3-Alkylthio-1,2,4-triazine dimers with potent antimalarial activity

被引：51

作者：

Ban, Kung ^{[1
]}

Duffy, Sandra ^{[2
]}

Khakham, Yelena ^{[1
]}

Avery, Vicky M. ^{[2
]}

Hughes, Andrew ^{[3
]}

Montagnat, Oliver ^{[4
]}

Katneni, Kasiram ^{[4
]}

Ryan, Eileen ^{[4
]}

Baell, Jonathan B. ^{[1
]}

机构：

[1] Royal Melbourne Hosp, Walter & Eliza Hall Inst Med Res, Parkville, Vic 3050, Australia

[2] Griffith Univ, Eskitis Inst Cell & Mol Therapies, Nathan, Qld 4111, Australia

[3] La Trobe Univ, Bundoora, Vic, Australia

[4] Monash Univ, Monash Inst Pharmaceut Sci, Ctr Drug Candidate Optimisat, Clayton, Vic 3800, Australia

来源：

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

基金：

澳大利亚国家健康与医学研究理事会;

关键词：

Plasmodium falciparum; Malaria; Triazenes; 1,2,4-TRIAZINES;

D O I：

10.1016/j.bmcl.2010.08.065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report on the discovery of 3-alkylthio-1,2,4-triazine dimers that are potently toxic to Plasmodium falciparum, with single digit nanomolar activity, and up to several thousand-fold lower toxicity to mammalian cells. They are equipotent against chloroquine-resistant strains of P. falciparum. (c) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6024 / 6029

页数：6

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