ArticleEuropean journal of medicinal chemistry2016
Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.
Article in European journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Global Health Priority Box: Discovering Flucofuron as a Promising Antikinetoplastid Compound.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Imidazole and nitroimidazole derivatives as NADH-fumarate reductase inhibitors: Density functional theory studies, homology modeling, and molecular docking.Journal of computational chemistry · 2022Article
- Synthesis and Structure-Activity Relationship of Thioacetamide-Triazoles againstMolecules (Basel, Switzerland) · 2022Article
- 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
- Mutually Isomeric 2- and 4-(3-nitro-1,2,4-triazol-1-yl)pyrimidines Inspired by an Antimycobacterial Screening Hit: Synthesis and Biological Activity against the ESKAPE Panel of Pathogens.Antibiotics (Basel, Switzerland) · 2020Article
- Chagas Disease Treatment and Rational Drug Discovery: A Challenge That Remains.Frontiers in pharmacology · 2019Article
- Nitrotriazole-Based Compounds as Antichagasic Agents in a Long-TreatmentAntimicrobial agents and chemotherapy · 2017Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
3-Nitro-1H-1,2,4-triazole-based acetamides bearing a biphenyl- or a phenoxyphenyl moiety have shown remarkable antichagasic activity both in vitro and in an acute murine model, as well as substantial in vitro antileishmanial activity but lacked activity against human African trypanosomiasis. We have shown now that by inserting a methylene group in the linkage to obtain the corresponding propanamides, both antichagasic and in particular anti-human African trypanosomiasis potency was increased. Therefore, IC50 values at low nM concentrations against both T. cruzi and T. b. rhodesiense, along with huge selectivity indices were obtained. Although several propanamides were active against Leishmania donovani, they were slightly less potent than their corresponding acetamides. There was a good correlation between lipophilicity (clogP value) and trypanocidal activity, for all new compounds. Type I nitroreductase, an enzyme absent from the human host, played a role in the activation of the new compounds, which may function as prodrugs. Antichagasic activity in vivo was also demonstrated with representative propanamides.
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