The antimicrobial natural product chuangxinmycin and some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3171-4. doi: 10.1016/s0960-894x(02)00604-2.


The antimicrobial natural product chuangxinmycin has been found to be a potent and selective inhibitor of bacterial tryptophanyl tRNA synthetase (WRS). A number of analogues have been synthesised. The interaction with WRS appears to be highly constrained, as only sterically smaller analogues afforded significant inhibition. The only analogue to show inhibition comparable to chuangxinmycin also had antibacterial activity. WRS inhibition may contribute to the antibacterial action of chuangxinmycin.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology*
  • Hydrolysis
  • Indicators and Reagents
  • Indoles / chemical synthesis
  • Indoles / pharmacology*
  • Microbial Sensitivity Tests
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / enzymology*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Tryptophan-tRNA Ligase / antagonists & inhibitors*


  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Indicators and Reagents
  • Indoles
  • chuangxinmycin
  • Tryptophan-tRNA Ligase