Journal
ACS INFECTIOUS DISEASES
Volume 7, Issue 7, Pages 2013-2024Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsinfecdis.1c00066
Keywords
antiplasmodium; antimalarial; artemsinin; endoperoxide; artemisinin dimers
Categories
Funding
- National Institutes of Health [R01AI090662, R01AI144464]
- Georgia Research Alliance
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Research focuses on the antimalarial activity of artemisinin dimers, particularly the increase in activity of artemisinin moieties and the impact of deactivation caused by degradation of the peroxide bridge.
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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