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

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

  • Bioorg Med Chem Lett. 2022 Feb 15:58:128521. doi: 10.1016/j.bmcl.2021.128521.
Marta Jędrzejczyk 1,  Natalia Stępczyńska 1,  Greta Klejborowska 1,  Małgorzata Podsiad 2,  Joanna Stefańska 3,  Dietmar Steverding 4,  Adam Huczyński 5
Affiliations

Affiliations

  • 1 Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
  • 2 Chair and Department of Biochemistry, Medical University of Warsaw, Banacha 1, 02-097 Warsaw, Poland.
  • 3 Department of Pharmaceutical Microbiology, Centre for Preclinical Research, Medical University of Warsaw, Banacha 1b, 02-097 Warsaw, Poland.
  • 4 Bob Champion Research and Education Centre, Norwich Medical School, University of East Anglia, Norwich, United Kingdom.
  • 5 Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland. Electronic address: adhucz@amu.edu.pl.
PMID: 34968675 DOI: 10.1016/j.bmcl.2021.128521
Abstract

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.

Keywords

Antimicrobial activity; Antiparasitic activity; Natural products; Polyether ionophores.

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