Synthesis and antimicrobial activity of novel globomycin analogues

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2315-8. doi: 10.1016/s0960-894x(03)00432-3.

Abstract

Globomycin, a signal peptidase II inhibitor, and its derivatives show potent antibacterial activity against Gram-negative bacteria. The synthesis and antimicrobial activity of novel globomycin analogues are reported. One of the analogues showed a more potent activity against Gram-negative bacteria than globomycin and also exhibited antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Indicators and Reagents
  • Microbial Sensitivity Tests
  • Peptides / chemical synthesis*
  • Peptides / pharmacology*
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / pharmacology*
  • Staphylococcus aureus / drug effects
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Indicators and Reagents
  • Peptides
  • Protease Inhibitors
  • globomycin