Antimalarial Activity of New Dihydroartemisinin Derivatives. 5. Sugar Analogues

摘要

The prevention and treatment of malaria have been thwarted in the developingcountries due to the development of drug resistance by malaria parasites to existing antimalarial agents, such as chloroquine and pyrimethamine. The search for new antimalarial drugs has become, therefore, an urgent mission of drug research programs worldwide. Artemisinin (qinghaosu), a new clinically useful antimalarial agent, is an unsual sesquiterpene lactone containing an endoperoxide function. Its unique chemical structure, coupled with its low toxicity and proven antimalarial efficacy have attracted attention from both chemists and pharmacologists since its discovery in China in the early 1970s. The practical use of artemisinin as an antimalarial agent, however, is impaired by (a) its low solubility in both water and oil, (b) its poor efficacy by oral administration, and the high rate of recrudescence in treated patients. Extensive structure modifications of artemisinin have produced several compounds with improved solubility and efficacy.