ArticleEuropean journal of medicinal chemistry2016
Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.
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 11 papers.
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Who cites it
11 citing papers in PubMed, 30 citations in OpenAlex.
- High and Selective TrypanocidalMicroorganisms · 2026Article
- Hit-to-Lead Studies of Pyrazinylpiperazines against Visceral Leishmaniasis: Pharmacokinetic Profile andACS pharmacology & translational science · 2025Article
- Sulfonamide based pyrimidine derivatives combatingRSC advances · 2024Article
- Single- and Two-Electron Reduction of Nitroaromatic Compounds by Flavoenzymes: Mechanisms and Implications for Cytotoxicity.International journal of molecular sciences · 2021Review
- Design, synthesis, crystal structure and anti-plasmodial evaluation of tetrahydrobenzo[4,5]thieno[2,3-RSC medicinal chemistry · 2021Article
- New Series of Imidazoles Showed Promising Growth Inhibitory and Curative Potential Against Trypanosoma Infection.The Yale journal of biology and medicine · 2021Article
- Structure-Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents.ChemMedChem · 2020Article
- Synthesis and biological evaluation of thiazole derivatives as LbSOD inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- In vitro activity of aryl-thiazole derivatives against Schistosoma mansoni schistosomula and adult worms.PloS one · 2019Article
- Molecular Cloning and Biochemical Characterization of Iron Superoxide Dismutase from Leishmania braziliensis.Molecular biotechnology · 2018Article
- 4-Phenyl-1,3-thiazole-2-amines as scaffolds for new antileishmanial agents.The journal of venomous animals and toxins including tropical diseases · 2018Article
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as antitrypanosomatid agents. All tested compounds were active or moderately active against Trypanosoma cruzi amastigotes in infected L6 cells and Trypanosoma brucei brucei, four of eleven compounds were moderately active against Leishmania donovani axenic parasites while none were deemed active against T. brucei rhodesiense. For the most active/moderately active compounds a moderate selectivity against each parasite was observed. There was good correlation between lipophilicity (clogP value) and antileishmanial activity or toxicity against L6 cells. Similarly, good correlation existed between clogP values and IC50 values against T. cruzi in structurally related subgroups of compounds. Three compounds were more potent as antichagasic agents than benznidazole but were not activated by the type I nitrorectusase (NTR).
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