 16(6): 429-439.
引用本文: 李英, 虞佩琳, 陈一心, 李良泉, 盖元珠, 王德生, 郑亚平. 青蒿素类似物的研究——Ⅰ、还原青蒿素的醚类、羧酸酯类及碳酸酯类衍生物的合成J. 药学学报, 1981, 16(6): 429-439.
Li Ying, Yu Peilin, Chen Yixin, Li Liangquan, Gai Yuanzhu, Wang Desheng , Zheng Yaping, . STUDIES ON ANALOGS OF ARTEMISININE Ⅰ. THE SYNTHESIS OF ETHERS, CARBOXYLIC ESTERS AND CARBONATES OF DIHYDROARTEMISININEJ. Acta Pharmaceutica Sinica, 1981, 16(6): 429-439.
Citation: Li Ying, Yu Peilin, Chen Yixin, Li Liangquan, Gai Yuanzhu, Wang Desheng , Zheng Yaping, . STUDIES ON ANALOGS OF ARTEMISININE Ⅰ. THE SYNTHESIS OF ETHERS, CARBOXYLIC ESTERS AND CARBONATES OF DIHYDROARTEMISININEJ. Acta Pharmaceutica Sinica, 1981, 16(6): 429-439.

青蒿素类似物的研究——Ⅰ、还原青蒿素的醚类、羧酸酯类及碳酸酯类衍生物的合成

STUDIES ON ANALOGS OF ARTEMISININE Ⅰ. THE SYNTHESIS OF ETHERS, CARBOXYLIC ESTERS AND CARBONATES OF DIHYDROARTEMISININE

  • 摘要: 青蒿素是当前治疗抗恶性疟疾的首选药物。为克服它的近期复燃率高的缺点,我们以还原青蒿素为中间体,在酸或碱的催化下与各种醇、羧酸酐或酰氯、氯甲酸酯反应,合成了它的醚类,羧酸酯类和碳酸酯类衍生物47个。经鼠疟(P.berghei)抗氯喹原虫株筛选,发现其中大多数化合物的抗疟效果超过青蒿素;以SD90)作比较标准,超过青蒿素十倍左右的化合物有12个。

     

    Abstract: Artemisinine is a new antimalarial drug which has marked theraputic effect on patients suffering from chloroquine-resistant strain of Plasmodium falciparum. In order to find more potent antimalarials, we prepared ethers, carboxylic esters and carbonates of dihydroartemisinine. Forty seven new compounds were evaluated against chloroquineresistant strain of Plasmodium berghei in mice. Most of them are superior to artemisinine itself.The relationship between chemical structure and antimalarial activity in these derivatives of artemisinine is briefly mentioned.Some compounds tested against Schistosoma japonicum in laboratory animals are also shown to be more active than artemisinine.

     

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