In Vitro and In Vivo Studies of the Trypanocidal Activity of a Diarylthiophene Diamidine against Trypanosoma cruzi

摘要: Aromatic diamidines are DNA minor groove-binding ligands that display excellent antimicrobial activity against fungi, bacteria, and protozoa. Due to the currently unsatisfactory chemotherapy for Chagas' disease in view of our previous reports regarding effect analogues both vitro vivo Trypanosoma cruzi infection, this study evaluated effects a diarylthiophene diamidine (DB1362) amastigotes bloodstream trypomastigotes T. cruzi, etiological agent disease. The data show potent DB1362 parasite forms relevant mammalian infection at doses which do not exhibit cytotoxicity. Ultrastructural analysis flow cytometry studies striking alterations nuclei mitochondria parasites. In were performed two different drug concentrations (25 50 mg/kg/day) using 2-day or 10-day regimen. best results obtained when acutely infected mice treated with lower concentration, resulting 100% survival, compared untreated mice. Although it did higher efficacy than benznidazole, reduced cardiac parasitism inflammation, addition, protected (determined by measurements) common infection. These support further investigation related compounds as potential agents