Antibacterial activity of singly and doubly modified salinomycin derivatives

Bioorganic & Medicinal Chemistry Letters
Michał SulikMichał Antoszczak

Abstract

The increasing challenge of antibiotic resistance stimulates the search for novel antibacterial agents, especially such that would be effective against multi-drug resistant bacterial strains. Fortunately, natural compounds are excellent sources of potentially new drug leads. Particularly interesting in this context are polyether antibiotic salinomycin (SAL) and its semi-synthetic derivatives, as they exhibit large spectrum of bioactivity. We synthesized and evaluated the antibacterial activity of a series of SAL analogs; four singly (2-3, 15, 17) and two doubly modified (16, 18) derivatives were found to show excellent inhibitory activity not only against planktonic Gram(+) bacterial cells, but also towards select strains of methicillin-resistant staphylococci with the MIC values of 1-4 µg mL-1. Of note, the most promising candidates were more effective in preventing bacterial biofilm formation than unmodified SAL and a commonly used antibiotic - ciprofloxacin. Furthermore, we proved that rational modification of C20 hydroxyl of SAL may reduce genotoxic properties of the obtained analogs. Mechanistically, the structure-activity relationship studies suggested that electroneutral transport mechanism could be beneficial in terms o...Continue Reading

Citations

Jul 16, 2020·Biomolecules·Michał SulikMichał Antoszczak
Jun 16, 2021·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Alicja UrbaniakAngus M MacNicol
Jul 16, 2021·European Journal of Pharmacology·Dominika CzerwonkaAdam Huczyński

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