Browsing by Autor "Deharo, Eric"

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    Aminothiol multidentate chelators against Chagas disease
    (Facultad de Medicina, Enfermería, Nutrición y Tecnología Médica, 2000) Deharo, Eric
    Abstract 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 4º C for 24 h (IC(50) 67.7+/-7 µM), while BAT-TM arrested growth at 630 µM (IC(50) 158+/-17 µM) and TAT at concentrations >800 µM (IC(50) 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 IC(50) 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 4º C makes these compounds potential candidates for the purpose of clearing donated blood of trypomastigotes.