Lappas L C, Hirsch C A, Winely C L
J Pharm Sci. 1976 Sep;65(9):1301-5. doi: 10.1002/jps.2600650910.
Various derivatives of 5-nitro-1, 3-dioxane were synthesized to determine the relative effect of chemical substitution in the 2-and 5-positions on broad spectrum antimicrobial activity. Each compound was evaluated quantitatively by calculation of a microbiocidal index, which measured the time to kill several different microorganisms. This test system indicated that 5-bromo-5-nitro substitution was essential for significant activity. Optimal activity was effected by 2-methyl substitution in the alkyl series and 2-hydroxy-phenyl substitution in the aryl series. The antimicrobial activity of the substituted dioxanes was not related directly to water solubility or hydrolysis to microbiocidal diols or aldehydes.
合成了5-硝基-1,3-二氧六环的各种衍生物，以确定2位和5位化学取代对广谱抗菌活性的相对影响。通过计算杀菌指数对每种化合物进行定量评估，该指数测量杀灭几种不同微生物的时间。该测试系统表明，5-溴-5-硝基取代对于显著活性至关重要。在烷基系列中，2-甲基取代以及在芳基系列中，2-羟基苯基取代可实现最佳活性。取代二氧六环的抗菌活性与水溶性或水解为杀菌二醇或醛没有直接关系。
