Antibacterials pp 151-183 | Cite as

Sideromycins as Pathogen-Targeted Antibiotics

Part of the Topics in Medicinal Chemistry book series (TMC, volume 26)


The overuse of broad-spectrum antibiotics rapidly selects for dangerous multi-drug resistant bacterial pathogens. The landscape of antibiotic drug discovery is adapting to this wave of resistance with a movement towards narrow-spectrum, pathogen-targeted antibiotics that limit the emergence of new resistance. Sideromycins (siderophore-antibiotic conjugates) exploit essential iron acquisition pathways to achieve receptor-mediated cell entry where the spectrum of antibiotic activity is determined by highly selective cell surface siderophore receptors rather than the widely distributed and highly conserved antibacterial target. Sideromycins overwhelm traditional resistance mechanisms through high intracellular antibiotic concentrations and resistance adaptation renders pathogens avirulent. The timing is optimal to pursue sideromycins as pathogen-targeted antibiotics and chemical probes for rapid pathogen diagnostics.


Albomycin Antibiotic-delivery systems Baulamycin Enterobactin Grisein Microcin Mycobactin Pyoverdine Salmycin Sideromycin Staphyloferrin Tetroazolemycin Trojan horse Xenosiderophore 



MJM thanks all group members and collaborators who worked on the synthesis and study of siderophores and sideromycins in his research laboratory at the University of Notre Dame over the past 40 years (1977–2017) with near continuous support from the NIH. MJM and TAW sincerely thank Dr. Ute Möllmann (Leibniz Institute for Natural Product Research and Infection Biology – Hans Knöll Institute) for years of friendship and collaboration on siderophore microbiology. TAW acknowledges the NSF for a CAREER Award (1654611) that supports siderophore research in his laboratory.


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Copyright information

© Springer International Publishing AG, part of Springer Nature 2017

Authors and Affiliations

  1. 1.Department of ChemistryWashington University in St. LouisSt. LouisUSA
  2. 2.Department of Chemistry and BiochemistryUniversity of Notre DameNotre DameUSA

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