Patent Evaluation: Artemisinin Analogues as Potential Antimalarial Agents

Summary

Novelty: A process for synthesizing polyoxa heterocyles and, in particular, the antimalarial agent artemisinin and its analogues is disclosed. A new family of artemisinin analogues is disclosed.

Biology: In vitro IC₅₀ data for selected tricyclic artemisinin analogues in drug-resistant strains of P. falciparum are presented. For example, t-butylteperether has IC₅₀ values of 0.41 and 0.53 mg/ml against W-2 and D-6 clones, respectively.

Chemistry: The total synthesis by diastereo-selective silyation is described.