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.
2018
13
2448
2454
Tiziano Marzo, Damiano Cirri, Simona Pollini, Marco Prato, Stefania Fallani, Maria Iris Cassetta, Andrea Novelli, Gian Maria Rossolini, Luigi Messori
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1140129
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