FIGURE 1: Artemisinin (ART) and some of its derivatives. The endoperoxide bond constitutes the pharmacophore for the action of ARTs. Direct ART derivatives are usually modifiers of ART at the C10 position. Some other endoperoxides differ greatly structurally but also manifest potent anti-malarial activities. See also references [23, 24, 25]. 1 Artemisinin. 2a Dihydroartemisinin (DHA). 2b Artemether. 2c Arteether. 2d Artesunate. 3, 4 An analogue with close structure to artemisinin. 5a, 5b Enantiomers with similar activities against malaria parasites. 6 An antimalarial tetraoxane. 7 OZ439 (in clinical trial).

23. Li J, Zhou B (2010). Biological actions of artemisinin: insights from medicinal chemistry studies. Molecules 15(3): 1378-1397.

24. Haynes RK, Ho WY, Chan HW, Fugmann B, Stetter J, Croft SL, Vivas L, Peters W, Robinson BL (2004). Highly antimalaria-active artemisinin derivatives: biological activity does not correlate with chemical reactivity. Angew Chem Int Ed Engl 43(11): 1381-1385.

25. Ploypradith P (2004). Development of artemisinin and its structurally simplified trioxane derivatives as antimalarial drugs. Acta Trop 89(3): 329-342.

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