ArticleJournal of medicinal chemistry2009
Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 78 citations in OpenAlex.
- Structural basis for substrate recognition and inhibition of thioredoxin glutathione reductase from Schistosoma japonicum: Implications for antiparasitic development.PLoS pathogens · 2026Article
- Screening Novel Furoxan Derivatives as Potential Inhibitors Targeting Thioredoxin Glutathione Reductase ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Non-covalent inhibitors of thioredoxin glutathione reductase with schistosomicidal activity in vivo.Nature communications · 2023Article
- Recent progress in synthesis and application of furoxan.RSC advances · 2023Review
- Synthesis of oxadiazole-2-oxide derivatives as potential drug candidates for schistosomiasis targeting SjTGR.Parasites & vectors · 2021Article
- A Machine Learning Strategy for Drug Discovery Identifies Anti-Schistosomal Small Molecules.ACS infectious diseases · 2021Article
- Effects of Mammalian Thioredoxin Reductase Inhibitors.Handbook of experimental pharmacology · 2021Article
- Nitric oxide debilitates the neuropathogenic schistosome Trichobilharzia regenti in mice, partly by inhibiting its vital peptidases.Parasites & vectors · 2020Article
- Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?RSC medicinal chemistry · 2020Review
- UHPLC-MS-Based Metabolomics Analysis Reveals the Process of Schistosomiasis in Mice.Frontiers in microbiology · 2020Article
- Fragment-Based Discovery of a Regulatory Site in Thioredoxin Glutathione Reductase Acting as "Doorstop" for NADPH Entry.ACS chemical biology · 2018Article
- Computer-Aided Drug Design Using Sesquiterpene Lactones as Sources of New Structures with Potential Activity against Infectious Neglected Diseases.Molecules (Basel, Switzerland) · 2017Review
- Discovery of New Anti-Schistosomal Hits by Integration of QSAR-Based Virtual Screening and High Content Screening.Journal of medicinal chemistry · 2016Article
- QSAR-Driven Discovery of Novel Chemical Scaffolds Active against Schistosoma mansoni.Journal of chemical information and modeling · 2016Article
- Oxadiazole-2-oxides may have other functional targets, in addition to SjTGR, through which they cause mortality in Schistosoma japonicum.Parasites & vectors · 2016Article
- High-throughput screening against thioredoxin glutathione reductase identifies novel inhibitors with potential therapeutic value for schistosomiasis.Infectious diseases of poverty · 2015Article
- Inhibition of Tapeworm Thioredoxin and Glutathione Pathways by an Oxadiazole N-Oxide Leads to Reduced Mesocestoides vogae Infection Burden in Mice.Molecules (Basel, Switzerland) · 2015Article
- Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents.Current medicinal chemistry · 2015Review
- New praziquantel derivatives containing NO-donor furoxans and related furazans as active agents against Schistosoma mansoni.European journal of medicinal chemistry · 2014Article
- Leishmanicidal activities of novel synthetic furoxan and benzofuroxan derivatives.Antimicrobial agents and chemotherapy · 2014Article
Corrections and comments
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Authors and funding
17 authors at 6 institutions in 3 countries.
Funding
Abstract
Schistosomiasis is a chronic parasitic disease affecting hundreds of millions of individuals worldwide. Current treatment depends on a single agent, praziquantel, raising concerns of emergence of resistant parasites. Here, we continue our explorations of an oxadiazole-2-oxide class of compounds we recently identified as inhibitors of thioredoxin glutathione reductase (TGR), a selenocysteine-containing flavoenzyme required by the parasite to maintain proper cellular redox balance. Through systematic evaluation of the core molecular structure of this chemotype, we define the essential pharmacophore, establish a link between the nitric oxide donation and TGR inhibition, determine the selectivity for this chemotype versus related reductase enzymes, and present evidence that these agents can be modified to possess appropriate drug metabolism and pharmacokinetic properties. The mechanistic link between exogenous NO donation and parasite injury is expanded and better defined. The results of these studies verify the utility of oxadiazole-2-oxides as novel inhibitors of TGR and as efficacious antischistosomal agents.
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Registered trials
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