ArticleBioorganic & medicinal chemistry2013
Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents.
Article in Bioorganic & medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
19 citing papers in PubMed, 52 citations in OpenAlex.
- The carbonic anhydrase enzymes as new targets for the management of neglected tropical diseases.Archiv der Pharmazie · 2025Review
- Article
- Identification of 1,2,3-triazole-phthalimide derivatives as potential drugs against COVID-19: a virtual screening, docking and molecular dynamic study.Journal of biomolecular structure & dynamics · 2022Article
- Phenylbenzothiazole derivatives: effects against a Trypanosoma cruzi infection and toxicological profiles.Parasitology research · 2021Article
- Synthesis, Characterization, and Preliminary In Vitro Cytotoxic Evaluation of a Series of 2-Substituted Benzo [Molecules (Basel, Switzerland) · 2021Article
- Review on Experimental Treatment Strategies AgainstJournal of experimental pharmacology · 2021Review
- An insight on medicinal attributes of 1,2,4-triazoles.European journal of medicinal chemistry · 2020Review
- Facile Synthesis of a Series of Non-Symmetric Thioethers Including a Benzothiazole Moiety and Their Use as Efficient In Vitro anti-Molecules (Basel, Switzerland) · 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
- Synthesis and antibacterial evaluation of new N- and S-glycosides analogues with dinitrophenyl-substituted heterocyclic bases.Molecular diversity · 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
- How an Inhibitor Bound to Subunit Interface Alters Triosephosphate Isomerase Dynamics.Biophysical journal · 2015Article
- 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
- Nitro drugs for the treatment of trypanosomatid diseases: past, present, and future prospects.Trends in parasitology · 2014Review
- Megazol and its bioisostere 4H-1,2,4-triazole: comparing the trypanocidal, cytotoxic and genotoxic activities and their in vitro and in silico interactions with the Trypanosoma brucei nitroreductase enzyme.Memorias do Instituto Oswaldo Cruz · 2014Article
- Utility of Diagnostic Imaging in the Diagnosis and Management of Schistosomiasis.Clinical microbiology (Los Angeles, Calif.) · 2014Article
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 2 countries.
Funding
Abstract
We have previously shown that 3-nitro-1H-1,2,4-triazole-based amines demonstrate significant trypanocidal activity, in particular against Trypanosoma cruzi, the causative parasite of Chagas disease. In the present work we further expanded our research by evaluating in vitro the trypanocidal activity of nitrotriazole-based piperazines and nitrotriazole-based 2-amino-1,3-benzothiazoles to establish additional SARs. All nitrotriazole-based derivatives were active or moderately active against T. cruzi; however two of them did not fulfill the selectivity criteria. Five derivatives were active or moderately active against Trypanosoma brucei rhodesiense while one derivative was moderately active against Leishmania donovani. Active compounds against T. cruzi demonstrated selectivity indexes (toxicity to host cells/toxicity to T. cruzi amastigotes) from 117 to 1725 and 12 of 13 compounds were up to 39-fold more potent than the reference compound benznidazole. Detailed SARs are discussed.
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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.