- Novel fluorescent cephalosporins: Synthesis, antimicrobial activity and photodynamic inactivation of antibiotic resistant bacteria
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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.
- Xiao, Jian-Min,Feng, Lei,Zhou, Li-Sheng,Gao, Hui-Zhou,Zhang, Yi-Lin,Yang, Ke-Wu
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p. 150 - 159
(2013/03/13)
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- Design and synthesis of a β-lactamase activated 5-fluorouracil prodrug
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An efficient synthesis of a 5-fluorouracil-cephalosporin prodrug is described for use against colorectal and other cancers in antibody and gene-directed therapies. The compound shows stability in aqueous media until specifically activated by β-lactamase (
- Phelan, Ryan M.,Ostermeier, Marc,Townsend, Craig A.
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scheme or table
p. 1261 - 1263
(2009/08/07)
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