ArticleTherapeutic advances in infectious disease
Antileishmanial activity of 5-nitroindazole derivatives.
Article in Therapeutic advances in infectious disease. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed, 3 citations in OpenAlex.
- Computational Investigation of the Potential Antileishmanial Mechanism of the Nitroindazole Derivative VATR131.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Indazole Derivatives Against Murine Cutaneous Leishmaniasis.Pharmaceuticals (Basel, Switzerland) · 2025Article
- In Vitro Evaluation of New 5-Nitroindazolin-3-one Derivatives as Promising Agents againstInternational journal of molecular sciences · 2024Article
- 3-Alkoxy-1-Benzyl-5-Nitroindazole Derivatives Are Potent Antileishmanial Compounds.International journal of molecular sciences · 2024Article
Corrections and comments
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Authors and funding
9 authors at 6 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Background: Currently, there is no safe and effective vaccine against leishmaniasis and existing therapies are inadequate due to high toxicity, cost and decreased efficacy caused by the emergence of resistant parasite strains. Some indazole derivatives have shown Objective: To evaluate the Design: For the selection of promising compounds, it is necessary to evaluate the indicators for Methods: Results: Eight compounds showed selectivity index >10% and 50% inhibitory concentration <1 µM against the promastigote stage. Against intracellular amastigotes, four were as active as Amphotericin B. The best results were obtained for 2-(benzyl-2,3-dihydro-5-nitro-3-oxoindazol-1-yl) ethyl acetate, with 50% inhibitory concentration of 0.46 ± 0.01 µM against amastigotes and a selectivity index of 875. The SAR study showed the positive effect on the selectivity of the hydrophilic fragments substituted in position 1 of 2-benzyl-5- nitroindazolin-3-one, which played a key role in improving the selectivity profile of this series of compounds. Conclusion: 2-bencyl-5-nitroindazolin-3-one derivatives showed selective and potent
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Registered trials
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