Juneja T R, Bala A, Kumar P, Gupta R L
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
Mutat Res. 1995 Nov;348(3):137-45. doi: 10.1016/0165-7992(95)00058-5.
Ortho-, meta- and para-nitrobenzyl bromides, alcohols, ethers and esters were synthesised and tested for their mutagenicity toward Salmonella typhimurium TA100, TA100NR (nitroreductase deficient) and TA98 in absence of S9 mix and in TA100 with S9 mix. Compounds of the ortho- and meta-series were non mutagenic with and without S9 mix. Except for the alcohol and ether, the compounds of the para-series were mutagenic in TA100 with activity sequence propionate > butyrate > benzoate > acetate > bromide and this specific activity was reduced considerably by S9 mix. The Ames Salmonella test system does not seem to be an appropriate model to evaluate mutagenicity of o-nitrobenzyls. However, further work is in progress to test all the compounds for mutagenicity in mammalian system.
合成了邻、间、对硝基苄基溴、醇、醚和酯，并在无S9混合液的情况下以及在有S9混合液的TA100中测试了它们对鼠伤寒沙门氏菌TA100、TA100NR（硝基还原酶缺陷型）和TA98的致突变性。邻位和间位系列的化合物在有和没有S9混合液的情况下均无致突变性。除醇和醚外，对位系列的化合物在TA100中具有致突变性，活性顺序为丙酸盐＞丁酸盐＞苯甲酸盐＞乙酸盐＞溴化物，并且这种比活性会被S9混合液显著降低。艾姆斯沙门氏菌试验系统似乎不是评估邻硝基苄基致突变性的合适模型。然而，正在进行进一步的工作，以测试所有化合物在哺乳动物系统中的致突变性。
