Antimalarial Effect of 3-Methoxy-1,2-Dioxetanes on the Erythrocytic Cycle of Plasmodium falciparum

作者：Lopes Nicolas S; Yoshitake Ariane M; Silva Adriana F; Oliveira Vani X Jr; Silva Leandro S; Pinheiro Ana A S; Ciscato Luiz Francisco M L^*

来源：Chemical Biology & Drug Design, 2015, 86(6): 1373-1377.

DOI：10.1111/cbdd.12599

• 1,2-dioxetanes
• antimalarial peroxides
• Fenton reaction
• Plasmodium falciparum

The antimalarial activity of peroxides most likely originates from their interaction with iron(II) species located inside the malaria parasite, which forms destructive radical species through a Fenton-like mechanism. This article reports the first evaluation of the in vitro antimalarial activity of three peroxides of the class 1,2-dioxetanes against Plasmodium falciparum; the results reveal that the studied 3-methoxy-1,2-dioxetanes display significant antimalarial activity, at a similar level as artemisinin and also that their reactivity toward iron (II) correlate linearly with their antimalarial activity.

• 出版日期2015-12