ArticleAntimicrobial agents and chemotherapy2016
In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Kinetoplast-Directed Therapies: A Selective Mitochondrial Approach to Combat Leishmaniasis.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Cafestol and kahweol: coffee diterpenes with trypanocidal activity and cardioprotective effects.Frontiers in cellular and infection microbiology · 2026Article
- Review
- The impact of probiotic administration on experimental in vitro and in vivo infection by Trypanosoma cruzi.Memorias do Instituto Oswaldo Cruz · 2025Article
- Amidine containing compounds: Antimicrobial activity and its potential in combating antimicrobial resistance.Heliyon · 2024Review
- Article
- Phenotypic Evaluation of Nucleoside Analogues againstMolecules (Basel, Switzerland) · 2022Article
- The Impact of the CTHRSSVVC Peptide Upon Experimental Models ofFrontiers in cellular and infection microbiology · 2022Article
- 7-Aryl-7-deazapurine 3'-deoxyribonucleoside derivative as a novel lead for Chagas' disease therapy:JAC-antimicrobial resistance · 2021Article
- Activity of the sesquiterpene lactone goyazensolide againstParasitology · 2020Article
- Impact of autologous whole blood administration upon experimental mouse models of acuteThe journal of venomous animals and toxins including tropical diseases · 2018Article
- Biological factors that impinge on Chagas disease drug development.Parasitology · 2017Review
- 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
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16 authors.
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Abstract
Arylimidamides (AIAs) have been shown to have considerable biological activity against intracellular pathogens, includingTrypanosoma cruzi, which causes Chagas disease. In the present study, the activities of 12 novel bis-AIAs and 2 mono-AIAs against different strains ofT. cruziin vitroandin vivowere analyzed. The most active wasm-terphenyl bis-AIA (35DAP073), which had a 50% effective concentration (EC50) of 0.5 μM for trypomastigotes (Y strain), which made it 26-fold more effective than benznidazole (Bz; 13 μM). It was also active against the Colombiana strain (EC50= 3.8 μM). Analysis of the activity against intracellular forms of the Tulahuen strain showed that this bis-AIA (EC50= 0.04 μM) was about 100-fold more active than Bz (2 μM). The trypanocidal effect was dissociated from the ability to trigger intracellular lipid bodies within host cells, detected by oil red labeling. Both an active compound (35DAP073) and an inactive compound (26SMB060) displayed similar activation profiles. Due to their high selectivity indexes, two AIAs (35DAP073 and 35DAP081) were moved toin vivostudies, but because of the results of acute toxicity assays, 35DAP081 was excluded from the subsequent tests. The findings obtained with 35DAP073 treatment of infections caused by the Y strain revealed that 2 days of therapy induced a dose-dependent action, leading to 96 to 46% reductions in the level of parasitemia. However, the administration of 10 daily doses in animals infected with the Colombiana strain resulted in toxicity, preventing longer periods of treatment. The activity of the combination of 0.5 mg/kg of body weight/day 35DAP073 with 100 mg/kg/day Bz for 10 consecutive days was then assayed. Treatment with the combination resulted in the suppression of parasitemia, the elimination of neurological toxic effects, and survival of 100% of the animals. Quantitative PCR showed a considerable reduction in the parasite load (60%) compared to that achieved with Bz or the amidine alone. Our results support further investigations of this class with the aim of developing novel alternatives for the treatment of Chagas disease.
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