Diol Bridged Dimer Derivatives Of Artemisinin Cleavage

As the malaria parasites produced resistance or reduced sensitivity against all existing antimalarial drugs, such as chloroquine, a new star of antimalarial compound, now called qinghaosu or artemisinin, has become wordwide used. But because of its high re-combustion rate, qinghaosu and the derivatives have become the focus of this field. Many 1,2,4-trioxane dimers have high in vitro antimalarial, antiproliferative and antitumor activities, and some of them have high in vivo anticancer activity. In this thesis we reviewed the exploits and the antimalarial mechanisms of artemisinin-type drugs, and prepared dihydroartemisinin ethanediol dimer with simple structure and high stability, which was characterized by single crystal X-ray diffraction. Then we used ferrous ion to cleave the peroxy bonds of above dimer and examined the influence of cysteine on the reaction and the amount of FeSO4. The corresponding compounds were characterized by melting point, IR, MS and NMR.The mode of action to cleave the peroxy bond into free radicals may explain antimalarial and antitumor activities of the dimer of dihydroartemisinin on molecular level. The result provides support to some extent for research of structure-function relation and exploitation of new antimalarial drugs.