| Author | Silva, C. F. | |
| Author | Batista, Marcos Meuser | |
| Author | Mota, Renata Alves | |
| Author | Souza, Elen Mello de | |
| Author | Stephens, Chad E. | |
| Author | Som, Phanneth | |
| Author | Boykin, David Wilson | |
| Author | Soeiro, Maria de Nazare C. | |
| Access date | 2020-02-06T17:03:34Z | |
| Available date | 2020-02-06T17:03:34Z | |
| Document date | 2007 | |
| Citation | SILVA, C. F. et al. Activity of ‘‘reversed’’ diamidines against Trypanosoma cruzi ‘‘in vitro’’. Biochemical Pharma, v. 73, p. 1939-1946, 2007. | pt_BR |
| ISSN | 0006-2952 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/39788 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Trypanosoma cruzi | pt_BR |
| Subject in Portuguese | Doença de Chagas | pt_BR |
| Subject in Portuguese | Quimioterapia | pt_BR |
| Subject in Portuguese | Diamidinas invertidas | pt_BR |
| Title | Activity of ‘‘reversed’’ diamidines against Trypanosoma cruzi ‘‘in vitro’’ | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.bcp.2007.03.020 | |
| Abstract | Chagas’ disease is an important parasitic illness caused by the flagellated protozoan Trypanosoma cruzi. The disease affects nearly 17 million individuals in endemic areas of Latin America and the current chemotherapy is quite unsatisfactory based on nitroheterocyclic agents (nifurtimox and benznidazol). The need for new compounds with different modes of action is clear. Due to the broad-spectrum antimicrobial activity of the aromatic dicationic compounds, this study focused on the activity of four such diamidines (DB811, DB889, DB786, DB702) and a closely related diguanidine (DB711) against bloodstream trypomastigotes as well as intracellular amastigotes of T. cruzi in vitro. Additional studies were also conducted to access the toxicity of the compounds against mammalian cells in vitro. Our data show that the four diamidines compounds presented early and high antiparasitic activity (IC50 in low-micromolecular range) exhibiting trypanocidal dose-dependent effects against both trypomastigote and amastigote forms of T. cruzi 2 h after drug treatment. Most of the diamidines compounds (except the DB702) exerted high anti-parasitic activity and low toxicity to the mammalian cells. Our results show the activity of reversed diamidines against T. cruzi and suggested that the compounds merit in vivo studies. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil. | 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 | Georgia State University. Department of Chemistry. Atlanta, GA, USA. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Subject | Chagas disease | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Chemotherapy | pt_BR |
| e-ISSN | 1873-2968 | |
| Embargo date | 2025-01-01 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
