ArticleBioorganic & medicinal chemistry2019
Tryptamine derivatives disarm colistin resistance in polymyxin-resistant gram-negative bacteria.
Article in Bioorganic & medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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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
17 citing papers in PubMed, 29 citations in OpenAlex.
- Biogenic amine tryptamine in human vaginal probiotic isolates mediates matrix inhibition and thwarts uropathogenic E. coli biofilm.Scientific reports · 2024Article
- Synthesis of β-Carbolines with Electrocyclic Cyclization of 3-Nitrovinylindoles.International journal of molecular sciences · 2023Article
- Total Synthesis of (±)-Tetrahedron letters · 2023Article
- Structure-activity relationship studies of [1,2,5]oxadiazolo[3,4-b]pyrazine-containing polymyxin-selective resistance-modifying agents.Bioorganic & medicinal chemistry letters · 2022Article
- Inhibitors ofPharmaceuticals (Basel, Switzerland) · 2022Article
- Serendipitous Discovery of a Highly Active and Selective Resistance-Modifying Agent for Colistin-Resistant Gram-Negative Bacteria.ACS omega · 2022Article
- Diarylamine-Guided Carboxamide Derivatives: Synthesis, Biological Evaluation, and Potential Mechanism of Action.Frontiers in chemistry · 2022Article
- Physicochemical and Structural Parameters Contributing to the Antibacterial Activity and Efflux Susceptibility of Small-Molecule Inhibitors of Escherichia coli.Antimicrobial agents and chemotherapy · 2021Article
- Current Update on Intrinsic and Acquired Colistin Resistance Mechanisms in Bacteria.Frontiers in medicine · 2021Review
- Eukaryotic phosphatase inhibitors enhance colistin efficacy in gram-negative bacteria.Chemical biology & drug design · 2020Article
- A novel colistin adjuvant identified by virtual screening for ArnT inhibitors.The Journal of antimicrobial chemotherapy · 2020Article
- Article
- Recent progress on elucidating the molecular mechanism of plasmid-mediated colistin resistance and drug design.International microbiology : the official journal of the Spanish Society for Microbiology · 2020Review
- A Whole-Cell Screen Identifies Small Bioactives That Synergize with Polymyxin and Exhibit Antimicrobial Activities against Multidrug-Resistant Bacteria.Antimicrobial agents and chemotherapy · 2020Article
- Structure-Function Studies on IMD-0354 Identifies Highly Active Colistin Adjuvants.ChemMedChem · 2020Article
- Considerations and Caveats in Combating ESKAPE Pathogens against Nosocomial Infections.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2020Review
- Repurposing Eukaryotic Kinase Inhibitors as Colistin Adjuvants in Gram-Negative Bacteria.ACS infectious diseases · 2019Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
The last three decades have seen a dwindling number of novel antibiotic classes approved for clinical use and a concurrent increase in levels of antibiotic resistance, necessitating alternative methods to combat the rise of multi-drug resistant bacteria. A promising strategy employs antibiotic adjuvants, non-toxic molecules that disarm antibiotic resistance. When co-dosed with antibiotics, these compounds restore antibiotic efficacy in drug-resistant strains. Herein we identify derivatives of tryptamine, a ubiquitous biochemical scaffold containing an indole ring system, capable of disarming colistin resistance in the Gram-negative bacterial pathogens Acinetobacter baumannii, Klebsiella pneumoniae, and Escherichia coli while having no inherent bacterial toxicity. Resistance was overcome in strains carrying endogenous chromosomally-encoded colistin resistance machinery, as well as resistance conferred by the mobile colistin resistance-1 (mcr-1) plasmid-borne gene. These compounds restore a colistin minimum inhibitory concentration (MIC) below the Clinical & Laboratory Sciences Institute (CLSI) breakpoint in all resistant strains.
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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.