McLafferty M A, Koch R L, Goldman P
Antimicrob Agents Chemother. 1982 Jan;21(1):131-4. doi: 10.1128/AAC.21.1.131.
The kinetics of the lethal action of metronidazole and the formation of acetamide have been studied in a strain of Bacteroides fragilis which is relatively resistant to metronidazole. As with a susceptible strain of B. fragilis, the data are consistent with a model in which a labile intermediate in metronidazole metabolism interacts either with water to form acetamide or with a bacterium to cause its death. Although the relatively resistant strain grows more slowly than the susceptible one and is killed less rapidly by metronidazole, the resistant strain displays the same relationship between the lethal action of metronidazole and metronidazole metabolism to acetamide. The relatively resistant strain, like the susceptible one, has an enhanced lethal response to metronidazole in the presence of a strain of Escherichia coli. The results suggest that the proposed labile reactive intermediate of metronidazole forms more slowly in the resistant strains.
在一株对甲硝唑相对耐药的脆弱拟杆菌中,研究了甲硝唑致死作用的动力学以及乙酰胺的形成。与敏感的脆弱拟杆菌菌株一样,数据符合这样一个模型:甲硝唑代谢过程中的不稳定中间体要么与水反应形成乙酰胺,要么与细菌相互作用导致其死亡。尽管相对耐药的菌株生长速度比敏感菌株慢,且被甲硝唑杀死的速度也较慢,但耐药菌株在甲硝唑的致死作用与甲硝唑代谢为乙酰胺之间表现出相同的关系。与敏感菌株一样,在存在大肠杆菌菌株的情况下,相对耐药的菌株对甲硝唑的致死反应增强。结果表明,所提出的甲硝唑不稳定反应中间体在耐药菌株中形成得更慢。