Sovari, Sara Nasiri Vojnovic, Sandra Bogojevic, Sanja Skaro Crochet, Aurélien Pavic, Aleksandar Nikodinovic-Runic, Jasmina Zobi, Fabio 2020-11-01 We have prepared a series of ten 3-arylcoumarin molecules, their respective fac- [Re(CO)3(bpy)L]+ and fac-[Re(CO)3(L⁀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 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. application/pdf https://folia.unifr.ch/global/documents/308825 https://folia.unifr.ch/documents/308825/files/zob_dsv.pdf https://folia.unifr.ch/documents/308825/files/zob_dsv_sm.pdf eng info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejmech.2020.112533 info:eu-repo/semantics/openAccess License undefined European Journal of Medicinal Chemistry. - 2020, vol. 205, p. 112533 info:eu-repo/classification/udc/54 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) http://purl.org/coar/resource_type/c_6501