CT3

CT3 is a cyanotriazole antiparasitic.1 It is active against T. b. brucei, T. b. gambiense, T. b. rhodesiense, T. cruzi, and L. donovani (EC50s = 180, 31, 57, 78, and 134 nM, respectively). CT3 (4 µM) inhibits nuclear, but not kinetoplastid, DNA replication in the bloodstream form of T. b. brucei. It inhibits T. cruzi topoisomerase II but not human topoisomerase II-α. CT3 (30 mg/kg per day for five days) eradicates T. cruzi in a mouse model of Chagas disease. It also eradicates the T. b. brucei strain STIB975 at stage I and stage II in a mouse model of African trypanosomiasis when administered at a dose of 10 mg/kg for four or seven days, respectively.