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

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.

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-03, Vol.18 (5), p.1555-1558
Hauptverfasser:	Zhou, Lin, Alker, André, Ruf, Armin, Wang, Xiaofang, Chiu, Francis C.K., Morizzi, Julia, Charman, Susan A., Charman, William N., Scheurer, Christian, Wittlin, Sergio, Dong, Yuxiang, Hunziker, Daniel, Vennerstrom, Jonathan L.
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2,4-Trioxolane Adamantane - analogs & derivatives Adamantane - chemistry Adamantane - metabolism Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarial Antimalarials - chemistry Antimalarials - metabolism Antiparasitic agents Biological and medical sciences CYP450 Cytochrome P-450 Enzyme System - metabolism Heterocyclic Compounds - chemistry Heterocyclic Compounds - metabolism Heterocyclic Compounds, 1-Ring - chemistry Heterocyclic Compounds, 1-Ring - metabolism Humans Medical sciences Microsomes, Liver - metabolism Molecular Structure Ozonide Peroxides - chemistry Peroxides - metabolism Pharmacology. Drug treatments Spiro Compounds - chemistry Spiro Compounds - metabolism Synthetic peroxide
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.01.087