Inhibition of biofilm formation by conformationally constrained indole-based analogues of the marine alkaloid oroidin |
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| Institution: | 1. University of Ljubljana, Faculty of Pharmacy, Aškerčeva 7, 1000 Ljubljana, Slovenia;2. University of Gdańsk, Department of Molecular Biology, Wita Stwosza 59, 80-308 Gdańsk, Poland;3. From the Masonic Cancer Center and Department of Medicinal Chemistry, University of Minnesota, Minneapolis, Minnesota 55455 and;4. UMR INSERM 1085 IRSET, Rennes 1 University, UMS 3480 Biosit, F-35043 Rennes, France;1. Department of Periodontics, University of Texas Health Science Center at San Antonio, San Antonio, TX, 78229, USA;2. Department of Periodontology, Tufts University School of Dental Medicine, Boston, MD, 02111, USA;3. Department of Developmental Dentistry, University of Texas Health Science Center at San Antonio, San Antonio, TX, 78229, USA;1. Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Stremayrgasse 16, A-8010 Graz, Austria;2. Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland;3. Institute for Chemistry and Technology of Materials (ICTM), Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria |
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| Abstract: | Herein, we describe indole-based analogues of oroidin as a novel class of 2-aminoimidazole-based inhibitors of methicillin-resistant Staphylococcus aureus biofilm formation and, to the best of our knowledge, the first reported 2-aminoimidazole-based inhibitors of Streptococcus mutans biofilm formation. This study highlighted the indole moiety as a dibromopyrrole mimetic for obtaining inhibitors of S. aureus and S. mutans biofilm formation. The most potent compound in the series, 5-(trifluoromethoxy)indole-based analogue 4b (MBIC50 = 20 μM), emerged as a promising hit for further optimisation of novel inhibitors of S. aureus and S. mutans biofilms. |
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| Keywords: | Biofilm Indole Inhibition Marine Oroidin |
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