There has been considerable effort expended in the investigation of the potential of siderophore conjugates of antibiotics to circumvent the permeability barrier imposed by the outer membrane of Gram-negative bacteria. There is also a small group of natural conjugates, the sideromycins. Among the synthetic analogues that have been investigated are conjugates of nucleosides, glycopeptides, macrolides, fluroquinolones, and, above all, β-lactams. Despite this effort, few compounds have progressed beyond experimental studies. One compound, the siderophore monosulfactam BAL30072, is in early clinical studies.