ArticleJournal of medicinal chemistry2013
Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Aminopyridines in the development of drug candidates against protozoan neglected tropical diseases.Future medicinal chemistry · 2024Review
- Applications of palladium-catalyzed C-N cross-coupling reactions in pharmaceutical compounds.RSC advances · 2023Review
- Miltefosine and Benznidazole Combination Improve Anti-Frontiers in cellular and infection microbiology · 2022Article
- Benznidazole Treatment: Time- and Dose-Dependence Varies with thePathogens (Basel, Switzerland) · 2021Article
- Naturally Occurring Ecdysteroids inInternational journal of molecular sciences · 2021Article
- An Overview on the Therapeutics of Neglected Infectious Diseases-Leishmaniasis and Chagas Diseases.Frontiers in chemistry · 2021Review
- A new chemotype with promise against Trypanosoma cruzi.Bioorganic & medicinal chemistry letters · 2020Article
- Experimental models in Chagas disease: a review of the methodologies applied for screening compounds against Trypanosoma cruzi.Parasitology research · 2018Review
- Searching for new drugs for Chagas diseases: triazole analogs display high in vitro activity against Trypanosoma cruzi and low toxicity toward mammalian cells.Journal of bioenergetics and biomembranes · 2018Article
- Addressing the most neglected diseases through an open research model: The discovery of fenarimols as novel drug candidates for eumycetoma.PLoS neglected tropical diseases · 2018Article
- Experimental and Clinical Treatment of Chagas Disease: A Review.The American journal of tropical medicine and hygiene · 2017Review
- Electrochemically Enabled, Nickel-Catalyzed Amination.Angewandte Chemie (International ed. in English) · 2017Article
- Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.Journal of medicinal chemistry · 2017Article
- In vitro drug susceptibility of two strains of the wildlife trypanosome, Trypanosoma copemani: A comparison with Trypanosoma cruzi.International journal for parasitology. Drugs and drug resistance · 2017Article
- Applications of Palladium-Catalyzed C-N Cross-Coupling Reactions.Chemical reviews · 2016Review
- A new experimental model for assessing drug efficacy against Trypanosoma cruzi infection based on highly sensitive in vivo imaging.Journal of biomolecular screening · 2015Review
- Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties.Antimicrobial agents and chemotherapy · 2015Article
- Translational challenges of animal models in Chagas disease drug development: a review.Drug design, development and therapy · 2015Review
- Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.Journal of medicinal chemistry · 2014Article
- Drug strategies targeting CYP51 in neglected tropical diseases.Chemical reviews · 2014Review
Corrections and comments
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Authors and funding
21 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chagas disease, caused by the protozoan parasite Trypanosoma cruzi (T. cruzi), is an increasing threat to global health. Available medicines were introduced over 40 years ago, have undesirable side effects, and give equivocal results of cure in the chronic stage of the disease. We report the development of two compounds, 6 and (S)-7, with PCR-confirmed curative activity in a mouse model of established T. cruzi infection after once daily oral dosing for 20 days at 20 mg/kg 6 and 10 mg/kg (S)-7. Compounds 6 and (S)-7 have potent in vitro activity, are noncytotoxic, show no adverse effects in vivo following repeat dosing, are prepared by a short synthetic route, and have druglike properties suitable for preclinical development.
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Registered trials
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.