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

Kung Ban; Sandra Duffy; Yelena Khakham; Vicky M Avery; Andrew Hughes; Oliver Montagnat; Kasiram Katneni; Eileen Ryan; Jonathan B Baell

doi:10.1016/j.bmcl.2010.08.065

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

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6024-9. doi: 10.1016/j.bmcl.2010.08.065. Epub 2010 Aug 19.

Authors

Kung Ban¹, Sandra Duffy, Yelena Khakham, Vicky M Avery, Andrew Hughes, Oliver Montagnat, Kasiram Katneni, Eileen Ryan, Jonathan B Baell

Affiliation

¹ Walter & Eliza Hall Institute of Medical Research, Parkville, Victoria, Australia.

PMID: 20822904
DOI: 10.1016/j.bmcl.2010.08.065

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antimalarials / chemical synthesis
Antimalarials / chemistry*
Antimalarials / metabolism
Antimalarials / pharmacology*
Cell Line
Cell Survival
Humans
Malaria, Falciparum / drug therapy
Microsomes, Liver / metabolism
Plasmodium falciparum / drug effects*
Triazines / chemical synthesis
Triazines / chemistry*
Triazines / metabolism
Triazines / pharmacology*

Substances

Antimalarials
Triazines
1,2,4-triazine