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

3-Alkylthio-1,2,4-triazine dimers with potent antimalarial activity
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DOI:
10.1016/j.bmcl.2010.08.065
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发表时间:
2010-10-15
影响因子:
2.7
通讯作者:
Baell, Jonathan B.
Baell, Jonathan B.
中科院分区:
医学4区
文献类型:
--
作者:
Ban, Kung;Duffy, Sandra;Baell, Jonathan B.

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我们报告的发现3-烷硫基-1,2,4-三嗪二聚体,是恶性疟原虫,具有单位数纳摩尔活性的潜在毒性,并高达几千倍的哺乳动物细胞的毒性低。它们对恶性疟原虫的氯喹抗性株具有同等效力。(c)2010爱思唯尔有限公司版权所有。
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.