| Author | Silva, Cristiane França Da | |
| Author | Junqueira, Angela | |
| Author | Lima, Marli Maria | |
| Author | Romanha, Alvaro José | |
| Author | Sales Junior, Policarpo Ademar | |
| Author | Stephens, Chad E. | |
| Author | Som, Phanneth | |
| Author | Boykin, David W. | |
| Author | Soeiro, Maria de Nazaré Correia | |
| Access date | 2014-10-21T17:16:20Z | |
| Available date | 2014-10-21T17:16:20Z | |
| Document date | 2011 | |
| Citation | SILVA, Cristiane França da et al. In vitro trypanocidal activity of DB745B and other novel arylimidamides against Trypanosoma cruzi. Journal of antimicrobial chemotherapy, 66(6): 1295-1297. | pt_BR |
| ISSN | 0305-7453 | |
| URI | https://www.arca.fiocruz.br/handle/icict/8644 | |
| Language | eng | pt_BR |
| Publisher | Academic Press. | pt_BR |
| Rights | open access | pt_BR |
| Title | In vitro trypanocidal activity of DB745B and other novel arylimidamides against Trypanosoma cruzi | pt_BR |
| Type | Article | pt_BR |
| Abstract | OBJECTIVES: As part of a search for new therapeutic 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. cruzi was 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 to0.2 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. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Doenças Parasitárias Rio de Janeiro, RJ, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz, Laboratório de Eco-epidemiologia da doença de Chagas. Rio de Janeiro, RJ, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brazil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Parasitologia Celular e Molecular. Belo Horizonte, MG, Brazil | pt_BR |
| Affilliation | Augusta State University. Department of Chemistry and Physics Augusta, GA, USA | pt_BR |
| Affilliation | Georgia State University. Department of Chemistry. Atlanta, GA, USA | pt_BR |
| Affilliation | Georgia State University. Department of Chemistry. Atlanta, GA, USA | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brazil | pt_BR |
| Subject | Trypanosoma cruzi/drug effects | pt_BR |
| Subject | Antiprotozoal Agents/toxicity | pt_BR |
| Subject | Cell Survival/drug effects | pt_BR |
| Subject | Parasitic Sensitivity Tests | pt_BR |
