IN VITRO OXIDATION OF THE 8-HYDROXYQUINOLINE MOIETY WITH METABOLIC ACTIVATION SYSTEM TO A MUTAGENIC QUINOLOQUINONE COMPOUND OF LAVENDAMYCIN ANALOGS

概要

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Intermediary products in the synthesis of lavendamycin were tested for mutagenic activities in Salmonella typhimurium TA 98 and TA 100 with and without a metabolic activation system. Lavendamycin analogs having a methyl group at the 3' position showed a significant mutagenicity to TA 100 after the metabolic activation using S9 mix prepared from rat liver homogenate. Oxidative products of the 8-hydroxyguinoline derivatives were mutagenic without the metabolic activation. Of these oxidative products, desamino-desmethyllavendamycin methyl ester was identified as a metabolic product obtained by the incubation of the 8-hydroxyguinoline derivative with mouse liver homogenate.
社団法人日本薬学会の論文
1986-03-25