Synthesis and antibacterial activity of hydrolytically stable (-)-epicatechin gallate analogues for the modulation of beta-lactam resistance in Staphylococcus aureus

合成水解稳定的(-)-表儿茶素没食子酸酯类似物及其抗菌活性,用于调节金黄色葡萄球菌的β-内酰胺类抗生素耐药性

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Abstract

Hydrolytically more stable analogues of (-)-epicatechin gallate (ECg) have been synthesised from ECg where an amine or amide function has been substituted for the ester linkage that joins the C-ring with the galloyl D-ring. Sub-inhibitory concentrations (25 mg/L) of the amide analogue 7, possessing the natural C-3 stereochemistry, were able to reduce the resistance to oxacillin of three strains of methicillin resistant Staphylococcus aureus (BB 568, EMRSA-15 and EMRSA-16) comparable to levels achieved with ECg.

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