Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 205, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112533
Keywords
Rhenium(I) tricarbonyl complex; Antibiotic; MRSA; Staphylococcus aureus
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Funding
- University of Fribourg
- Ministry of Education, Science and Technological Development of the Republic of Serbia [173048]
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We have prepared a series of ten 3-arylcoumarin molecules, their respective fac-[Re(CO)(3)(bpy)L](+) and fac-[Re(CO)(3)(L(sic)L)Br] complexes and tested all compounds for their antimicrobial efficacy. Whereas the 3-arylcoumarin ligands are virtually inactive against the human-associated pathogens with minimum inhibitory concentrations (MICs) > 150 mu M, when coordinated to the fac-[Re(CO)(3)](+) core, most of the resulting complexes showed remarkable antibacterial potency. Several rhenium complexes exhibit activity in nanomolar concentrations against Gram-positive pathogens such as Staphylococcus aureus strains, including methicillin-resistant S. aureus (MRSA) and Enterococcus faecium. The molecules do not affect bacterial cell membrane potential, but some of the most potent complexes strongly interact with DNA, indicating it as a possible target for their mode of action. In vivo studies in the zebrafish model showed that the complexes with anti-staphylococcal/MRSA activity were non-toxic to the organism even at much higher doses of the corresponding MICs. In the zebrafish-MRSA infection model, the complexes increased the survival rate of infected fish up to 100% and markedly reduced bacterial burden. Moreover, all rescued fish developed normally following the treatments with the metallic compounds. (C) 2020 The Authors. Published by Elsevier Masson SAS.
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