Artemisinins improving metabolism

The use of these artemisinin derivatives in combination with an antimalarial drug with a longer half-life, as recommended by WHO, can not only delay emergence of resistance but also partially overcome the problem of short plasma half-life [19]. Nevertheless, chemically and metabolically more stable artemisinins would bring improvement in malaria therapy and bitherapy (or combination therapy) [20],... 

Artemisinin 337 is a natural efficient antimalarial drug for the treatment of multidrug-resistant forms of P. falciparum. However, pharmacological problems associated with 337, especially a short plasma half-life prompted scientists to search for more metabolically stable derivative. 10-Triiluoromethyl artemisinin 338 was shown to have improved stability. ... 

A series of artemisinin-based semisynthetic antimalarial derivatives, with all of them maintaining the key endoperoxide bridge, such as arteether (18), artemether (19), artesunate (20), and dihydroartemisinin (21), have been designed to improve the water solubility and the metabolic stability of artemisinin [53, 54], Among them, dihydroartemisinin (artenimol), is considered as a common active metaboUte of artemisinin derivatives [53, 54]. Currently, artemisinin-based therapies eombined with standard antimalarials such as amodiaquine, sulfadoxine-pyrimethamine, mefloquine, and lumefantrine are recommended by the World Health Organization (WHO) as first-line therapies for malaria [55, 56]. 

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