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.

过去十年间，作为抗疟药物的青蒿素（artemisinin）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天然青蒿素二聚化可显著提升其抗疟活性，但过氧桥键（peroxide bridge）无法解释的活性提升机制仍有待探索。本研究针对一类青蒿素二聚体开展合成与抗疟活性测试：该类二聚体其中一个单体的过氧桥键被还原，最终得到仅含一个活性青蒿素基团、另一个基团失活的二聚体。