Ye B, Wu Y L, Li G F, Jiao X Q
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences.
Yao Xue Xue Bao. 1991;26(3):228-30.
Compound 3 (deoxoqinghaosu) and compound 4 (deoxocarbaqinghaosu) were synthesized from arteannuic acid (2). Primary exploration of their antimalarial effect against K173 strain of Plasmodium berghei shows that compound 3 is somewhat more effective than the natural compound--qinghaosu. However, the carba-analogue compound 4 is almost ineffective. The enhanced activity of compound 3 is supposedly ascribed to its higher lipophilicity and, hence, higher affinity for plasmodial membrane. Further studies are in progress.
化合物3（脱氧青蒿素）和化合物4（脱氧碳青霉烯青蒿素）由青蒿酸（2）合成。对它们针对伯氏疟原虫K173株的抗疟效果进行的初步探索表明，化合物3比天然化合物青蒿素稍有效。然而，碳青霉烯类似物化合物4几乎无效。化合物3活性增强据推测归因于其较高的亲脂性，因此对疟原虫膜具有更高的亲和力。进一步的研究正在进行中。
