Researchers from several countries have turned hazardous pesticides into a means of fighting resistant bacteria. Its effectiveness is comparable to that of modern antibiotics.
N-Aryl-C-nitroazoles are an important class of heterocyclic compounds. They are used as pesticides and fungicides. However, these substances are toxic to humans and cause mutations. Researchers have repeatedly suggested that these groups of compounds may help fight pathogenic bacteria. However, a great deal of molecular work is needed to reduce toxicity.
Now an international team of researchers, including scientists from Russia, have been able to establish that when processed, the compounds can fight against drug-sensitive strains of tuberculosis pathogens. At the same time, they were powerless against strains of pathogens included in the ESKAPE group (an abbreviation of the names of the types of bacteria that most often develop resistance to antibiotics: Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginogenes and Enterobacter).
After that, the researchers modified the compound again and built two isomeric (identical in atomic arrangement) series of substances. The amino side groups have changed their position to make the aromatic nucleus of the nitrogen-rich substance more compact, thus reducing the toxicity of the substance. In this case, the sensitivity of microorganisms to the new compound was tested by the disk-diffusion method.
It turned out that the representatives of the ESKAPE group were easily suppressed by the new substances. The minimum concentration of a chemical compound that prevents visible growth of bacteria or bacteria (μg / ml) for the test substance shows a result comparable to the antibiotic ciprofloxacin. For example, enterococcus requires 0.3 μg / ml of an antibiotic or 2 μg / ml of one of the new substances. At the same time, M. Tuberculosis, which was initially damaged by OTB-021 pyrimidine, turned out to be completely insensitive to new substances.