The direct‐acting mutagenicity of nitroimidazo[2,1‐b]thiazoles in Salmonella typhimurium

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Abstract
A series of nitroimidazo[2,1‐b]thiazole derivatives was investigated for directacting mutagenic potency with the Salmonella assay. All of the nine derivatives tested were mutagenic. The compounds induced predominantly base displacements resulting in frame‐shift mutations. The mutagenic activity did not require the S9 fraction but was largely dependent on “classical” bacterial nitroreductase. The primary basis of the mutagenic activity of nitroimidazo[2,1‐b]thiazoles appears to be a reduction of the nitro‐function to the corresponding hydroxylamine. Mutagenicity seems to be paralleled by an increase of the nitro groups: dinitroderivatives were more active than nitroderivatives. Other electrophiles and sterically constrained nitro groups could account for differences in genotoxicity.