ArticlePharmaceuticals (Basel, Switzerland)2021
Antimicrobial Activity of a Library of Thioxanthones and Their Potential as Efflux Pump Inhibitors.
Article in Pharmaceuticals (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 18 citations in OpenAlex.
- Identification of Compounds With Potential Dual Inhibitory Activity Against Drug Efflux Pumps in Resistant Cancer Cells and Bacteria: Protocol for a Systematic Review.JMIR research protocols · 2025Article
- Study Models of Drug-Drug Interactions Involving P-Glycoprotein: The Potential Benefit of P-Glycoprotein Modulation at the Kidney and Intestinal Levels.Molecules (Basel, Switzerland) · 2023Review
- Antibacterial activities of anthraquinones: structure-activity relationships and action mechanisms.RSC medicinal chemistry · 2023Review
- Effect of Indole-Containing Pyrazino[2,1-Antibiotics (Basel, Switzerland) · 2023Article
- Probing the Allosteric Modulation of P-Glycoprotein: A Medicinal Chemistry Approach Toward the Identification of Noncompetitive P-Gp Inhibitors.ACS omega · 2023Article
- SARS-CoV-2 main protease targeting potent fluorescent inhibitors: Repurposing thioxanthones.Turkish journal of chemistry · 2023Article
- Exploring Oceans for Curative Compounds: Potential New Antimicrobial and Anti-Virulence Molecules againstMarine drugs · 2022Review
- New Chalcone-Triazole Hybrids with Promising Antimicrobial Activity in Multidrug Resistance Strains.International journal of molecular sciences · 2022Article
- Antifungal Activity of a Library of Aminothioxanthones.Antibiotics (Basel, Switzerland) · 2022Article
- Enantioselectivity of Chiral Derivatives of Xanthones in Virulence Effects of Resistant Bacteria.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Metabolites from Marine-Derived Fungi as Potential Antimicrobial Adjuvants.Marine drugs · 2021Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
Abstract
The overexpression of efflux pumps is one of the causes of multidrug resistance, which leads to the inefficacy of drugs. This plays a pivotal role in antimicrobial resistance, and the most notable pumps are the AcrAB-TolC system (AcrB belongs to the resistance-nodulation-division family) and the NorA, from the major facilitator superfamily. In bacteria, these structures can also favor virulence and adaptation mechanisms, such as quorum-sensing and the formation of biofilm. In this study, the design and synthesis of a library of thioxanthones as potential efflux pump inhibitors are described. The thioxanthone derivatives were investigated for their antibacterial activity and inhibition of efflux pumps, biofilm formation, and quorum-sensing. The compounds were also studied for their potential to interact with P-glycoprotein (P-gp, ABCB1), an efflux pump present in mammalian cells, and for their cytotoxicity in both mouse fibroblasts and human Caco-2 cells. The results concerning the real-time ethidium bromide accumulation may suggest a potential bacterial efflux pump inhibition, which has not yet been reported for thioxanthones. Moreover, in vitro studies in human cells demonstrated a lack of cytotoxicity for concentrations up to 20 µM in Caco-2 cells, with some derivatives also showing potential for P-gp modulation.
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Registered trials
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