Reversal Agent and Linker Variants of Reversed Chloroquines: Activities against Plasmodium falciparum

被引：117

作者：

Andrews, Simeon ^{[1
]}

Burgess, Steven J. ^{[1
,2
]}

Skaalrud, Deborah ^{[1
]}

Kelly, Jane Xu ^{[1
,2
,3
]}

Peyton, David H. ^{[1
]}

机构：

[1] Portland State Univ, Dept Chem, Portland, OR 97207 USA

[2] DesignMedix Inc, Portland, OR 97201 USA

[3] Portland VA Med Ctr, Portland, OR 97239 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 02期

基金：

美国国家科学基金会; 美国国家卫生研究院;

关键词：

BETA-HEMATIN INHIBITION; DRUG-RESISTANCE; MALARIA; ANTIMALARIAL; COMBINATIONS; TRANSPORTER;

D O I：

10.1021/jm900972u

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have shown that "reversed chloroquine molecules" constructed from chloroquine-like and resistance "reversal-agent"-like cores can be powerful drugs against malaria (J. Med. Chem. 2006, 49, 5623-5625). Several reversed chloroquines are now presented that probe parameters governing the activities against chloroquine-resistant and chloroquine-sensitive malaria strains. The design is tolerant to linker and reversal agent changes, but it piperazinyl group adjacent to the quinoline, at least for the group Of Compounds studied here, may be detrimental.

引用

页码：916 / 919

页数：4

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