ArticleOrganic & biomolecular chemistry2013
Synthesis and biological evaluation of triazole-containing N-acyl homoserine lactones as quorum sensing modulators.
Article in Organic & biomolecular chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 65 citations in OpenAlex.
- Discovery of triazole-tethered glycinate and propanoate derivatives bearing a thiolactone moiety as quorum sensing inhibitors ofRSC advances · 2026Article
- Structure-Aided Design of a LuxR-Type Quorum Sensing SuFEx-Based Potential Inhibitor: Covalent or Competitive Inhibition?Biomolecules · 2026Article
- Effects on LuxR-Regulated Bioluminescence of Cyclodextrin-Acyl-L-Homoserine Lactone Hybrids.Chembiochem : a European journal of chemical biology · 2025Article
- Molecular simulation-based investigation of thiazole derivatives as potential LasR inhibitors of Pseudomonas aeruginosa.PloS one · 2025Article
- A data-driven machine learning approach for discovering potent LasR inhibitors.Bioengineered · 2023Article
- Hybrid Androgen Receptor Inhibitors Outperform Enzalutamide and EPI-001 in in vitro Models of Prostate Cancer Drug Resistance.ChemMedChem · 2023Article
- Bacterial virulence factors: a target for heterocyclic compounds to combat bacterial resistance.RSC advances · 2021Review
- Heterocyclic Chemistry Applied to the Design ofMolecules (Basel, Switzerland) · 2021Review
- Quorum sensing N-Acyl homoserine lactones are a new class of anti-schistosomal.PLoS neglected tropical diseases · 2020Article
- Considerations and Caveats in Combating ESKAPE Pathogens against Nosocomial Infections.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2020Review
- Quorum Quenching: A Potential Target for Antipseudomonal Therapy.Infection and drug resistance · 2020Review
- Quorum Sensing as a Target for Controlling Surface Associated Motility and Biofilm Formation inFrontiers in microbiology · 2020Article
- Design, synthesis and biological evaluation of 1,2,3-triazole based 2-aminobenzimidazoles as novel inhibitors of LasR dependent quorum sensing inRSC advances · 2019Article
- Chemical probes of quorum sensing: from compound development to biological discovery.FEMS microbiology reviews · 2016Review
- Quorum sensing signal-response systems in Gram-negative bacteria.Nature reviews. Microbiology · 2016Review
- Interfering with Bacterial Quorum Sensing.Perspectives in medicinal chemistry · 2016Article
- Efficient Syntheses of 1,2,3-Triazoloamide Derivatives Using Solid- and Solution-Phase Synthetic Approaches.Molecules (Basel, Switzerland) · 2015Article
- Unraveling the contributions of hydrogen-bonding interactions to the activity of native and non-native ligands in the quorum-sensing receptor LasR.Organic & biomolecular chemistry · 2015Article
- Non-native N-aroyl L-homoserine lactones are potent modulators of the quorum sensing receptor RpaR in Rhodopseudomonas palustris.Chembiochem : a European journal of chemical biology · 2014Article
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 3 countries.
Funding
Abstract
Many bacterial species are capable of assessing their local population densities through a cell-cell signaling mechanism termed quorum sensing (QS). This intercellular communication process is mediated by small molecule or peptide ligands and their cognate protein receptors. Numerous pathogens use QS to initiate virulence once they achieve a threshold cell number on a host. Consequently, approaches to intercept QS have attracted considerable attention as potential anti-infective therapies. Our interest in the development of small molecule tools to modulate QS pathways motivated us to evaluate triazole-containing analogs of natural N-acyl L-homoserine lactone (AHL) signals as non-native QS agonists and antagonists in Gram-negative bacteria. We synthesized 72 triazole derivatives of five broad structure types in high yields and purities using efficient Cu(I)-catalyzed azide-alkyne couplings. These compounds were evaluated for their ability to activate or inhibit two QS receptors from two prevalent pathogens - LasR from Pseudomonas aeruginosa and AbaR from Acinetobacter baumannii- using bacterial reporter strains. Several triazole derivatives were identified that were capable of strongly modulating the activity of LasR and AbaR. These compounds represent a new and synthetically accessible class of AHL analogs, and could find utility as chemical tools to study QS and its role in bacterial virulence.
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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.