選択毒性に関する研究(第9報) : Haloacetamide系化合物の生物活性

概要

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In connection with the question of a relationship between chemical structure and selective toxicity of halogenoacetamide compounds, antimicrobial activity was examined in a group of compounds having a general formula of Ar-N(-R)-C(=O)-CH_2X, where Ar was limited to 2,4,5-substituted phenyl or naphthyl group. The compounds showed stronger activity when X was fluorine, chlorine, bromine, and iodine in that order, and also showed antimicrobial activity of a wide spectrum. Compounds having electronegative substituents in the 2-, 4-, and 5-positions showed a good activity, and 2,4,5-trichlorophenylmonoiodoacetamide and 2,4,5-trichlorophenylmonobromoacetamide were especially good, showing a broad spectrum and excellent therapeutic effect against experimental trichophytosis in animals. All the compounds, except those with fluorine, showed a low acute toxicity. The characteristic pharmacological action included hypothermia and a slight sedative action. Fluorine-substituted compounds of this series are known to be an aconitase inhibitor of the TCA cycle, have a strong toxicity in mammals, and show central stimulation and inhibition of respiratory and circulatory organs.
社団法人日本薬学会の論文
1968-12-25