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Two in one: bifunctional derivatives of trolox acting as antimalarial and antioxidant agents

par Souard, Florence ;Nicolle, E;Cressend, Delphine;Valentin, Alexis;Boumendjel, Ahcène
Référence Future Medicinal Chemistry, 12, 20, page (1845-1854)
Publication Publié, 2020-10

Article révisé par les pairs

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Résumé :

Background: The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect. Results: Ten compounds were prepared in one step and evaluated on chloroquino-sensitive (3D7) and chloroquino-resistant (FcB1) strains of Plasmodium falciparum. The most active compound (3d) shows antiplasmodial activity in the range of chloroquine against chloroquino-sensitive and chloroquino-resistant P. falciparum strain. The antioxidant activity of (3d) was conducted through four tests and was found to be more potent than trolox itself and L-ascorbic acid. Conclusion: Compound (3d) can be considered as an excellent lead molecule for further in vivo studies. This study paves the way for building large chemical libraries to be investigated in the field of malaria.