(2-Bromoacyl)ureidesの生体内脱ブロム反応に関する研究(第2報) : (2-Bromopropionyl)ureaおよび(2-Bromocaproyl)ureaの脱ブロムについて

概要

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In the previous work of this series, it was found that bromine atom in bromural, Carbromal, and Acetylcarbromal was reductively removed in rabbits, ureide chain remaining intact. The present experiment was undertaken to obtain further confirmation that this pathway occurs generally in the metabolism of 2-bromoacylureides, using (2-bromopropionyl) urea and (2-bromocaproyl) urea. Rabbits were used as experimental animals, and the urine collected 24 hours after medication was extracted continuously with ethyl acetate. Crude crystals obtained from urine extracts of rabbits were further purified by column chromatography over alumina and identified to be the debrominated metabolites, n-propionyl urea and n-caproylurea. Determination of these metabolites excreted in the 24-urine after medication was carried out by the combination of thin-layer chromatography and ultraviolet absorption spectra. Since the above conversion did proceed in the homogenate of the liver and kidney, but the activity disappeared completely in the boiled homogenates, it was assumed that this debromination had occurred enzymatically. From these findings, in addition to the previous ones, it may be concluded that this reductive debromination is a metabolic process occurring generally in (2-bromoacyl) ureides.
公益社団法人日本薬学会の論文
1967-06-25