ArticlePloS one2012
In vitro and in vivo investigation of the efficacy of arylimidamide DB1831 and its mesylated salt form--DB1965--against Trypanosoma cruzi infection.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers, 1 of them a synthesis that pooled it.
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Who cites it
21 citing papers in PubMed, 1 synthesis or guideline pooled it, 37 citations in OpenAlex.
- Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.Parasitology · 2013Pooled it
- Arylimidamides Have Potential for Chemoprophylaxis against Blood-Transmitted Chagas Disease.Pathogens (Basel, Switzerland) · 2023Article
- Escaping ESKAPE resistance:Royal Society open science · 2023Article
- In vitro interaction of polyethylene glycol-block-poly(D,L-lactide) nanocapsule devices with host cardiomyoblasts and Trypanosoma cruzi-infective forms.Parasitology research · 2022Article
- In Vitro Phenotypic Activity and In Silico Analysis of Natural Products from Brazilian Biodiversity onMolecules (Basel, Switzerland) · 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
- Article
- Efficacy of sertraline againstThe journal of venomous animals and toxins including tropical diseases · 2018Article
- Elucidating the impact of low doses of nano-formulated benznidazole in acute experimental Chagas disease.PLoS neglected tropical diseases · 2017Article
- Phenotypic evaluation and in silico ADMET properties of novel arylimidamides in acute mouse models ofDrug design, development and therapy · 2017Article
- Phenotypic Screening In Vitro of Novel Aromatic Amidines against Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2016Article
- In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2016Article
- Different Therapeutic Outcomes of Benznidazole and VNI Treatments in Different Genders in Mouse Experimental Models of Trypanosoma cruzi Infection.Antimicrobial agents and chemotherapy · 2015Article
- Ciprofloxacin Derivatives Affect Parasite Cell Division and Increase the Survival of Mice Infected with Toxoplasma gondii.PloS one · 2015Article
- In vitro and in vivo studies of the biological activity of novel arylimidamides against Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2014Article
- In vitro and in vivo biological effects of novel arylimidamide derivatives 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
- Assessment of the anti-protozoal activity of crude Carica papaya seed extract against Trypanosoma cruzi.Molecules (Basel, Switzerland) · 2013Article
- In vitro and in vivo studies of the antiparasitic activity of sterol 14α-demethylase (CYP51) inhibitor VNI against drug-resistant strains of Trypanosoma cruzi.Antimicrobial agents and chemotherapy · 2013Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chagas disease is caused by infection with the intracellular protozoan parasite Trypanosoma cruzi. At present, nifurtimox and benznidazole, both compounds developed empirically over four decades ago, represent the chemotherapeutic arsenal for treating this highly neglected disease. However, both drugs present variable efficacy depending on the geographical area and the occurrence of natural resistance, and are poorly effective against the later chronic stage. As a part of a search for new therapeutic opportunities to treat chagasic patients, pre-clinical studies were performed to characterize the activity of a novel arylimidamide (AIA--DB1831 (hydrochloride salt) and DB1965 (mesylate salt)) against T. cruzi. These AIAs displayed a high trypanocidal effect in vitro against both relevant forms in mammalian hosts, exhibiting a high selectivity index and a very high efficacy (IC(50) value/48 h of 5-40 nM) against intracellular parasites. DB1965 shows high activity in vivo in acute experimental models (mouse) of T. cruzi, showing a similar effect to benznidazole (Bz) when compared under a scheme of 10 daily consecutive doses with 12.5 mg/kg. Although no parasitological cure was observed after treating with 20 daily consecutive doses, a combined dosage of DB1965 (5 mg/kg) with Bz (50 mg/kg) resulted in parasitaemia clearance and 100% animal survival. In summary, our present data confirmed that aryimidamides represent promising new chemical entities against T. cruzi in therapeutic schemes using the AIA alone or in combination with other drugs, like benznidazole.
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