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      Antimicrobial properties of highly fluorinated tris(pyrazolyl)borates.

      Journal of Inorganic Biochemistry

      Anti-Infective Agents, chemistry, metabolism, pharmacology, Bacillus subtilis, drug effects, growth & development, Borates, Fluorine, Ligands, Microbial Sensitivity Tests, Pyrazoles, Silver Sulfadiazine, Staphylococcus aureus

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          Abstract

          Highly fluorinated tris(pyrazolyl)borates were tested for their antimicrobial activity against various bacterial species. Both the silver(I) tris(pyrazolyl)borate [HB(3,5-(CF(3))(2)Pz)(3)]Ag(THF) (THF=tetrahydrofuran) and the sodium analog [HB(3,5-(CF(3))(2)Pz)(3)]Na(THF) appeared highly effective at inhibiting the growth of two different species of Gram-positive bacteria (i.e. being 12 and 21 fold more effective, respectively, (on a molar basis, based on the minimum inhibitory concentrations) against Staphylococcus aureus than silver sulfadiazine, a currently used silver antimicrobial). This suggests that the ligand portion of these molecules is responsible for the observed high effectiveness against the Gram-positive species. Furthermore, it appeared that the fluorinated substituents on the tris(pyrazolyl)borate were important for this high level of growth inhibition. Against two species of Gram-negative bacteria, including Pseudomonas aeruginosa, the fluorinated silver(I) tris(pyrazolyl)borate exhibited a moderate level of growth inhibition (similar to that of silver sulfadiazine), while the sodium analog showed very little ability to inhibit growth, indicating that for the Gram-negative species, the apparent responsible antimicrobial portion is the silver ion.

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          Journal
          17586048
          10.1016/j.jinorgbio.2007.05.002

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