In vitro trypanocidal activity of DB745B and other novel arylimidamides against Trypanosoma cruzi

Cristiane França da Silva, Angela Junqueira, Marli Maria Lima, Alvaro José Romanha, Policarpo Ademar Sales Junior, Chad E. Stephens, Phanneth Som, David W. Boykin, Maria de Nazaré Correia Soeiro

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13 Scopus citations

Abstract

Objectives: As part of a search for newtherapeutic opportunities to treat chagasic patients, in vitro efficacy studies were performed to characterize the activity of five novel arylimidamides (AIAs) against Trypanosoma cruzi. Methods: The trypanocidal effect against T. cruziwas evaluated by light microscopy through the determination of IC50 values. Cytotoxicity was determined by MTT assays against mouse cardiomyocytes. Results: Our data demonstrated the trypanocidal efficacy of these new compounds against bloodstream trypomastigotes and intracellular amastigotes, exhibiting IC50 values ranging from 0.015 to 2.5 and 0.02 to 0.2 μM, respectively. One of the compounds, DB745B, was also highly active against a broad panel of isolates, including those naturally resistant to benznidazole. DB745B showed higher in vitro efficacy than the reference drugs used to treat patients (benznidazole IC50=12.94 μM) and to prevent blood bank infection (gentian violet IC50=30.6 μM). Conclusions: AIAs represent promising new chemical entities against T. cruzi and are also potential trypanocidal agents to prevent transfusion-associated Chagas' disease.

Original languageEnglish (US)
Article numberdkr140
Pages (from-to)1295-1297
Number of pages3
JournalJournal of Antimicrobial Chemotherapy
Volume66
Issue number6
DOIs
StatePublished - Jun 1 2011

Keywords

  • Chagas' disease
  • Chemotherapy
  • T. cruzi

ASJC Scopus subject areas

  • Pharmacology
  • Microbiology (medical)
  • Pharmacology (medical)
  • Infectious Diseases

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    da Silva, C. F., Junqueira, A., Lima, M. M., Romanha, A. J., Sales Junior, P. A., Stephens, C. E., Som, P., Boykin, D. W., & de Nazaré Correia Soeiro, M. (2011). In vitro trypanocidal activity of DB745B and other novel arylimidamides against Trypanosoma cruzi. Journal of Antimicrobial Chemotherapy, 66(6), 1295-1297. [dkr140]. https://doi.org/10.1093/jac/dkr140