Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (10): 3026-3043.DOI: 10.6023/cjoc202006042 Previous Articles     Next Articles


刘君, 侯劲松, 孟影, 缪志颖, 林静, 陈卫民   

  1. 暨南大学药学院 广州 510632
  • 收稿日期:2020-06-21 修回日期:2020-08-20 发布日期:2020-08-27
  • 通讯作者: 陈卫民
  • 基金资助:

Research Progress of Antibiotics Conjugated with Siderophores

Liu Jun, Hou Jinsong, Meng Ying, Miao Zhiying, Lin Jing, Chen Weimin   

  1. College of Pharmacy, Jinan University, Guangzhou 510632
  • Received:2020-06-21 Revised:2020-08-20 Published:2020-08-27
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 81872776).

The natural siderophore is a class of small-molecule iron ion chelating agents secreted by bacteria, which can be recognized by specific outer membrane receptors and transported into cytoplasm to provide iron for bacteria. Using this characteristic of siderophore, antibiotics can be coupled with them and enter into bacteria through the bacterial iron uptake system. This strategy is called "Trojan horse" strategy. Recently, cefiderocol, the first siderophore-antibiotic conjugate, was approved for marketing, which has aroused accumulated interest of scientists and pharmaceutical companies in this field. This paper provides a comprehensive review of the progress in antibiotics conjugated with siderophores from three aspects:the types of siderophore molecules, antibiotics with different action mechanisms, and the role of linkers. The basic relationship between anti-bacterial activity and three moieties of this novel type of anti-bacterial agents has been revealed. This review will provide a reference for the development of new antibiotics conjugated with siderophores.

Key words: antibiotic, siderophore, conjugate, "Trojan horse" strategy