Discovery of bisindolyl-substituted cycloalkane-anellated indoles as novel class of antibacterial agents against S. aureus and MRSA

Bioorg Med Chem Lett. 2016 Jan 1;26(1):218-21. doi: 10.1016/j.bmcl.2015.10.085. Epub 2015 Oct 29.

Abstract

Antibiotic resistance is an ongoing problem in the treatment of bacterial diseases. Among the various antibacterial infections Staphylococcus aureus infections remain critical due to the increasing resistances, especially against the methicillin-resistant S. aureus (MRSA). We discovered novel antibacterial compounds with activities against both S. aureus and MRSA types. Structure-activity relationships (SAR) are discussed and show that the activity depends on the ring size of the anellated cycloalkane. Moreover, first substituent effects have been investigated for both the cycloalkane and the indole residues.

Keywords: Antibacterial activity; Cycloalkane indoles; MRSA; Structure–activity relationships.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Cycloparaffins / chemistry*
  • Dose-Response Relationship, Drug
  • Drug Discovery*
  • Indoles / chemical synthesis
  • Indoles / chemistry*
  • Indoles / pharmacology*
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Molecular Structure
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Cycloparaffins
  • Indoles