BIOACTIVATIONS INVOLVING HALOGEN-CONTAINING SUBSTITUENTS

作者: Norio Kurihara

DOI: 10.1016/B978-0-08-029224-3.50046-0

关键词: ToxicationYield (chemistry)Combinatorial chemistryChemistryPhosgeneOrganic chemistryMoleculeConjugateChloroformBromobenzeneMetabolite

摘要: Bioactivations involving halogen-containing substituents can be divided into 2 classes: (I) modifications in the shape, size and/or physical properties of molecule and (II) introduction a new reactive group that attack target. Aldrin epoxidation is class I bioactivation, toxication by oxygenation xenobiotics such as bromobenzene, chloroform halothane belongs to II. Epoxidation may convert compound stable metabolite dieldrin, but usually it gives product which sometimes rearranges yield carbonyl compound. Oxygenation carbon-hydrogen bond hydroxyl group; when gemhalohydrin spontaneously transformed very toxic like phosgene from chloroform. Glutathione conjugation compounds detoxicated metabolites, an intermediary conjugate responsible for adverse effects 1,2-dibromoethane. At present, we cannot predict bioactivation specific compound, anticipate its possible metabolites. Thus, discuss beforehand their toxicities based on chemical structures above findings.

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