B 环修饰的 (-)-表儿茶素没食子酸酯类似物的不对称全合成及其对金黄色葡萄球菌β-内酰胺抗性的调节作用
Asymmetric total synthesis of B-ring modified (-)-epicatechin gallate analogues and their modulation of beta-lactam resistance in Staphylococcus aureus.
作者信息
Anderson James C, Headley Catherine, Stapleton Paul D, Taylor Peter W
机构信息
School of Chemistry, University of Nottingham, Nottingham, NG7 2RD, UK.
出版信息
Tetrahedron. 2005 Aug 8;61(32):7703-7711. doi: 10.1016/j.tet.2005.05.086.
Two enantiomerically pure B-ring modified analogues of (-)-epicatechin gallate were synthesised and their modulation of beta-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.
合成了（-）-表儿茶素没食子酸酯的两种对映体纯的B环修饰类似物，并使用三株耐甲氧西林金黄色葡萄球菌（BB 568、EMRSA - 15和EMRSA - 16）评估了它们对β-内酰胺抗性的调节作用。两种类似物的亚抑制浓度（12.5和25 mg/L）使三种MRSA菌株中的每一种对苯唑西林完全敏感，将最低抑菌浓度降低至低于0.5 mg/L，与表儿茶素没食子酸酯所达到的水平相同。较低浓度表明B环的羟基化位置和程度对活性很重要。
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