| Author | Souza, E. M. de | |
| Author | Silva, P. B. da | |
| Author | Nefertiti, A. S. G. | |
| Author | Ismail, M. A. | |
| Author | Arafa, R. K. | |
| Author | Tao, B | |
| Author | Nixon-Smith, C. K. | |
| Author | Boykin, D. W. | |
| Author | Soeiro, M. N. C. | |
| Access date | 2016-09-22T13:16:06Z | |
| Available date | 2016-09-22T13:16:06Z | |
| Document date | 2011 | |
| Citation | SOUZA, E. M. de; et al. Trypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi. Experimental Parasitology, v.127, n.2, p.429-435, Feb. 2011. | pt_BR |
| ISSN | 0014-4894 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/15907 | |
| 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 | Atividade tripanocida | pt_BR |
| Subject in Portuguese | Aromáticos de amidina | pt_BR |
| Title | Trypanocidal activity and selectivity in vitro of aromatic amidine compounds upon bloodstream and intracellular forms of Trypanosoma cruzi | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.exppara.2010.10.010 | |
| Abstract | Trypanosoma cruzi is the etiological agent of Chagas disease, an important neglected illness affecting
about 12–14 million people in endemic areas of Latin America. The chemotherapy of Chagas disease is
quite unsatisfactory mainly due to its poor efficacy especially during the later chronic phase and the considerable
well-known side effects. These facts emphasize the need to search for find new drugs. Diamidines
and related compounds are minor groove binders of DNA at AT-rich sites and present excellent
anti-trypanosomal activity. In the present study, six novel aromatic amidine compounds (arylimidamides
and diamidines) were tested in vitro to determine activity against the infective and intracellular stages of
T. cruzi, which are responsible for sustaining the infection in the mammalian hosts. In addition, their
selectivity and toxicity towards primary cultures of cardiomyocyte were evaluated since these cells represent
important targets of infection and inflammation in vivo. The aromatic amidines were active
against T. cruzi in vitro, the arylimidamide DB1470 was the most effective compound presenting a submicromolar
LD50 values, good selectivity index, and good activity at 4 C in the presence of blood constituents.
Our results further justify trypanocidal screening assays with these classes of compounds both
in vitro and in vivo in experimental models of T. cruzi infection. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório 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 | 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, Brasil. | pt_BR |
| Subject | Aromatic amidine | pt_BR |
| Subject | Trypanocidal activity | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Chagas Disease | pt_BR |
| e-ISSN | 1090-2449 | |
| Embargo date | 2030-01-01 | |
| xmlui.metadata.dc.subject.ods | 03 Saúde e Bem-Estar | |
