Scientists in Russia Synthesize Variants of Toxic Pesticide That Are Effective Against ESKAPE Panel of Antibiotic-Resistant Bacteria; Human Toxicity May Be Reduced by Careful Optimization of Molecular Periphery Around Nitro Heteroaromatic “Warhead”

N-aryl-C-nitroazoles are an important class of heterocyclic compounds. They are used as pesticides and fungicides. However, these substances could be toxic to humans and cause mutations. As they are not frequently used, there is little data about them in the medicinal chemistry literature. However, it has been suggested recently that the groups of compounds that are traditionally avoided may help to fight pathogenic bacteria. Yet, to reduce toxic effects, a great amount of work must be carried out at the molecular level, accurate optimization of the molecular environment of the nitro-heteroaromatic "warhead.” The validity of this approach was demonstrated in the early 2000s through the development of anti-tuberculosis drugs delamanid and pretomanid, currently approved for medical use. They act like prodrugs, that is, the substance itself is inactive, but acquires effective new properties when it enters the human body. In terms of the new work described here, scientists from the Immanuel Kant Baltic Federal University in Kaliningrad, together with colleagues from St. Petersburg State University, the L. Pasteur Research Institute of Epidemiology and Microbiology, and the Research Institute of Phthisiopulmonology, all in St. Petersburg (photo), are looking for new effective antibacterial drugs, studying various nitrogen heteroaromatic compounds with a nitro group which might be used in medicine further. The compound OTB-021 was found to work well against drug-sensitive strains of tuberculosis pathogens, but was powerless against strains of pathogens that belong to the so-called ESKAPE panel.
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