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

被引：32

作者：

Anderson, JC ^{[1
]}

Headley, C

Stapleton, PD

Taylor, PW

机构：

[1] Univ Nottingham, Sch Chem, Nottingham NG7 2RD, England

[2] Univ London, Sch Pharm, Microbiol Grp, London WC1N 1AX, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 10期

基金：

英国医学研究理事会;

关键词：

MRSA; (-)-epicatechingallate analogues; beta-lactam antibiotics;

D O I：

10.1016/j.bmcl.2005.03.063

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2633 / 2635

页数：3

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