Due to the so called “antibiotic resistance crisis” new antibacterial agents are urgently sought to treat multi-resistant pathogens. A group of gold- or silver-based complexes, of general formula M(PEt3)X (with M=Au or Ag, and X=Cl, Br or I), alongside with three complexes bearing a positive or negative charge, i.e. [Au(PEt3)2]Cl, K[Au(CN)2] and [Ag(PEt3)2]NO3, have been prepared and comparatively tested with Auranofin (AF) toward a representative panel of pathogens including Gram-positive, Gram-negative and Candida strains. Interestingly, all tested gold and silver complexes are active on Gram-positive strains, with the gold complexes presenting a greater efficacy. The effects of the gold compounds are potentiated to a larger extent than silver compounds when tested in combination with a permeabilizing agent. A few relevant structure-activity relationships emerge from comparative analysis of the obtained antibacterial profiles shedding new light on the underlying molecular mechanisms.
Auranofin and its Analogues Show Potent Antimicrobial Activity Covering Multiresistant Pathogens: Structure-Activity Relationships / Tiziano Marzo, Damiano Cirri, Simona Pollini, Marco Prato, Stefania Fallani, Maria Iris Cassetta, Andrea Novelli, Gian Maria Rossolini, Luigi Messori. - In: CHEMMEDCHEM. - ISSN 1860-7179. - STAMPA. - 13:(2018), pp. 2448-2454. [10.1002/cmdc.201800498]
Auranofin and its Analogues Show Potent Antimicrobial Activity Covering Multiresistant Pathogens: Structure-Activity Relationships
Tiziano Marzo;Damiano Cirri;Simona Pollini;Marco Prato;Stefania Fallani;Maria Iris Cassetta;Andrea Novelli;Gian Maria Rossolini;Luigi Messori
2018
Abstract
Due to the so called “antibiotic resistance crisis” new antibacterial agents are urgently sought to treat multi-resistant pathogens. A group of gold- or silver-based complexes, of general formula M(PEt3)X (with M=Au or Ag, and X=Cl, Br or I), alongside with three complexes bearing a positive or negative charge, i.e. [Au(PEt3)2]Cl, K[Au(CN)2] and [Ag(PEt3)2]NO3, have been prepared and comparatively tested with Auranofin (AF) toward a representative panel of pathogens including Gram-positive, Gram-negative and Candida strains. Interestingly, all tested gold and silver complexes are active on Gram-positive strains, with the gold complexes presenting a greater efficacy. The effects of the gold compounds are potentiated to a larger extent than silver compounds when tested in combination with a permeabilizing agent. A few relevant structure-activity relationships emerge from comparative analysis of the obtained antibacterial profiles shedding new light on the underlying molecular mechanisms.File | Dimensione | Formato | |
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