| Abstract: | Studies of the N-Oxygenation of N-(tert.Alkyl)benzamidines in vitro N-tert.Butyl- and N-tert.octylbenzamidine ( 1a and b ) and their potential N-oxygenated metabolites, the amidoximes 2a and b , have been synthesized and characterized. N-tert.Butylbenzamidine 1a is N-oxygenated to the amidoxime 2a by aerobic incubation with non-induced microsomal fractions of rabbit liver homogenates and NADPH. This transformation supports the hypothesis that benzamidines undergo N-oxygenation by the cytochrome P-450 enzyme system when N-dealkylation is not possible (absence of hydrogen atoms in α-position to the amidine nitrogen atoms). |
