Synthesis and biological investigation of new 4"-malonyl tethered derivatives of erythromycin and clarithromycin

被引：10

作者：

Sherman, D

Xiong, LQ

Mankin, AS

Melman, A ^{[1
]}

机构：

[1] Hebrew Univ Jerusalem, Dept Organ Chem, IL-91904 Jerusalem, Israel

[2] Univ Illinois, Ctr Pharmaceut Biotechnol, Chicago, IL 60607 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 06期

关键词：

macrolides; ribosome; antibiotics; tethering;

D O I：

10.1016/j.bmcl.2005.12.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new approach to 4 ''-substituted derivatives of erythromycin and clarithromycin was developed by converting them into corresponding 4"-malonic monoesters. Subsequent carbodiimide coupling with alcohols and amines provided new macrolide derivatives that are capable of binding to 50S ribosomal subunits and inhibiting protein synthesis in cell-free system. (C) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1506 / 1509

页数：4

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