沙门氏菌致突变性试验中硝基咪唑并（2,1 - b）噻唑的构效关系
Structure-activity relationship of nitroimidazo (2,1-b) thiazoles in the Salmonella mutagenicity assay.
作者信息
Biagi G L, Hrelia P, Guerra M C, Paolini M, Barbaro A M, Cantelli-Forti G
出版信息
Arch Toxicol Suppl. 1986;9:425-9. doi: 10.1007/978-3-642-71248-7_86.
The mutagenic activity of a series of nitroimidazo (2,1-b) thiazoles was determined in Salmonella typhimurium TA-100 strain by means of the Ames test. A multiple regression analysis showed a highly significant parabolic relationship between mutagenic activity and the Rm values as an expression of the lipophilic character of molecules. The lipophilic character should be important in determining an optimal cell permeation. However when the lipophilic character was expressed by means of the sigma pi values the equation was much less satisfactory. This could be due to the fact that the Rm values of nitroheterocyclic compounds actually represent a measure both of lipophilic and polar character.
通过艾姆斯试验，在鼠伤寒沙门氏菌TA-100菌株中测定了一系列硝基咪唑并（2,1-b）噻唑的诱变活性。多元回归分析表明，诱变活性与作为分子亲脂性特征表达的Rm值之间存在高度显著的抛物线关系。亲脂性特征在确定最佳细胞渗透方面应该很重要。然而，当通过σπ值来表示亲脂性特征时，该方程的拟合度要低得多。这可能是由于硝基杂环化合物的Rm值实际上同时代表了亲脂性和极性特征。
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