The effect of varying halogen substituent patterns on the cytochrome P450 catalysed dehalogenation of 4-halogenated anilines to 4-aminophenol metabolites

NHP Cnubben, J Vervoort, MG Boersma…

Index: Cnubben, Nicole H. P.; Vervoort, Jacques; Boersma, Marelle G.; Rietjens, Ivonne M. C. M. Biochemical Pharmacology, 1995 , vol. 49, # 9 p. 1235 - 1248

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Citation Number: 37

Abstract

The cytochrome P450 catalysed biotransformation of 4-halogenated anilines was studied in vitro with special emphasis on the dehalogenation to 4-aminophenol metabolites. The results demonstrated that a fluorine substituent at the C4 position was more easily eliminated from the aromatic ring than a chloro-, bromo-or iodo-substituent. HPLC analysis of in vitro biotransformation patterns revealed that the dehalogenation of the C4-position ...