ArticleEuropean journal of medicinal chemistry2020
Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction.
Article in European journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 18 citations in OpenAlex.
- Purification, Characterization, and In Vitro Safety Assessment of the Antimicrobial Peptide SAM-KB40 from Bacillus licheniformis SAM-D318.Applied biochemistry and biotechnology · 2026Article
- Development of triaryl antimicrobials by scaffold hopping from an aminopropanol hit targeting bacterial RNA polymerase-NusG interactions.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Development of a luciferase-based Gram-positive bacterial reporter system for the characterization of antimicrobial agents.Applied and environmental microbiology · 2024Article
- Inhibition of bacterial RNA polymerase function and protein-protein interactions: a promising approach for next-generation antibacterial therapeutics.RSC medicinal chemistry · 2024Review
- Ligand-Based Drug Design of Novel Antimicrobials againstInternational journal of molecular sciences · 2022Article
- QSAR, Docking, and Molecular Dynamics Simulation Studies of Sigmacidins as Antimicrobials againstInternational journal of molecular sciences · 2022Article
- RNA polymerases from low G+C gram-positive bacteria.Transcription · 2021Review
- Modulators of protein-protein interactions as antimicrobial agents.RSC chemical biology · 2021Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
Abstract
Transcription is an essential biological process in bacteria requiring a core enzyme, RNA polymerase (RNAP). Bacterial RNAP is catalytically active but requires sigma (σ) factors for transcription of natural DNA templates. σ factor binds to RNAP to form a holoenzyme which specifically recognizes a promoter, melts the DNA duplex, and commences RNA synthesis. Inhibiting the binding of σ to RNAP is expected to inhibit bacterial transcription and growth. We previously identified a triaryl hit compound that mimics σ at its major binding site of RNAP, thereby inhibiting the RNAP holoenzyme formation. In this study, we modified this scaffold to provide a series of benzyl and benzoyl benzoic acid derivatives possessing improved antimicrobial activity. A representative compound demonstrated excellent activity against Staphylococcus epidermidis with minimum inhibitory concentrations reduced to 0.5 μg/mL, matching that of vancomycin. The molecular mechanism of inhibition was confirmed using biochemical and cellular assays. Low cytotoxicity and metabolic stability of compounds demonstrated the potential for further studies.
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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.