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

ABSTRACT: 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.

SUBMITTER: Lichorowic CL

PROVIDER: S-EPMC9247344 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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

Lichorowic Cynthia L CL Zhao Yingzhao Y Maher Steven P SP Padín-Irizarry Vivian V Mendiola Victoria C VC de Castro Sagan T ST Worden Jacob A JA Casandra Debora D Kyle Dennis E DE Manetsch Roman R

ACS infectious diseases 20210401 7

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 p ...[more]

PMID: 33792305

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| S-EPMC6735958 | biostudies-literature

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