Synthesis of Mono- and Bisperoxide-Bridged Artemisinin Dimers to Elucidate the Contribution of Dimerization to Antimalarial Activity

During the past decade, artemisinin as an antimalarial has been in the spotlight, in part due to the Nobel Prize in Physiology or Medicine awarded to Tu Youyou. While many studies have been completed detailing the significant increase in activity resulting from the dimerization of natural product artemisinin, activity increases unaccounted for by the peroxide bridge have yet to be researched. Here we outline the synthesis and testing for antimalarial activity of artemisinin dimers in which the peroxide bridge in one-half of the dimer is reduced, resulting in a dimer with one active and one deactivated artemisinin moiety.过去十年来，青蒿素（artemisinin）作为抗疟药物备受关注，这在一定程度上源于屠呦呦获得诺贝尔生理学或医学奖。尽管已有多项研究阐明了天然产物青蒿素二聚化所带来的活性显著提升，但其中无法通过过氧桥键（peroxide bridge）解释的活性增强机制仍有待深入研究。本研究详细阐述了一类青蒿素二聚体的合成方法与抗疟活性测试流程：该类二聚体其中一个单体的过氧桥键被还原，最终得到一个包含一个活性青蒿素结构单元与一个失活青蒿素结构单元的二聚体。