Auranofin and its Analogues Show Potent Antimicrobial Activity against Multidrug-Resistant Pathogens: Structure-Activity Relationships.
Tiziano MarzoDamiano CirriSimona PolliniMarco PratoStefania FallaniMaria Iris CassettaAndrea NovelliGian Maria RossoliniLuigi MessoriPublished in: ChemMedChem (2018)
Due to the so-called "antibiotic resistance crisis" new antibacterial agents are urgently sought to treat multidrug-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-[Au(PEt3 )2 ]Cl, K[Au(CN)2 ] and [Ag(PEt3 )2 ]NO3 -were prepared and comparatively tested with auranofin on a representative panel of pathogens including Gram-positive, Gram-negative and Candida strains. Interestingly, all the gold and silver complexes tested were active on Gram-positive strains, with the gold complexes having greater efficacy. The effects of the gold compounds were potentiated to a larger extent than silver compounds when tested in combination with a permeabilizing agent. A number of relevant structure-activity relationships emerged from the comparative analysis of the observed antibacterial profiles, shedding new light on the underlying molecular mechanisms of the action of these compounds.
Keyphrases
- gram negative
- silver nanoparticles
- multidrug resistant
- drug resistant
- acinetobacter baumannii
- sensitive detection
- pet ct
- computed tomography
- positron emission tomography
- klebsiella pneumoniae
- gold nanoparticles
- escherichia coli
- quantum dots
- reduced graphene oxide
- visible light
- pet imaging
- public health
- cross sectional
- molecular docking
- candida albicans
- anti inflammatory
- biofilm formation
- pseudomonas aeruginosa
- human milk
- preterm infants
- low birth weight
- wound healing
- preterm birth