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

…, Y Khakham, VM Avery, A Hughes, O Montagnat…

Index: Ban, Kung; Duffy, Sandra; Khakham, Yelena; Avery, Vicky M.; Hughes, Andrew; Montagnat, Oliver; Katneni, Kasiram; Ryan, Eileen; Baell, Jonathan B. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 20 p. 6024 - 6029

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Citation Number: 15

Abstract

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.