Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase. (1st November 2016)

• Record Type: Journal Article
• Authors: El-Sayed, Mardia Telep; Zoraghi, Roya; Reiner, Neil; Suzen, Sibel; Ohlsen, Knut; Lalk, Michael; Altanlar, Nurten; Hilgeroth, Andreas
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 31:Number 6(2016:Dec.)
• Page Start: 1666
• Page End: 1671
• Publication Date: 2016-11-01
• Subjects: Antimicrobial compounds -- biological activity -- indolyl-derived compounds; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2015.1118685
• Languages: English
• ISSNs: 1475-6366

Abstract

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.