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Manuscript_Nasiri et al_FZ_ESI.pdf (4.55 MB)

Design, Synthesis and in Vivo Evaluation of 3-Arylcoumarin Derivatives of rhenium(I) Tricarbonyl Complexes as Potent Antibacterial Agents Against Methicillin-Resistant Staphylococcus Aureus (MRSA)

submitted on 21.04.2020, 16:02 and posted on 23.04.2020, 21:51 by Sara Nasiri Sovari, Sandra Vojnovic, Sanja Skaro Bogojevic, Aurélien Crochet, Aleksandar Pavic, Jasmina Nikodinovic-Runic, Fabio Zobi

Preparation of a series of ten 3-arylcoumarin molecules, their respective fac-[Re(CO)3(bpy)L]+ and fac-[Re(CO)3(L⁀L)Br] complexes. All compounds were tested for their antimicrobial efficacy. Whereas the 3-arylcoumarin ligands are virtually inactive against the human-associated pathogens with minimum inhibitory concentrations (MICs) > 150 µM, 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.


University of Fribourg

Ministry of Education, Science and Technological Development of the Republic of Serbia (Grant No. 173048)


Email Address of Submitting Author


Université de Fribourg



ORCID For Submitting Author


Declaration of Conflict of Interest

No conflict of interest