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青蒿琥酯钠(3)在水溶液中不稳定会造成抗疟疗效下降。因其结构上酯键易水解所致,为此,合成了含有羧酸的二氢青蒿素(2)呈醚键结合的一系列新化合物,其中以蒿醚林酸(Artelinic acid,8d)最有前途,其结构式为; 本品对Plasmodium falciparam D-6(塞拉利昂无性系)和W-2(印度支那无性系)进行了体外抗疟试验,结果表明,青蒿素(1),(2)及(8d)对一些抗疟剂,如氯喹、奎宁、乙胺嘧啶、周效磺胺等均无交叉对抗,而三者对抗W-2比D-6更为有效。合
Artesunate sodium (3) instability in aqueous solution will lead to decreased anti-malarial efficacy. A series of new compounds with ether bond of dihydroartemisinin (2) containing carboxylic acid were synthesized for their hydrolysis of the ester bond. For Artelinic acid (8d) The most promising and the most promising one is its structure. The anti-malaria test in vitro of Plasmodium falciparam D-6 and W-2 (Indochinese clones) showed that artemisinin (1), (2 ) And (8d) did not cross-fight against some anti-malarial agents such as chloroquine, quinine, pyrimethamine, psoraleamide and the like, and the three were more effective against D-6 than W-2. Together