Characterization of a melamino nitroheterocycle as a potential lead for the treatment of human african trypanosomiasis.

ABSTRACT: This paper reports an evaluation of a melamino nitroheterocycle, a potential lead for further development as an agent against human African trypanosomiasis (HAT). Studies on its efficacy, physicochemical and biopharmaceutical properties, and potential for toxicity are described. The compound previously had been shown to possess exceptional activity against Trypanosoma brucei in in vitro assays comparable to that of melarsoprol. Here, we demonstrate that the compound also was curative in the stringent acute mouse model T. brucei rhodesiense STIB 900 when given intraperitoneally at 40 mg/kg of body weight. Nevertheless, activity was only moderate when the oral route was used, and no cure was obtained when the compound was tested in a stage 2 rodent model of infection. Genotoxic profiling rev

SUBMITTER: Giordani F 

PROVIDER: S-EPMC4187918 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature