Résumé
Deharo, E., Loyevsky, M., John, C., Balanza, E., Ruiz, G., Muñoz, V., and Gordeuk, V. R. 2000. Aminothiol multidentate chelators against Chagas disease. Experimental Parasitology94, 198–200. Three compounds of an aminothiol family of iron chelators were examined for activity against trypomastigote (human) and epimastigote (vector) forms of Trypanosoma cruzi: tetraethyl and tetramethyl derivatives of ethane-1,2-bis (N-1-amino-3-ethyl butyl-3-thiol) (BAT-TE and BAT-TM) and N′,N′,N′-tris-(2-methyl-2-mercaptopriopyl)-1.4.7-triazacyclonane (TAT). BAT-TE at 270 μM completely arrested the growth of trypomastigote forms in mouse blood stored at 4°C for 24 h (IC50 67.7 ± 7 μM), while BAT-TM arrested growth at 630 μM (IC50 158 ± 17 μM) and TAT at concentrations >800 μM (IC50 415 ± 55 μM). In T. cruzi-infected mice, BAT-TE and BAT-TM had no anti-trypanosomal activity in doses up to 200 mg/kg, whether the route of administration was intraperitoneal or oral, and TAT was not tested due to insufficient quantity. TAT had an IC50 of 52 ± 7 μM against the epimastigote forms while BAT-TM and BAT-TE were inhibitory only at concentrations >250 μM. The trypanocidal activity of BAT derivatives in blood stored at 4°C makes these compounds potential candidates for the purpose of clearing donated blood of trypomastigotes.