Oxidized Metabolites of p-(±)-α-Hydroxyethylbenzenesulfonamide and p-(±)-α-Hydroxyethylbenzenesulfonylurea Derivatives Appeared in Rat Plasma

Abstract

The oxidized metabolites appeared in the rat plasma after intravenous administration of benzenesulfonamide (Ia), 1-cyclohexyl-3-benzenesulfonylurea (Ib) and 1-n-butyl-3-benzene-sulfonylurea (Ic) with a (±)-α-hydroxyethyl substituent at the para position were investigated. The metabolically produced ketones were identified with those of authentic samples by comparing their high performance liquid chromatographic retention times. On the other hand, Ib (hydroxyhexamide) and its major metabolite, IIb (acetohexamide) extracted from the rat plasma, were identified by gas chromatography-mass spectrometry after trimethyl-silylation. These alcohols and respective ketones are presumably related to reversible drug-metabolite in rats.