Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277

Lin Zhou, André Alker, Armin Ruf, Xiaofang Wang, Francis C.K. Chiu, Julia Morizzi, Susan A. Charman, William N. Charman, Christian Scheurer, Sergio Wittlin, Yuxiang Dong, Daniel Hunziker, Jonathan L. Vennerstrom

Research output: Contribution to journalArticle

29 Scopus citations

Abstract

The antimalarial synthetic ozonide OZ277 (RBx11160) was hydroxylated by human liver microsomes at the distal bridgehead carbon atoms of the spiroadamantane substructure to form two carbinol metabolites devoid of antimalarial activity.

Original languageEnglish (US)
Pages (from-to)1555-1558
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number5
DOIs
StatePublished - Mar 1 2008

Keywords

  • 1,2,4-Trioxolane
  • Antimalarial
  • CYP450
  • Ozonide
  • Synthetic peroxide

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Zhou, L., Alker, A., Ruf, A., Wang, X., Chiu, F. C. K., Morizzi, J., Charman, S. A., Charman, W. N., Scheurer, C., Wittlin, S., Dong, Y., Hunziker, D., & Vennerstrom, J. L. (2008). Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277. Bioorganic and Medicinal Chemistry Letters, 18(5), 1555-1558. https://doi.org/10.1016/j.bmcl.2008.01.087