Evaluating 5-nitrothiazoles as trypanocidal agents

Abstract

The growth inhibitory properties of a 5-nitrothiazole series was evaluated against Trypanosoma brucei. A subset of related compounds displayed the greatest potency towards the parasite while exhibiting little cytotoxic effect on mammalian cells, with this anti-parasitic activity being dependent on expression of a type I nitroreductase by the trypanosome. We conclude that the 5-nitrothiazole class of nitroheterocycle may represent new leads in the treatment of human African trypanosomiasis.