ArticleJournal of medicinal chemistry2014
Optimization of potent and selective quinazolinediones: inhibitors of respiratory syncytial virus that block RNA-dependent RNA-polymerase complex activity.
Article in 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 14 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
14 citing papers in PubMed.
- An integrated in silico and ex vivo study identifies quinazolinedione L134716 as a potential inhibitor of infectious bronchitis virus.Veterinary research communications · 2025Article
- Rational Design and Lead Optimisation of Potent Antimalarial Quinazolinediones and Their Cytotoxicity against MCF-7.Molecules (Basel, Switzerland) · 2023Article
- Discovery of novel thioquinazoline-Journal of molecular structure · 2023Article
- Design, Synthesis, Anti-Varicella-Zoster and Antimicrobial Activity of (Isoxazolidin-3-yl)Phosphonate Conjugates of N1-Functionalised Quinazoline-2,4-Diones.Molecules (Basel, Switzerland) · 2022Article
- Electrophilically Activated Nitroalkanes in Synthesis of 3,4-Dihydroquinozalines.Molecules (Basel, Switzerland) · 2021Article
- Substituted N-(4-amino-2-chlorophenyl)-5-chloro-2-hydroxybenzamide analogues potently inhibit respiratory syncytial virus (RSV) replication and RSV infection-associated inflammatory responses.Bioorganic & medicinal chemistry · 2021Article
- Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension.Acta pharmaceutica Sinica. B · 2020Article
- Design, Synthesis, and the Biological Evaluation of a New Series of Acyclic 1,2,3-Triazole Nucleosides.Archiv der Pharmazie · 2017Article
- Synthesis, anti-varicella-zoster virus and anti-cytomegalovirus activity of quinazoline-2,4-diones containing isoxazolidine and phosphonate substructures.European journal of medicinal chemistry · 2017Article
- Structure-guided design of small-molecule therapeutics against RSV disease.Expert opinion on drug discovery · 2016Article
- Article
- Benzimidazole analogs inhibit respiratory syncytial virus G protein function.Antiviral research · 2015Article
- Respiratory Syncytial Virus Inhibitor AZ-27 Differentially Inhibits Different Polymerase Activities at the Promoter.Journal of virology · 2015Article
- The paramyxovirus polymerase complex as a target for next-generation anti-paramyxovirus therapeutics.Frontiers in microbiology · 2015Review
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
A quinazolinedione-derived screening hit 2 was discovered with cellular antiviral activity against respiratory syncytial virus (CPE EC50 = 2.1 μM), moderate efficacy in reducing viral progeny (4.2 log at 10 μM), and marginal cytotoxic liability (selectivity index, SI ∼ 24). Scaffold optimization delivered analogs with improved potency and selectivity profiles. Most notable were compounds 15 and 19 (EC50 = 300-500 nM, CC50 > 50 μM, SI > 100), which significantly reduced viral titer (>400,000-fold), and several analogs were shown to block the activity of the RNA-dependent RNA-polymerase complex of RSV.
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Registered trials
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