کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1394412 | 1501157 | 2013 | 10 صفحه PDF | دانلود رایگان |
Two novel fluorescent cephalosporins, TCA and TBCA, were synthesized and characterized by 1H NMR, 13C NMR, UV–vis, and fluorescence spectroscopies. Biological activity assays demonstrated that TCA inactivated a Klebsiella pneumonia strain that expressed extended-spectrum β-lactamases. Incubation of 6 μM TCA with K. pneumonia cultures resulted in cell death for 84% of the cells after 126 J/cm2 of light irradiation. In vitro, TCA exhibited a MIC = 0.5 μg/mL with Staphylococcus aureus. Kinetic evaluation revealed that TCA and TBCA were substrates for B1 and B3 subclass metallo-β-lactamases. TBCA exhibited stronger binding affinities to the Gram-positive bacterial strains MRSA1, MRSA2, and S. aureus with value of 2.95–6.59 μM per 108 cells/mL.
Photoinactivation of novel fluorescent cephalosporin TCA against K. pneumonia and fluorescence imaging of TBCA with Gram-positive bacterial strains MRSA2.Figure optionsDownload as PowerPoint slideHighlights
► Two novel fluorescent cephalosporins TCA and TBCA were designed and characterized.
► TCA exhibited photoinactivation of K. pneumonia & antimicrobial effect for S. aureus.
► TBCA could label Gram-positive bacterial strains MRSA1, MRSA2 and S. aureus.
Journal: European Journal of Medicinal Chemistry - Volume 59, January 2013, Pages 150–159