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  • Title: Quantitative relationships between lipophilicity and mutagenic effects of N-substituted amides of 3-(5-nitro-2-furyl)-acrylic acid on Salmonella typhimurium.
    Author: Baláz S, Sturdík E, Dibus I, Ebringer L, Stibrányi L, Rosenberg M.
    Journal: Chem Biol Interact; 1985 Oct; 55(1-2):93-108. PubMed ID: 3905031.
    Abstract:
    Mutagenic effects of 10 N-alkylamides of 3-(5-nitro-2-furyl)-acrylic acid were assessed in two strains of Salmonella typhimurium TA100 (rfa+ and rfa-). Experimental data were confronted with physiologically based compartment model comprising passive membrane transport, metabolical inactivation in cytoplasm and formation of a reactive intermediate which is responsible for receptor modification. The quantitative dependences observed between mutagenicity and lipophilicity indicate that, in both cases, the drug-receptor interaction takes place in a hydrophobic compartment localized in the cytoplasm. The mutagenic potency of some derivatives was influenced also by stericity.
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