ArticlePloS one2021
Design, synthesis and biological evaluation of N-oxide derivatives with potent in vivo antileishmanial activity.
Article in PloS one, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 13 citations in OpenAlex.
- Guanidines Conjugated with Cell-Penetrating Peptides: A New Approach for the Development of Antileishmanial Molecules.Molecules (Basel, Switzerland) · 2025Article
- Isoindoline-1,3-dione Derivatives as Prototypes for Anticonvulsant Drug Discovery.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Article
- Article
- Advances in Cysteine Protease B Inhibitors for Leishmaniasis Treatment.Current drug targets · 2025Review
- Design and Synthesis of Benzimidazole Carboxamide Cysteine Protease Inhibitors as Promising Anti-leishmanial Agents.Current medicinal chemistry · 2025Article
- Peptide Dimerization as a Strategy for the Development of Antileishmanial Compounds.Molecules (Basel, Switzerland) · 2024Article
- Medicinal Chemistry of Drugs withJournal of medicinal chemistry · 2024Review
- Recent progress in synthesis and application of furoxan.RSC advances · 2023Review
- Computational design, molecular properties, ADME, and toxicological analysis of substituted 2,6-diarylidene cyclohexanone analogs as potent pyridoxal kinase inhibitors.In silico pharmacology · 2023Article
- Novel Selective and Low-Toxic Inhibitor ofBiomolecules · 2022Article
- Antiparasitary and antiproliferative activities in vitro of a 1,2,4-oxadiazole derivative on Trypanosoma cruzi.Parasitology research · 2022Article
- Design and Synthesis of Hybrid Compounds as Epigenetic Modifiers.Pharmaceuticals (Basel, Switzerland) · 2021Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f, a furoxan derivative, was particularly remarkable in this regard, with EC50 value of 3.6 μM against L. infantum amastigote forms and CC50 value superior to 500 μM against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC50: 4.5 μM). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced ~90% of parasite burden in the liver and spleen of L. infantum-infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.
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