Reversed Chloroquines Based on the 3,4-Dihydropyrimidin-2(1H)-one Scaffold: Synthesis and Evaluation for Antimalarial, β-Haematin Inhibition, and Cytotoxic Activity

被引：43

作者：

October, Natasha ^{[1
]}

Watermeyer, Nicholas D. ^{[1
]}

Yardley, Vanessa ^{[3
]}

Egan, Timothy J. ^{[1
]}

Ncokazi, Kanyile ^{[1
]}

Chibale, Kelly ^{[1
,2
]}

机构：

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

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

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

来源：

CHEMMEDCHEM | 2008年 / 3卷 / 11期

关键词：

drug design; quinoline-containing antimalarials; dihydropyrimidinones; reversing agents; sensitizers;

D O I：

10.1002/cmdc.200800172

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Chemical Equation Presented) The synthesis, cytotoxicity, and antimalarial activity of resistance-reversing bifunctional dihydropyrimidone-chloroquinoline conjugates are reported herein. In vitro assay results indicate this class of compounds is highly active against both chloroquine-resistant and chloroquine-sensitive strains of P. falciparum. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：1649 / 1653

页数：5

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