4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 5, Pages 1555-1558

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.087

Keywords

1,2,4-trioxolane; ozonide; antimalarial; synthetic peroxide; CYP450

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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. (c) 2008 Elsevier Ltd. All rights reserved.

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