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Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase
Authors:Mardia Telep El-Sayed  Roya Zoraghi  Neil Reiner  Sibel Suzen  Knut Ohlsen  Michael Lalk
Institution:1. Department of Pharmaceutical Chemistry, Institute of Pharmacy, Martin Luther University, Halle, Germany,;2. Department of Medicine, Division of Infectious Diseases, University of British Columbia, Vancouver, BC, Canada,;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara, Turkey,;4. Institute for Molecular Biology of Infections, Julius Schneider University Würzburg, Würzburg, Germany,;5. Institute of Biochemistry, Ernst Moritz Arndt University Greifswald, Greifswald, Germany, and
Abstract:Novel bisindolyl-cycloalkane indoles resulted from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRSA PK inhibitors and now report first inhibiting activities. We discuss structure–activity relationships of structurally varied compounds. Activity influencing substituents have been characterized and relations to antibacterial activities of the most active compounds have been proved.
Keywords:Antimicrobial compounds  biological activity  indolyl-derived compounds
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