The discovery of the endoperoxide sesquiterpene lactone artemisinin in 1979 initiated a new era in malaria chemotherapy. The peroxide bond in artemisinin is essential for activity, suggesting a chemistry-driven mechanism of action. The semisynthetic artemisinins are important antimalarial drugs because they rapidly reduce parasite burden and have good therapeutic indices, but their short half-lives require three-day treatment regimens in combination with longer-acting antimalarials to maximize cure rates. With this in view, many synthetic peroxide antimalarials have been prepared. Yet, identification of synthetic peroxides that are easily synthesized, inexpensive, and with good biopharmaceutical properties has been surprisingly difficult. In this talk, we highlight the discovery of the antimalarial ozonides (1,2,4-trioxolanes) arterolane (OZ277) and artefenomel (OZ439). The former was registered in India as a combination product with piperaquine (Synriam) and the latter is in Phase IIb trials.

<b>Award Address</b> (ACS Award for Creative Invention sponsored by the ACS Corporation Associates). Antimalarial ozonides

2019 Spring National Meeting

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Award Address (ACS Award for Creative Invention sponsored by the ACS Corporation Associates). Antimalarial ozonides