ArticleJournal of medicinal chemistry2013
A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro.
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 11 papers.
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Who cites it
11 citing papers in PubMed, 54 citations in OpenAlex.
- 5‑Nitrofuran-Semicarbazone Hybrids as Antitrypanosomal Agents: Structure-Activity Relationship and Nitroreductase Activation.ACS medicinal chemistry letters · 2026Article
- Exploring Novel Nitrofuryl-1,3,4-Thiadiazole-Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity.Archiv der Pharmazie · 2026Article
- A Subset Screen of the Compounds Australia Scaffold Library Identifies 7-Acylaminodibenzoxazepinones as Potent and Selective Hits for Anti-Biomedicines · 2022Article
- 2-(Nitroaryl)-5-Substituted-1,3,4-Thiadiazole Derivatives with Antiprotozoal Activities: In Vitro and In Vivo Study.Molecules (Basel, Switzerland) · 2022Article
- Biological evaluation and structure activity relationship of 9-methyl-1-phenyl-9H-pyrido[3,4-b]indole derivatives as anti-leishmanial agents.Bioorganic chemistry · 2019Article
- Engineered P450 biocatalysts show improved activity and regio-promiscuity in aromatic nitration.Scientific reports · 2017Article
- Development of Simplified Heterocyclic Acetogenin Analogues as Potent and Selective Trypanosoma brucei Inhibitors.ChemMedChem · 2016Article
- Visible light C-H amidation of heteroarenes with benzoyl azides.Chemical science · 2015Article
- Article
- Nitro drugs for the treatment of trypanosomatid diseases: past, present, and future prospects.Trends in parasitology · 2014Review
- Pharmacokinetics of hydroxymethylnitrofurazone, a promising new prodrug for Chagas' disease treatment.Antimicrobial agents and chemotherapy · 2013Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Recently, the World Health Organization approved the nifurtimox-eflornithine combination therapy for the treatment of human African trypanosomiasis, renewing interest in nitroheterocycle therapies for this and associated diseases. In this study, we have synthesized a series of novel 5-nitro-2-furancarboxylamides that show potent trypanocidal activity, ∼1000-fold more potent than nifurtimox against in vitro Trypanosoma brucei with very low cytotoxicity against human HeLa cells. More importantly, the most potent analogue showed very limited cross-resistance to nifurtimox-resistant cells and vice versa. This implies that our novel, relatively easy to synthesize and therefore cheap, 5-nitro-2-furancarboxylamides are targeting a different, but still essential, biochemical process to those targeted by nifurtimox or its metabolites in the parasites. The significant increase in potency (smaller dose probably required) has the potential for greatly reducing unwanted side effects and also reducing the likelihood of drug resistance. Collectively, these findings have important implications for the future therapeutic treatment of African sleeping sickness.
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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.