Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1666-71. doi: 10.3109/14756366.2015.1118685. Epub 2015 Dec 10.

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.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Methicillin-Resistant Staphylococcus aureus / enzymology*
  • Pyruvate Kinase / antagonists & inhibitors*
  • Spectrum Analysis / methods

Substances

  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Pyruvate Kinase