Chapter 25 - Advancement in Research on Artemisinin Derivatives and Relevant Compounds

Abstract

The Institute of Chinese Material Medica, China Academy of Chinese Medical Sciences, discovered artemisinin in 1972 and synthesized dihydroartemisinin in 1973. Shortly afterward, it started the exploration of the relationship between artemisinin derivatives and antimalarial activity. The research staff found that the antimalarial activity of the product was enhanced after the reduction of the carbonyl group in the lactone ring to a hydroxyl group (namely dihydroartemisinin) provided that the peroxide bridge of antimalarial activity groups in artemisinin was retained. After acetylation of hydroxyl group, the activity of the product was further improved. In 1975, the coding sequence diagram of artemisinin-like compounds was reported in the “523” internal meeting, thus promoting the development of domestic and foreign research on artemisinin derivatives. The new drugs that have been derived and developed include sodium artesunate, artemether, dihydroartemisinin, and arteether. Based on in-depth study on the structure–activity relationship, pharmaceutical chemists have conducted extensive research on other artemisinin derivatives and artemisinin-related compounds to seek for newer antimalarial therapy.