ArticleFuture medicinal chemistry2013
Novel 3-nitro-1H-1,2,4-triazole-based compounds as potential anti-Chagasic drugs: in vivo studies.
Article in Future medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 39 citations in OpenAlex.
- Triazole Scaffold-based DPP-IV Inhibitors for the Management of Type-II Diabetes Mellitus: Insight into Molecular Docking and SAR.Current topics in medicinal chemistry · 2026Review
- Synthesis and Biological Evaluation of 4‑(4-Nitrophenyl)‑1ACS omega · 2025Article
- The carbonic anhydrase enzymes as new targets for the management of neglected tropical diseases.Archiv der Pharmazie · 2025Review
- Anti-Molecules (Basel, Switzerland) · 2023Article
- Review on Experimental Treatment Strategies AgainstJournal of experimental pharmacology · 2021Review
- Chagas Disease Treatment and Rational Drug Discovery: A Challenge That Remains.Frontiers in pharmacology · 2019Article
- 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
- Nitrotriazole-Based Compounds as Antichagasic Agents in a Long-TreatmentAntimicrobial agents and chemotherapy · 2017Article
- Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.European journal of medicinal chemistry · 2016Article
- Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.European journal of medicinal chemistry · 2016Article
- Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.Journal of medicinal chemistry · 2015Article
- Nitrotriazole- and imidazole-based amides and sulfonamides as antitubercular agents.Antimicrobial agents and chemotherapy · 2014Article
- 4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.Journal of medicinal chemistry · 2014Article
- Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents.Bioorganic & medicinal chemistry · 2013Article
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Authors and funding
8 authors at 5 institutions in 3 countries.
Funding
Abstract
backgroundChagas disease is caused by the parasite Trypanosoma cruzi, is endemic in Latin America and leads to an estimated 14,000 deaths per year and around 100 million people at risk of infection. Drugs currently used in the treatment of Chagas are old, partially effective and have numerous side effects. METHODOLOGY: We have previously reported that 3-nitro-1H-1,2,4-triazole-based compounds demonstrate significant and selective activity against T. cruzi amastigotes in infected L6 cells via activation of a type I nitroreductase, specific to trypanosomatids. In the present work we evaluated in vivo 13 of these compounds based on their high in vitro potency against T. cruzi (IC50 < 1 µM) and selectivity (SI: toxicity to L6 cells/toxicity against T. cruzi amastigotes > 200). Representative compounds of different chemical classes were included. A fast luminescence assay with transgenic parasites that express luciferase, and live imaging techniques were used. A total of 11 out of 13 compounds demonstrated significant antichagasic activity when administered intraperitoneally for 5-10 days at relatively small doses. The best in vivo activity was demonstrated by amides and sulfonamide derivatives. ADMET studies were performed for specific compounds.
conclusionAt least three compounds were identified as effective, non-toxic antichagasic agents suitable for further development.
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