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

被引：4

作者：

Lichorowic, Cynthia L. ^{[1
]}

Zhao, Yingzhao ^{[1
]}

Maher, Steven P. ^{[2
]}

Padin-Irizarry, Vivian ^{[2
,3
]}

Mendiola, Victoria C. ^{[2
]}

de Castro, Sagan T. ^{[2
]}

Worden, Jacob A. ^{[2
]}

Casandra, Debora ^{[4
]}

Kyle, Dennis E. ^{[2
,4
]}

Manetsch, Roman ^{[1
,5
]}

机构：

[1] Northeastern Univ, Dept Chem & Chem Biol, Boston, MA 02115 USA

[2] Univ Georgia, Ctr Trop & Emerging Global Dis, Athens, GA 30602 USA

[3] Clayton State Univ, Dept Biol, Morrow, GA 30260 USA

[4] Univ S Florida, Coll Publ Hlth, Ctr Global Hlth & Infect Dis Res, Tampa, FL 33612 USA

[5] Northeastern Univ, Dept Pharmaceut Sci, Boston, MA 02115 USA

来源：

ACS INFECTIOUS DISEASES | 2021年 / 7卷 / 07期

基金：

美国国家卫生研究院;

关键词：

antiplasmodium; antimalarial; artemsinin; endoperoxide; artemisinin dimers; RUTHENIUM-CATALYZED CYCLOADDITION; PLASMODIUM-FALCIPARUM MALARIA; IN-VITRO; TRIOXANE DIMERS; CARBA ANALOGS; DRUG; ANTICANCER; PARASITES; POTENT; OPTIMIZATION;

D O I：

10.1021/acsinfecdis.1c00066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：2013 / 2024

页数：12