Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
IN VITRO OXIDATION OF THE 8-HYDROXYQUINOLINE MOIETY WITH METABOLIC ACTIVATION SYSTEM TO A MUTAGENIC QUINOLOQUINONE COMPOUND OF LAVENDAMYCIN ANALOGS
Satoshi HibinoMiko OkazakiMasataka IchikawaKohichi SatoAiichiro MotoshimaHiroshi Ueki
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1986 Volume 34 Issue 3 Pages 1376-1379

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Abstract

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.

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© The Pharmaceutical Society of Japan
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