Molecular Periphery Design Allows Control of the New Nitrofurans Antimicrobial Selectivity
Lyubov Vinogradova, Alexey Lukin, Kristina Komarova, Maxim Zhuravlev, Artem Fadeev, Mikhail Chudinov, Elizaveta Rogacheva, Lyudmila Kraeva, Maxim Gureev, Yuri Porozov, Marine Dogonadze, Tatiana Vinogradova
TL;DR
Researchers designed new nitrofuran compounds with controlled antimicrobial selectivity, showing strong activity against ESKAPE bacteria and tuberculosis.
Contribution
The study introduces a molecular periphery design strategy to enhance antimicrobial selectivity and efficacy of new nitrofuran derivatives.
Findings
Some compounds showed similar or lower MICs against ESKAPE pathogens compared to standard antibiotics.
Compound 2h inhibited S. aureus more effectively than ciprofloxacin, nitrofurantoin, and furazidin.
Compound 2e was active against Gram-positive ESKAPE pathogens and M. tuberculosis.
Abstract
A series of 13 new 3-substituted 5-(5-nitro-2-furyl)-1,2,4-oxadiazoles was synthesized from different aminonitriles. All compounds were screened in the disc diffusion test at a 100 μg/mL concentration to determine the bacterial growth inhibition zone presence and diameter, and then the minimum inhibitory concentrations (MICs) were determined for the most active compounds by serial dilution. The compounds showed antibacterial activity against ESKAPE bacteria, predominantly suppressing the growth of 5 species out of the panel. Some compounds had similar or lower MICs against ESKAPE pathogens compared to ciprofloxacin, nitrofurantoin, and furazidin. In particular, 3-azetidin-3-yl-5-(5-nitro-2-furyl)-1,2,4-oxadiazole (2h) inhibited S. aureus at a concentration lower than all comparators. Compound 2e (5-(5-nitro-2-furyl)-3-[4-(pyrrolidin-3-yloxy)phenyl]-1,2,4-oxadiazole) was active against…
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Taxonomy
TopicsBioactive Compounds and Antitumor Agents · Synthesis and Biological Evaluation · Antimicrobial Peptides and Activities