Artemisone—A Highly Active Antimalarial Drug of the Artemisinin Class

Abstract

Artemisinin—the next generation: Efficacies of artemisone against the malaria parasite are substantially greater than those of the current artemisinin “gold standard”, artesunate. Also, in contrast to most current artemisinins it displays low lipophilicity and negligible neuro‐ and cytotoxicity in in vitro and in vivo assays. Thus, the drug offers promise for use in artemisinin‐based combination therapy.

New Chemotherapeutic Strategies Against Malaria, Leishmaniasis and Trypanosomiases

“…In 2005 the estimated demand for the fixed combination drug artemetherlumifantrine, containing the dose of artemether required to cure a malaria patient (i.e. 500 mg) was for 120 million adult treatment courses, corresponding to approximately 114 tons of artemisinin, given that the overall chemical yield of artemether from artemisinin is 53% [56]. Following WHO recommendations in 2001, within 8 years 88 countries, including all African countries, had officially adopted ACTs as first-line treatment for uncomplicated malaria.…”

Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols

“…solubility profiles compared with the initial hit molecule 16. The concept of reducing ClogP in antimalarial endoperoxide drug design has been discussed, 39 and here the benefits are evident in terms of producing improved lead compounds with encouraging in vitro and in vivo (vide infra) antimalarial activity profiles. Table 5 below.…”

Antimalarial Drugs – What is in Use and What is in the Pipeline

“…Indeed, artemisone 36 did not show any neuro-or cytotoxicity. In animal experiments, artemisone 36 was about two to five times more efficient than artesunate 11 [190]. Artemisone 36 had been in clinical studies, but allegedly, further development is unsure.…”