ArticleAntimicrobial agents and chemotherapy2005
Biological characterization of novel inhibitors of the gram-positive DNA polymerase IIIC enzyme.
Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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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.
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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
10 citing papers in PubMed, 24 citations in OpenAlex.
- DNA replication proteins as potential targets for antimicrobials in drug-resistant bacterial pathogens.The Journal of antimicrobial chemotherapy · 2017Review
- Advances in MRSA drug discovery: where are we and where do we need to be?Expert opinion on drug discovery · 2013Review
- Characterization of a novel DNA polymerase activity assay enabling sensitive, quantitative and universal detection of viable microbes.Nucleic acids research · 2012Article
- Architecture and conservation of the bacterial DNA replication machinery, an underexploited drug target.Current drug targets · 2012Review
- Challenges of antibacterial discovery.Clinical microbiology reviews · 2011Review
- Structure of PolC reveals unique DNA binding and fidelity determinants.Proceedings of the National Academy of Sciences of the United States of America · 2008Article
- Novel whole-cell antibiotic biosensors for compound discovery.Applied and environmental microbiology · 2007Article
- Antibacterial activity and mechanism of action of a novel anilinouracil-fluoroquinolone hybrid compound.Antimicrobial agents and chemotherapy · 2007Article
- Novel bacterial acetyl coenzyme A carboxylase inhibitors with antibiotic efficacy in vivo.Antimicrobial agents and chemotherapy · 2006Article
- Hybrid antibacterials. DNA polymerase-topoisomerase inhibitors.Journal of medicinal chemistry · 2006Article
Corrections and comments
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Authors and funding
12 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Novel N-3-alkylated 6-anilinouracils have been identified as potent and selective inhibitors of bacterial DNA polymerase IIIC, the enzyme essential for the replication of chromosomal DNA in gram-positive bacteria. A nonradioactive assay measuring the enzymatic activity of the DNA polymerase IIIC in gram-positive bacteria has been assembled. The 6-anilinouracils described inhibited the polymerase IIIC enzyme at concentrations in the nanomolar range in this assay and displayed good in vitro activity (according to their MICs) against staphylococci, streptococci, and enterococci. The MICs of the most potent derivatives were about 4 microg/ml for this panel of bacteria. The 50% effective dose of the best compound (6-[(3-ethyl-4-methylphenyl)amino]-3-{[1-(isoxazol-5-ylcarbonyl)piperidin-4-yl]methyl}uracil) was 10 mg/kg of body weight after intravenous application in a staphylococcal sepsis model in mice, from which in vivo pharmacokinetic data were also acquired.
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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.