チオ尿素誘導体の代謝に関する研究 (第1報)

4,4´-Diethoxythiocarbanilide投与家兎尿中の代謝物について その1

抄録

Among the thiocarbanilide derivatives, being observed as an effective therapeutic agent for leprosy and tuberculosis, 4, 4′-diethoxythiocarbanilide (EtO-OEt) was administered per os to male rabbits and the metabolites excreted in urine were studied. Ether soluble metabolite was separated by the thin layer chromatography (TLC) and alumina column chromatography into non-reacted EtO-OEt, 4-ethoxy-4′-hydroxythiocarbanilide (EtO-OH), 4, 4′-dihydroxythiocarbanilide (HO-OH), 4, 4′-diethoxycarbanilide (EtO-O-OEt), 4-ethoxy-4′-hydroxycarbanilide (EtO-O-OH) and 4, 4′-dihydroxycarbanilide (HO-O-OH), produced by de-ethylation and desulfurization, as well as the decomposed phenetidine besides a few unknown substances. As to the conjugates, though they were not obtained purely, the Rf values of their crude conjugates were compared with that of synthesized compounds, and the hydrolysis of β-glucuronidase suggested that the presence of O-glucuronides with EtO-OH, EtO-O-OH and HO-OH have been identified. Smith did not observed the desulfurization product in rabbit urine metabolites by the administration of thiocarbanilide (H-H) and its some derivatives. However, the author, by tracing back the metabolism of H-H, identified the desulfurization product 4-hydroxycarbanilide (H-O-OH) by TLC.