Walter & Eliza Hall Institute of Medical Research, Parkville, Victoria, Australia.
Bioorg Med Chem Lett. 2010 Oct 15;20(20):6024-9. doi: 10.1016/j.bmcl.2010.08.065. Epub 2010 Aug 19.
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.
我们报告了 3-烷基硫代-1,2,4-三嗪二聚体的发现,这些二聚体对恶性疟原虫具有很强的毒性,活性达到纳摩尔级,对哺乳动物细胞的毒性低几千倍。它们对耐氯喹的恶性疟原虫菌株具有同等的效力。