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
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
收藏
页码:4934 / 4937
页数:4
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