Interaction of O-(undec-10-en)-yl-D-glucose derivatives with the Plasmodium falciparum hexose transporter (PfHT)

被引：12

作者：

Ionita, Marina

Krishna, Sanjeev

Leo, Pierre-Marc

Morin, Christophe

Patel, Asha Parbhu

机构：

[1] Univ Grenoble 1, CNRS UMR 5250, ICMG FR 2607, Dept Chim Mol,Serco, F-38041 Grenoble, France

[2] St Georges Univ London, Ctr Infect, Div Cellular & Mol Med, London SW17 0RE, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 17期

基金：

英国医学研究理事会;

关键词：

glucose; carbohydrate transporters; PfHT; inhibitors; malaria;

D O I：

10.1016/j.bmcl.2007.06.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

All-O-undec-en-10-yl derivatives Of D-glucose have been prepared and their affinities for the Plasmodium falciparum hexose transporter (PMT) determined; the O-2 derivative displays a good apparent affinity for PfHT (K-1 = 2 mu M) with no significant interaction with the mammalian transporter GLUT1. This selectivity points to position -2 of glucose as an appropriate substitution site for the development of inhibitors of P. falciparum glucose uptake. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4934 / 4937

页数：4

共 16 条

[1] Preparation of alkyl α- and β-D-glucopyranosides, thermotropic properties and X-ray analysis [J].