ArticleAntibiotics (Basel, Switzerland)2022
Guanidinylated Polymyxins as Outer Membrane Permeabilizers Capable of Potentiating Rifampicin, Erythromycin, Ceftazidime and Aztreonam against Gram-Negative Bacteria.
Article in Antibiotics (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Dual-Functional Antibiotic Adjuvants Based on Antibacterial Polyesters With Guanidinium and Boronic Acid Motifs.Macromolecular bioscience · 2026Article
- Old drugs, new weapons: current trends in repurposing therapies against antimicrobial resistance.Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques · 2026Review
- Noncytotoxic polymyxin derivatives enhance antibiotic action against multidrug-resistant Gram-negative bacteria.Antimicrobial agents and chemotherapy · 2025Article
- Development of polymyxin- and aminoglycoside-based outer membrane permeabilizers: a review.Frontiers in microbiology · 2025Review
- Guanethidine Enhances the Antibacterial Activity of Rifampicin Against Multidrug-Resistant Bacteria.Microorganisms · 2024Article
- Guanethidine Restores Tetracycline Sensitivity in Multidrug-ResistantAntibiotics (Basel, Switzerland) · 2024Article
- New Antimicrobial Strategies to Treat Multi-Drug Resistant Infections Caused by Gram-Negatives in Cystic Fibrosis.Antibiotics (Basel, Switzerland) · 2024Review
- Lipopeptide adjuvants for antibiotics and vaccines: the future step in the fight against multidrug-resistant and extensively drug-resistant pathogens.Exploration of drug science · 2024Article
- Antibiotic Potentiation as a Promising Strategy to Combat Macrolide Resistance in Bacterial Pathogens.Antibiotics (Basel, Switzerland) · 2023Review
- Article
- Exploring Antibiotic-Potentiating Effects of Tobramycin-Deferiprone Conjugates inAntibiotics (Basel, Switzerland) · 2023Article
- Overcoming intrinsic resistance in gram-negative bacteria using small molecule adjuvants.Bioorganic & medicinal chemistry letters · 2023Review
- Antibiotic adjuvants: synergistic tool to combat multi-drug resistant pathogens.Frontiers in cellular and infection microbiology · 2023Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Polymyxins are considered a last-line treatment against infections caused by multidrug-resistant (MDR) Gram-negative bacteria. In addition to their use as a potent antibiotic, polymyxins have also been utilized as outer membrane (OM) permeabilizers, capable of augmenting the activity of a partner antibiotic. Several polymyxin derivatives have been developed accordingly, with the objective of mitigating associated nephrotoxicity. The conversion of polymyxins to guanidinylated derivatives, whereby the L-γ-diaminobutyric acid (Dab) amines are substituted with guanidines, are described herein. The resulting guanidinylated colistin and polymyxin B (PMB) exhibited reduced antibacterial activity but preserved OM permeabilizing properties that allowed potentiation of several antibiotic classes. Rifampicin, erythromycin, ceftazidime and aztreonam were particularly potentiated against clinically relevant MDR Gram-negative bacteria. The potentiating effects of guanidinylated polymyxins with ceftazidime or aztreonam were further enhanced by adding the β-lactamase inhibitor avibactam.
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Registered trials
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