ArticleJournal of medicinal chemistry2016
Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials.
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
40 citing papers in PubMed, 1 synthesis or guideline pooled it.
- A Systematic Review of Synthetic and Anticancer and Antimicrobial Activity of Quinazoline/Quinazolin-4-one Analogues.ChemistryOpen · 2025Pooled it
- Synthesis and Biological Evaluation of New Quinazolin-4(3H)-One-Coumarin Hybrids Designed as Anticancer and Antibacterial Agents.International journal of molecular sciences · 2026Article
- Synthesis of 2-Aryl-4-aminoquinazolines: Design, Molecular Docking, and In Vitro Assessment of Antibacterial and Cytotoxic Potential.International journal of molecular sciences · 2026Article
- Halogenated Vitamin BACS omega · 2026Article
- Facile Chemodivergent Synthesis of Fused Indolo[2,3‑ACS omega · 2025Article
- Synthesis, evaluation ofRSC advances · 2025Article
- Article
- Sonosynthesis of new functionalized optically active triazinesRSC advances · 2025Article
- Aminoalkylation of Alkenes Enabled by Triple Radical Sorting.Journal of the American Chemical Society · 2025Article
- Design and synthesis of novel main protease inhibitors of COVID-19: quinoxalino[2,1-RSC advances · 2024Article
- Aromatization-driven deconstructive functionalization of spiro dihydroquinazolinonesChemical science · 2024Article
- One-pot synthesis of quinazolinone heterocyclic compounds using functionalized SBA-15 with natural material ellagic acid as a novel nanocatalyst.Scientific reports · 2024Article
- Critical view on antimicrobial, antibiofilm and cytotoxic activities of quinazolin-4(3Heliyon · 2024Article
- In silico evaluation of a new compound incorporating 4(3H)-quinazolinone and sulfonamide as a potential inhibitor of a human carbonic anhydrase.BMC chemistry · 2024Article
- Unraveling the mechanism of ceftaroline-induced allosteric regulation in penicillin-binding protein 2a: insights for novel antibiotic development against methicillin-resistantAntimicrobial agents and chemotherapy · 2023Article
- Design, synthesis, docking, ADMET and anticancer evaluations ofRSC advances · 2023Article
- A Review on Five and Six-Membered Heterocyclic Compounds Targeting the Penicillin-Binding Protein 2 (PBP2A) of Methicillin-ResistantMolecules (Basel, Switzerland) · 2023Review
- Penicillin-binding protein (PBP) inhibitor development: A 10-year chemical perspective.Experimental biology and medicine (Maywood, N.J.) · 2023Review
- Actinoquinazolinone, a New Quinazolinone Derivative from a Marine BacteriumMarine drugs · 2023Article
- Novel Quinazoline Derivative Induces Differentiation of Keratinocytes and Enhances Skin Barrier Functions against Th2 Cytokine-Mediated Signaling.Molecules (Basel, Switzerland) · 2023Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
We recently reported on the discovery of a novel antibacterial (2) with a 4(3H)-quinazolinone core. This discovery was made by in silico screening of 1.2 million compounds for binding to a penicillin-binding protein and the subsequent demonstration of antibacterial activity against Staphylococcus aureus. The first structure-activity relationship for this antibacterial scaffold is explored in this report with evaluation of 77 variants of the structural class. Eleven promising compounds were further evaluated for in vitro toxicity, pharmacokinetics, and efficacy in a mouse peritonitis model of infection, which led to the discovery of compound 27. This new quinazolinone has potent activity against methicillin-resistant (MRSA) strains, low clearance, oral bioavailability and shows efficacy in a mouse neutropenic thigh infection model.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.