Dispiro-1,2,4,5-tetraoxanes: A New Class of Antimalarial Peroxides

Jonathan L. Vennerstrom, Hong Ling Fu, William Y. Ellis, Steven L. Andersen, Lucia Gerena, Arba L. Ager, James K. Wood

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Dispiro-1,2,4,5-tetraoxanes 2-4 were synthesized as potential peroxide antimalarial drugs. They had curative activity against Plasmodium berghei in vivo at single doses of 320 and 640 mg/kg which confirms earlier unpublished data. Moreover, artemisinin (1) and 4 had equivalent ED50′s against P. berghei in vivo in the multiple-dose Thompson test; neither showed any evidence of acute toxicity at total doses of more than 12 g/kg. Dispiro-1,2,4,5-tetraoxane 4 had IC50′s comparable to those of 1 against Plasmodium falciparum clones in vitro. These results confirm the potential of dispiro-1,2,4,5-tetraoxanes as a new class of inexpensive peroxide antimalarial drugs.

Original languageEnglish (US)
Pages (from-to)3023-3027
Number of pages5
JournalJournal of Medicinal Chemistry
Issue number16
StatePublished - Aug 1 1992

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Vennerstrom, J. L., Fu, H. L., Ellis, W. Y., Andersen, S. L., Gerena, L., Ager, A. L., & Wood, J. K. (1992). Dispiro-1,2,4,5-tetraoxanes: A New Class of Antimalarial Peroxides. Journal of Medicinal Chemistry, 35(16), 3023-3027. https://doi.org/10.1021/jm00094a015