The search for new classes of antibiotics is a real concern of public health due to the emergence of multi-resistant bacteria strains. We report herein the synthesis and characterization of a new series of 13 molecules combining isoxazoline/isoxazole sulfonamides and hydrazides motives. These molecules were obtained according to a costless eco-friendly procedure, and a one-pot three-step cascade synthesis under ultrasonic cavitation. All the synthesized compounds were fully characterized by HRMS, H NMR, C NMR spectroscopy and HPLC analysis. These new molecules have been evaluated against the major human opportunistic pathogen Pseudomonas aeruginosa to determine their potential to affect its growth and biofilm formation or dispersion. Two derivatives (5a and 6a) demonstrated their ability to destabilize a mature biofilm by about 50 % within 24 h. This may pave the way to the development of a new class of compounds affecting biofilm, which are easy to synthesize according to green chemistry processes.
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http://dx.doi.org/10.1016/j.bmcl.2023.129517 | DOI Listing |
Sci Total Environ
January 2025
National Institute for Public Health and the Environment (RIVM), Bilthoven, the Netherlands; Department of Biotechnology, Technical University Delft, Delft, the Netherlands. Electronic address:
Water systems can act as an important reservoir for Pseudomonas aeruginosa, which can pose public health risks during human contact. Carbapenem resistance is one of the most concerning resistances in P. aeruginosa making it a high-priority pathogen according to the World Health Organization (WHO), due to its ability to cause difficult-to-treat infections.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
January 2025
Key Laboratory of Molecular Nanostructure and Nanotechnology, Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
Emerging evidence indicates that intratumor bacteria exist as an active and specific tumor component in many tumor types beyond digestive and respiratory tumors. However, the biological impact and responsible molecules of such local bacteria-tumor direct interaction on cancer therapeutic response remain poorly understood. Trastuzumab is among the most commonly used drugs targeting the receptor tyrosine-protein kinase erbB-2 (ErbB2) in breast cancer, but its resistance is inevitable, severely limiting its clinical effectiveness.
View Article and Find Full Text PDFSci Rep
January 2025
School of Engineering and Materials Science, Queen Mary University of London, Mile End Road, London, E1 4NS, UK.
Antimicrobial resistance (AMR) is a major cause of death worldwide, with 1.27 M direct deaths from bacterial drug-resistant infections as of 2019. Dissemination of multidrug-resistant (MDR) bacteria in the environment, in conjunction with pharmapollution by active pharmaceutical ingredients (APIs), create and foster an environmental reservoir of AMR.
View Article and Find Full Text PDFNPJ Biofilms Microbiomes
January 2025
Department of Microbiology and Immunology, University of Otago, Dunedin, New Zealand.
Chronic infections represent a significant global health and economic challenge. Biofilms, which are bacterial communities encased in an extracellular polysaccharide matrix, contribute to approximately 80% of these infections. In particular, pathogens such as Pseudomonas aeruginosa and Staphylococcus aureus are frequently co-isolated from the sputum of patients with cystic fibrosis and are commonly found in chronic wound infections.
View Article and Find Full Text PDFCarbohydr Polym
March 2025
Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Faculty of Pharmacy, Instituto de Materiales (iMATUS), and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. Electronic address:
Biofilm formation on biological and material surfaces represents a heavy health and economic burden for both patient and society. To contrast this phenomenon, medical devices combining antibacterial and pro-wound healing abilities are a promising strategy. In the present work, Xanthan gum/Guar gum (XG/GG)-based scaffolds were tuned with thymol and Zn to obtain wound dressings that combine antibacterial and antibiofilm properties and favour the healing process.
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