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Xenobiotica
the fate of foreign compounds in biological systems
Volume 13, 1983 - Issue 8
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Original Article

The N-oxidation of benzamidines in vitro

Pages 467-473 | Received 24 Dec 1982, Published online: 30 Sep 2009
 

Abstract

1. The enzymic N-oxidation of a series of N-unsubstituted basic benzamidines (I) to a new type of metabolite, the amidoximes (II), is reported.

2. Rabbit liver homogenates (9000g supernatant) were used as enzyme source, and metabolites were identified by t.l.c. and mass spectral analysis using synthetic reference compounds.

3. The microsomal NADPH- and oxygen-dependent hydroxylation of benzamidines was not detected after incubation of benzamidine in the presence of SKF 525-A, a known inhibitor of cytochrome P-450.

4. Neither benzamidine or p-methoxybenzamidine is a good substrate for purified microsomal FAD-containing mono-oxygenase.

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