Synthesis and evaluation of antibacterial and trypanocidal activity of derivatives of monensin A

Marta Jędrzejczyk, Natalia Stępczyńska, Greta Klejborowska, Małgorzata Podsiad, Joanna Stefańska, Dietmar Steverding, Adam Huczyński

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The synthesis and biological evaluation of eleven derivatives of the natural polyether ionophore monensin A (MON), modified at the C-26 position, is presented. Eight urethane and three ester derivatives were tested for their antimicrobial activity against different strains of Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Pseudomonas aeruginosa. In addition, their antiparasitic activity was also evaluated with bloodstream forms of Trypanosoma brucei. The majority of the modified ionophores were active against a variety of Gram-positive bacterial strains, including methicillin-resistant S. epidermidis, and showed better antibacterial activity than the unmodified MON. The phenyl urethane derivative of MON exhibited the most promising antibacterial activity of all tested compounds, with minimal inhibitory concentration values of 0.25-0.50 μg/ml. In contrast, none of the MON derivatives displayed higher antitrypanosomal activity than the unmodified ionophore.
Original languageEnglish
Article number128521
JournalBioorganic & Medicinal Chemistry Letters
Early online date27 Dec 2021
Publication statusPublished - 15 Feb 2022

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