The comparative antimalarial properties of weak base and neutral synthetic ozonides

Yuanqing Tang, Sergio Wittlin, Susan A. Charman, Jacques Chollet, Francis C.K. Chiu, Julia Morizzi, Lisa M. Johnson, Josefina Santo Tomas, Christian Scheurer, Chistopher Snyder, Lin Zhou, Yuxiang Dong, William N. Charman, Hugues Matile, Heinrich Urwyler, Arnulf Dorn, Jonathan L. Vennerstrom

Research output: Contribution to journalArticlepeer-review

14 Scopus citations


Thirty-three N-acyl 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. For these ozonides, weak base functional groups were not required for high antimalarial potency against Plasmodium falciparum in vitro, but were necessary for high antimalarial efficacy in Plasmodium berghei-infected mice. A wide range of Log P/DpH 7.4 values were tolerated, although more lipophilic ozonides tended to be less metabolically stable.

Original languageEnglish (US)
Pages (from-to)563-566
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number2
StatePublished - Jan 15 2010
Externally publishedYes


  • 1,2,4-Trioxolanes
  • Antimalarial
  • Artemisinin
  • Peroxides
  • Secondary ozonides


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