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

Jędrzejczyk, Marta, Stępczyńska, Natalia, Klejborowska, Greta, Podsiad, Małgorzata, Stefańska, Joanna, Steverding, Dietmar and Huczyński, Adam (2022) Synthesis and evaluation of antibacterial and trypanocidal activity of derivatives of monensin A. Bioorganic & Medicinal Chemistry Letters, 58. ISSN 0960-894X

[img] PDF (Accepted_Mnauscript) - Accepted Version
Restricted to Repository staff only until 27 December 2022.
Available under License Creative Commons Attribution Non-commercial No Derivatives.

Request a copy

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.

Item Type: Article
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 05 Jan 2022 12:31
Last Modified: 24 May 2022 14:46
URI: https://ueaeprints.uea.ac.uk/id/eprint/82894
DOI: 10.1016/j.bmcl.2021.128521

Actions (login required)

View Item View Item