Synthesis of Mono- and Bisperoxide-Bridged Artemisinin Dimers to Elucidate the Contribution of Dimerization to Antimalarial Activity.
Synthesis of Mono- and Bisperoxide-Bridged Artemisinin Dimers to Elucidate the Contribution of Dimerization to Antimalarial Activity.
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DOI：
10.1021/acsinfecdis.1c00066
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发表时间：
2021-07-09
影响因子：
5.3
通讯作者：
Manetsch, Roman
中科院分区：
文献类型：
--
作者：
Lichorowic, Cynthia L.;Zhao, Yingzhao;Maher, Steven P.;Padin-Irizarry, Vivian;Mendiola, Victoria C.;de Castro, Sagan T.;Worden, Jacob A.;Casandra, Debora;Kyle, Dennis E.;Manetsch, Roman
在过去的十年中，青蒿素作为一种抗疟疾药物一直备受关注，部分原因是屠呦呦获得了诺贝尔生理学或医学奖。虽然已经完成了许多研究，详细说明了天然产品青蒿素二聚化导致的活性显著增加，但尚未研究过氧化桥导致的活性增加。在这里，我们概述了青蒿素二聚体的抗疟活性的合成和测试，其中二聚体的一半中的过氧化桥被减少，导致具有一个活性和一个失活青蒿素部分的二聚体。
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.
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影响因子：
3.5
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影响因子：
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