Discovery of quinoline small molecules with potent dispersal activity against methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis biofilms using a scaffold hopping strategy |
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Affiliation: | 1. Nicolaus Copernicus University, Collegium Medicum, Faculty of Pharmacy, Department of Physical Chemistry, Kurpińskiego 5, 85-950 Bydgoszcz, Poland;2. UTP University of Science and Technology, Faculty of Chemical Technology and Engineering, Seminaryjna 3, 85-326 Bydgoszcz, Poland;3. Wroclaw Medical University, Department of Inorganic Chemistry, Faculty of Pharmacy, Borowska 211a, 50-556 Wroclaw, Poland |
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Abstract: | Staphylococcus aureus and Staphylococcus epidermidis are recognized as the most frequent cause of biofilm-associated nosocomial and indwelling medical device infections. Biofilm-associated infections are known to be highly resistant to our current arsenal of clinically used antibiotics and antibacterial agents. To exacerbate this problem, no therapeutic option exists that targets biofilm-dependent machinery critical to Staphylococcal biofilm formation and maintenance. Here, we describe the discovery of a series of quinoline small molecules that demonstrate potent biofilm dispersal activity against methicillin-resistant S. aureus and S. epidermidis using a scaffold hopping strategy. This interesting class of quinolines also has select synthetic analogues that demonstrate potent antibacterial activity and biofilm inhibition against S. aureus and S. epidermidis. |
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Keywords: | Drug discovery Biofilm dispersal agent Biofilm inhibitor Antibacterial agent Quinoline |
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