Inhibition of nucleic acid and protein synthesis in Escherichia coli by a new triazenomidazole.

Abstract

Methyl S (or 4) - (3,3 - dimethyl −1 - triazeno) imidazole-4 (or 5)-carboxylate(1), designated NSC 87982 by the Cancer Chemotherapy National Service Center, National Cancer Institute, National Institutes of Health, has been reported to be a potent inhibitor of Gram-positive and Gram-negative bacteria, yeasts, filamentous fungi and algae in vitro and to protect mice against an experimental infection of Staphylococcus aureus (2). Microbiological assay of various mouse tissues indicates that not only are significantly high blood levels obtained following oral, intraperitoneal, or intravenous administration of the drug, but also that detectable concentrations of NSC 87982 are found in the brain and other organs of the mice(3). The broad-spectrum antimicrobial activity of NSC 87982 and the knowledge that it is being considered for clinical trial prompted a study of the mechanism of action of this compound.Materials and methods. The inhibitory activity of NSC 87982 against numerous strains of Escherichia coli a...