ArticleAntimicrobial agents and chemotherapy2008
In vitro and in vivo studies of the trypanocidal activity of a diarylthiophene diamidine against Trypanosoma cruzi.
Article in Antimicrobial agents and chemotherapy, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers, 1 of them a synthesis that pooled it.
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Who cites it
23 citing papers in PubMed, 1 synthesis or guideline pooled it, 63 citations in OpenAlex.
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Evaluation of the anti-Trypanosoma cruzi activity in vitro and in vivo of silibinin and silibinin in association to benznidazole.Parasitology research · 2021Article
- Therapeutic potential of the methanolic extract ofSaudi journal of biological sciences · 2019Article
- Experimental models in Chagas disease: a review of the methodologies applied for screening compounds against Trypanosoma cruzi.Parasitology research · 2018Review
- Experimental and Clinical Treatment of Chagas Disease: A Review.The American journal of tropical medicine and hygiene · 2017Review
- 3-Hydroxykynurenine, a Tryptophan Metabolite Generated during the Infection, Is Active AgainstACS medicinal chemistry letters · 2017Article
- Phenotypic evaluation and in silico ADMET properties of novel arylimidamides in acute mouse models ofDrug design, development and therapy · 2017Article
- An Aromatic Diamidine That Targets Kinetoplast DNA, Impairs the Cell Cycle in Trypanosoma cruzi, and Diminishes Trypomastigote Release from Infected Mammalian Host Cells.Antimicrobial agents and chemotherapy · 2016Article
- In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2016Article
- Discovery of novel polyamine analogs with anti-protozoal activity by computer guided drug repositioning.Journal of computer-aided molecular design · 2016Article
- In vitro and in vivo studies of the biological activity of novel arylimidamides against Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2014Article
- Activities of psilostachyin A and cynaropicrin against Trypanosoma cruzi in vitro and in vivo.Antimicrobial agents and chemotherapy · 2013Article
- In vitro and in vivo activities of dicationic diguanidino compounds against Echinococcus multilocularis metacestodes.Antimicrobial agents and chemotherapy · 2013Article
- Combined approaches for drug design points the way to novel proline racemase inhibitor candidates to fight Chagas' disease.PloS one · 2013Article
- CYP51 structures and structure-based development of novel, pathogen-specific inhibitory scaffolds.International journal for parasitology. Drugs and drug resistance · 2012Article
- In vitro and in vivo studies of the trypanocidal activity of four terpenoid derivatives against Trypanosoma cruzi.The American journal of tropical medicine and hygiene · 2012Article
- Article
- The trypanocidal activity of amidine compounds does not correlate with their binding affinity to Trypanosoma cruzi kinetoplast DNA.Antimicrobial agents and chemotherapy · 2011Article
- Screening of Potential anti-Trypanosoma cruzi Candidates: In Vitro and In Vivo Studies.The open medicinal chemistry journal · 2011Article
- Experimental Chemotherapy for Chagas Disease: A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma cruzi Targets of Amidines Derivatives and Naphthoquinones.Molecular biology international · 2011Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
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 and in view of our previous reports regarding the effect of diamidines and analogues against both in vitro and in vivo Trypanosoma cruzi infection, this study evaluated the effects of a diarylthiophene diamidine (DB1362) against both amastigotes and bloodstream trypomastigotes of T. cruzi, the etiological agent of Chagas' disease. The data show the potent in vitro activity of DB1362 against both parasite forms that are relevant for mammalian infection at doses which do not exhibit cytotoxicity. Ultrastructural analysis and flow cytometry studies show striking alterations in the nuclei and mitochondria of the bloodstream parasites. In vivo studies were performed at two different drug concentrations (25 and 50 mg/kg/day) using a 2-day or a 10-day regimen. The best results were obtained when acutely infected mice were treated with two doses at the lower concentration, resulting in 100% survival, compared to the infected and untreated mice. Although it did not display higher efficacy than benznidazole, DB1362 reduced both cardiac parasitism and inflammation, and in addition, it protected against the cardiac alterations (determined by measurements) common in T. cruzi infection. These results support further investigation of diamidines and related compounds as potential agents against Chagas' disease.
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