ArticleJournal of medicinal chemistry2017
Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 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.
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
27 citing papers in PubMed, 62 citations in OpenAlex.
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- Synthesis, Antimicrobial Activities, and Model of Action of Novel Tetralone Derivatives Containing Aminoguanidinium Moiety.International journal of molecular sciences · 2025Article
- Phenyltriazole-based sulfonamides: novel dual-target agents against MRSA biofilms and resistant pathogens.RSC advances · 2025Article
- Synthesis and structure-activity relationship of novel thiazole aminoguanidines against MRSA andRSC medicinal chemistry · 2024Article
- Investigation into the Mechanism of Action of the Tuberculosis Drug Candidate SQ109 and Its Metabolites and Analogues in Mycobacteria.Journal of medicinal chemistry · 2023Article
- A dynamic covalent polymeric antimicrobial for conquering drug-resistant bacterial infection.Exploration (Beijing, China) · 2022Article
- High-throughput platform for yeast morphological profiling predicts the targets of bioactive compounds.NPJ systems biology and applications · 2022Article
- β-Lactams against the Fortress of the Gram-PositiveChemical reviews · 2021Review
- Attenuating the Selection of Vancomycin Resistance AmongACS infectious diseases · 2020Article
- Aryl-alkyl-lysines: Novel agents for treatment of C. difficile infection.Scientific reports · 2020Article
- Identification of a Phenylthiazole Small Molecule with Dual Antifungal and Antibiofilm Activity Against Candida albicans and Candida auris.Scientific reports · 2019Article
- Article
- An aryl isonitrile compound with an improved physicochemical profile that is effective in two mouse models of multidrug-resistant Staphylococcus aureus infection.Journal of global antimicrobial resistance · 2019Article
- Peptidoglycan pathways: there are still more!RSC advances · 2019Review
- Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase.Journal of medicinal chemistry · 2019Article
- Article
- Antibacterial and antivirulence activities of auranofin against Clostridium difficile.International journal of antimicrobial agents · 2019Article
- Repurposing niclosamide for intestinal decolonization of vancomycin-resistant enterococci.International journal of antimicrobial agents · 2018Article
Corrections and comments
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Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
Abstract
The emergence of antibiotic-resistant bacterial species, such as vancomycin-resistant enterococci (VRE), necessitates the development of new antimicrobials. Here, we investigate the spectrum of antibacterial activity of three phenylthiazole-substituted aminoguanidines. These compounds possess potent activity against VRE, inhibiting growth of clinical isolates at concentrations as low as 0.5 μg/mL. The compounds exerted a rapid bactericidal effect, targeting cell wall synthesis. Transposon mutagenesis suggested three possible targets: YubA, YubB (undecaprenyl diphosphate phosphatase (UPPP)), and YubD. Both UPPP as well as undecaprenyl diphosphate synthase were inhibited by compound 1. YubA and YubD are annotated as transporters and may also be targets because 1 collapsed the proton motive force in membrane vesicles. Using Caenorhabditis elegans, we demonstrate that two compounds (1, 3, at 20 μg/mL) retain potent activity in vivo, significantly reducing the burden of VRE in infected worms. Taken altogether, the results indicate that compounds 1 and 3 warrant further investigation as novel antibacterial agents against drug-resistant enterococci.
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What OpenQuestion holds
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.