ArticleAntimicrobial agents and chemotherapy2010
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers, 2 of them syntheses that pooled it.
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Who cites it
44 citing papers in PubMed, 2 syntheses or guidelines pooled it, 80 citations in OpenAlex.
- In vitro susceptibility of Trypanosoma cruzi discrete typing units (DTUs) to benznidazole: A systematic review and meta-analysis.PLoS neglected tropical diseases · 2021Pooled it
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Kinetoplast-Directed Therapies: A Selective Mitochondrial Approach to Combat Leishmaniasis.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Synthesis and Biophysical and Biological Studies ofJournal of medicinal chemistry · 2023Article
- Antiparasitic Activity ofPharmaceutics · 2023Article
- Arylimidamides Have Potential for Chemoprophylaxis against Blood-Transmitted Chagas Disease.Pathogens (Basel, Switzerland) · 2023Article
- 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
- Structure Activity Relationship ofFrontiers in chemistry · 2021Article
- Review on Experimental Treatment Strategies AgainstJournal of experimental pharmacology · 2021Review
- Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2020Article
- Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents.ChemMedChem · 2019Article
- Therapeutic Interventions for Countering Leishmaniasis and Chagas's Disease: From Traditional Sources to Nanotechnological Systems.Pathogens (Basel, Switzerland) · 2019Review
- Imidazole Derivatives as Promising Agents for the Treatment of Chagas Disease.Antimicrobial agents and chemotherapy · 2019Article
- Successful Aspects of the Coadministration of Sterol 14α-Demethylase Inhibitor VFV and Benznidazole in Experimental Mouse Models of Chagas Disease Caused by the Drug-Resistant Strain of Trypanosoma cruzi.ACS infectious diseases · 2019Article
- Experimental models in Chagas disease: a review of the methodologies applied for screening compounds against Trypanosoma cruzi.Parasitology research · 2018Review
- Repurposing Strategy of Atorvastatin against Trypanosoma cruzi:Antimicrobial agents and chemotherapy · 2018Article
- Article
- Impact of autologous whole blood administration upon experimental mouse models of acuteThe journal of venomous animals and toxins including tropical diseases · 2018Article
- Experimental and Clinical Treatment of Chagas Disease: A Review.The American journal of tropical medicine and hygiene · 2017Review
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chagas' disease, a neglected tropical illness for which current therapy is unsatisfactory, is caused by the intracellular parasite Trypanosoma cruzi. The goal of this work is to investigate the in vitro and in vivo effects of the arylimidamide (AIA) DB766 against T. cruzi. This arylimidamide exhibits strong trypanocidal activity and excellent selectivity for bloodstream trypomastigotes and intracellular amastigotes (Y strain), giving IC(50)s (drug concentrations that reduce 50% of the number of the treated parasites) of 60 and 25 nM, respectively. DB766 also exerts striking effects upon different parasite stocks, including those naturally resistant to benznidazole, and displays higher activity in vitro than the reference drugs. By fluorescent and transmission electron microscopy analyses, we found that this AIA localizes in DNA-enriched compartments and induces considerable damage to the mitochondria. DB766 effectively reduces the parasite load in the blood and cardiac tissue and presents efficacy similar to that of benznidazole in mouse models of T. cruzi infection employing the Y and Colombian strains, using oral and intraperitoneal doses of up to 100 mg/kg/day that were given after the establishment of parasite infection. This AIA ameliorates electrocardiographic alterations, reduces hepatic and heart lesions induced by the infection, and provides 90 to 100% protection against mortality, which is similar to that provided by benznidazole. Our data clearly show the trypanocidal efficacy of DB766, suggesting that this AIA may represent a new lead compound candidate to Chagas' disease treatment.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.