An overview of recent progress in siderophore-antibiotic conjugates

Eur J Med Chem. 2019 Nov 15:182:111615. doi: 10.1016/j.ejmech.2019.111615. Epub 2019 Aug 12.

Abstract

Multi-drug resistant infections caused by Gram-negative bacteria have become one of the most important reasons for the failure of clinical anti-infective treatment. Siderophore-antibiotic conjugates, which were designed based on a "Trojan horse" strategy wherein features enabled active uptake to bypass the Gram-negative cell wall, have been expected to be a weapon for anti-infective treatment in the clinic. Herein, we review antibiotic drug design strategies based on mimics of nature siderophores reported in recent years, we also focus our attention on the relationship between the type of linker and the corresponding antibacterial activity.

Keywords: Antibiotic; Sideromycin; Siderophore; Siderophore-antibiotic conjugates; Trojan horse.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Gram-Negative Bacteria / drug effects*
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Siderophores / chemistry
  • Siderophores / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Siderophores