RELATIONSHIP BETWEEN BIOLOGICAL ACTIVITIES AND ENZYMATIC REDUCTION OF NITROFURAN DERIVATIVES

概要

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All nitrofuran derivatives tested, 3-(5-nitro-2-furyl)-2-(2-furyl) acrylic acid [I], 5-nitro-2-furanacrylic acid [II] and 5-nitro-2-furoic acid [III], and their amide and ester derivatives exhibited the mutagenic and antibacterial activities against Salmonella typhimurium TA 100. The amides and esters of [I] and [III] which were more rapidly reduced by intact Salmonella typhimurium TA 100 cells or milk xanthine oxidase showed apparently stronger mutagenicity than the corresponding carboxylic acids ([I] and [III]) which were less susceptible to the reduction. In the case of [II] and its derivatives, the correlation between the mutagenic activity and the reducibility was also observed, but not so clear as in other groups. Furthermore, antibacterial activities of the nitrofuran derivatives in each group were also well correlated to their reduction rates. However, the nitrofuran derivatives highly susceptible to the enzymatic reduction were not always strong mutagenic and antibacterial agents.
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