Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo

被引：21

作者：

Blackie, Margaret A. L. ^{[1
]}

Yardley, Vanessa ^{[2
]}

Chibale, Kelly ^{[1
,3
]}

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa

[2] Univ London London Sch Hyg & Trop Med, Dept Infect & Trop Dis, London WC1E 7HT, England

[3] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

Antiplasmodial; Biological activity; Bioorganic chemistry; Chloroquine analogue; Ferroquine; CHLOROQUINE; FERROQUINE; MECHANISM; ANALOGS;

D O I：

10.1016/j.bmcl.2009.12.030

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The in vivo efficacy of PQ, and salts thereof, have been determined in Plasmodium berghei ANKA and Plasmodium yoelii. Phenylequine hydrochloride has shown an ED50 of 0.81 in P. yoelii (cf chloroquine ED50 = 1.31). (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1078 / 1080

页数：3

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