Identification of novel deoxyribofuranosyl indole antimicrobial agents

J Antibiot (Tokyo). 2012 Feb;65(2):53-7. doi: 10.1038/ja.2011.110. Epub 2011 Dec 14.

Abstract

Three novel deoxyribofuranosyl indole derivatives, FG050227 (1), FG050223 (2) and FG050204 (3), were identified as antimicrobial agents effective against Gram-positive bacterial strains and some fungi. The MIC values of (1), (2) and (3) against methicillin-resistant Staphylococcus aureus were 3.0, 6.0 and 13 μg ml⁻¹, respectively. Compounds 1 and 3 had bactericidal activity against exponentially growing S. aureus and inhibited biosynthesis of peptidoglycan, protein, RNA and DNA. Compound 2 was bacteriostatic and inhibited the biosynthesis of protein and RNA. The results indicated that deoxyribofuranosyl indole derivatives could be potential lead compounds for the development of antimicrobial agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents / chemical synthesis
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Fungi / drug effects*
  • Gram-Positive Bacteria / drug effects*
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry
  • Indoles / pharmacology*
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Methicillin-Resistant Staphylococcus aureus / growth & development
  • Methicillin-Resistant Staphylococcus aureus / metabolism
  • Microbial Sensitivity Tests
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / growth & development
  • Staphylococcus aureus / metabolism

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Indoles