Abstract

Since the discovery of the endoperoxide sesquiterpene lactone artemisinin, numerous second-generation semisynthetic artemisinins and synthetic peroxides have been prepared and tested for their antimalarial properties. Using a case-study approach, we describe the discovery of the investigational semisynthetic artemisinins artelinic acid (8) and artemisone (9), and the structurally diverse synthetic peroxides arteflene (10), fenozan B07 (11), arterolane (12), PA1103/SAR116242 (13), and RKA182 (14).

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