In Vitro and In Vivo Evaluation of 28DAP010, a Novel Diamidine for Treatment of Second-Stage African Sleeping Sickness

摘要: African sleeping sickness is a neglected tropical disease transmitted by tsetse flies. New and better drugs are still needed especially for its second stage, which fatal if untreated. 28DAP010, dipyridylbenzene analogue of DB829, the simple diamidine found to cure mice with central nervous system infections parenteral route administration. 28DAP010 showed efficacy similar that DB829 in dose-response studies mouse models first- second-stage sickness. The vitro time kill, determined microcalorimetry, parasite clearance were shorter than DB829. No cross-resistance was observed between pentamidine on tested Trypanosoma brucei gambiense isolates from melarsoprol-refractory patients. promising preclinical candidate among diamidines treatment