期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 58, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128521
关键词
Antimicrobial activity; Antiparasitic activity; Natural products; Polyether ionophores
This study presents the synthesis and biological evaluation of eleven derivatives of the natural polyether ionophore monensin A, modified at the C-26 position. These derivatives showed varying degrees of antimicrobial and antiparasitic activity. One phenyl urethane derivative exhibited the most promising antibacterial activity.
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 mu g/ml. In contrast, none of the MON derivatives displayed higher antitrypanosomal activity than the unmodified ionophore.
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