Asymmetric total synthesis of B-ring modified (−)-epicatechin gallate analogues and their modulation of β-lactam resistance in Staphylococcus aureus |
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Authors: | James C. Anderson Catherine Headley Peter W. Taylor |
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Affiliation: | a School of Chemistry, University of Nottingham, Nottingham, NG7 2RD, UK b Microbiology Group, School of Pharmacy, University of London, 29-39 Brunswick Square, London, WC1, 1AX, UK |
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Abstract: | Two enantiomerically pure B-ring modified analogues of (−)-epicatechin gallate were synthesised and their modulation of β-lactam resistance using three strains of methicillin resistant Staphylococcus aureus (BB 568, EMRSA-15 and EMRSA-16) evaluated. Sub-inhibitory concentrations (12.5 and 25 mg/L) of the two analogues fully sensitised each of the three MRSA strains to oxacillin, reducing the MIC to less than 0.5 mg/L, identical to levels achieved with ECg. Lower concentrations demonstrated that the position and degree of hydroxylation of the B-ring is important for activity. |
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Keywords: | Epicatechin gallate Asymmetric synthesis Oxacillin MRSA |
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