Hof H, Chakraborty T, Royer R, Buisson J P
Institute of Hygiene and Microbiology, University of Würzburg, FRG.
Drugs Exp Clin Res. 1987;13(10):635-9.
The inhibitory and bactericidal activities of several different nitro-heterocyclic compounds, such as nitrofuran, nitronaphthofuran, nitrobenzofuran, nitroimidazole and nitrothiazole, were assessed in vitro. All these substances except nitroimidazole were active against Escherichia coli, though to different degrees. Under anaerobic test conditions the antibacterial activity increased slightly. Nitroreductase-deficient mutants, however, were highly resistant to all nitro-compounds, indicating that only when the nitro-group is reduced to these agents get into an active antibacterial form. SOS repair-deficient strains were much more susceptible to the nitro-containing substances than repair-proficient counterparts, indicating that damage to bacterial DNA is the essential mechanism of antibacterial activity of all nitro-heterocyclic compounds.
在体外评估了几种不同的硝基杂环化合物，如硝基呋喃、硝基萘并呋喃、硝基苯并呋喃、硝基咪唑和硝基噻唑的抑制和杀菌活性。除硝基咪唑外，所有这些物质对大肠杆菌均有活性，只是程度不同。在厌氧测试条件下，抗菌活性略有增加。然而，硝基还原酶缺陷型突变体对所有硝基化合物都具有高度抗性，这表明只有当硝基被还原时，这些药物才会转变为具有活性的抗菌形式。与修复功能正常的菌株相比，SOS修复缺陷型菌株对含硝基物质更为敏感，这表明细菌DNA损伤是所有硝基杂环化合物抗菌活性的基本机制。
