ArticleEuropean journal of medicinal chemistry2014
New praziquantel derivatives containing NO-donor furoxans and related furazans as active agents against Schistosoma mansoni.
Article in European journal of medicinal chemistry, 2014. 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, 58 citations in OpenAlex.
- Unexpected Synthesis of a Furoxan Derivative from 3-Acetyl-2,4,6-Trimethylpyridine: Structural Characterization and Biological Evaluation.Molecules (Basel, Switzerland) · 2026Article
- Fragment library screening by X-ray crystallography and binding site analysis on thioredoxin glutathione reductase of Schistosoma mansoni.Scientific reports · 2024Article
- Small change, big difference: A promising praziquantel derivative designated P96 with broad-spectrum antischistosomal activity for chemotherapy of schistosomiasis japonica.PLoS neglected tropical diseases · 2023Article
- Recent Advances in the Synthesis and Biomedical Applications of Heterocyclic NO-Donors.Molecules (Basel, Switzerland) · 2021Review
- Synthesis of oxadiazole-2-oxide derivatives as potential drug candidates for schistosomiasis targeting SjTGR.Parasites & vectors · 2021Article
- Medicinal chemistry perspectives of 1,2,3,4-tetrahydroisoquinoline analogs - biological activities and SAR studies.RSC advances · 2021Review
- Radicicol, a Novel Lead Compound against the Migratory-Stage Schistosomula ofAntimicrobial agents and chemotherapy · 2021Article
- A Machine Learning Strategy for Drug Discovery Identifies Anti-Schistosomal Small Molecules.ACS infectious diseases · 2021Article
- Nitric oxide debilitates the neuropathogenic schistosome Trichobilharzia regenti in mice, partly by inhibiting its vital peptidases.Parasites & vectors · 2020Article
- Praziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistance.Antimicrobial agents and chemotherapy · 2017Review
- Brønsted acid-mediated cyclization-dehydrosulfonylation/reduction sequences: An easy access to pyrazinoisoquinolines and pyridopyrazines.Beilstein journal of organic chemistry · 2017Article
- Something old, something new: is praziquantel enough for schistosomiasis control?Future medicinal chemistry · 2015Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
A series of NO-donor praziquantel hybrid compounds was obtained by combining praziquantel (PZQ) and furoxan moieties in a single entity. NO-donor properties of the furoxan derivatives were evaluated by detecting nitrite after incubation of the products in 7.4 pH buffered solution in the presence of L-cysteine. Structurally-related furazans, devoid of NO release capacity, were also synthesized for control purposes. All products were studied for their ability to inhibit recombinant Schistosoma mansoni thioredoxin glutathione reductase (TGR). Mobility and death of adult Schistosoma mansoni worms cultured in the presence of the products were evaluated versus PZQ. Analysis of the results showed that some products were endowed with both PZQ and NO-dependent antiparasitic properties. Compounds 6, 7, 18, and 24 emerged as the most interesting balanced hybrids, worthy of additional study on PZQ-resistant parasites.
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Registered trials
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