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 ar...

Full description

Saved in:
Bibliographic Details
Published in:ACS infectious diseases 2021-07, Vol.7 (7), p.2013-2024
Main Authors: Lichorowic, Cynthia L, Zhao, Yingzhao, Maher, Steven P, Padín-Irizarry, Vivian, Mendiola, Victoria C, de Castro, Sagan T, Worden, Jacob A, Casandra, Debora, Kyle, Dennis E, Manetsch, Roman
Format: Article
Language:English
Subjects:
Antimalarials - pharmacology
Artemisinins - pharmacology
Dimerization
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:2373-8227
2373-8227
DOI:10.1021/acsinfecdis.1c00066