The ability of fimsbactin B, a natural siderophore of Acinetobacter baumannii, to function as an antibiotic delivery vehicle was investigated by synthesizing three structurally diversified fimsbactin B-cefaclor conjugates. Their antimicrobial activities were Acinetobacter-selective and up to 128-fold more potent than that of cefaclor alone. This activity enhancement originated from the fimsbactin-B-dependent active uptake of cefaclor. Thus, fimsbactin-B-based antibiotic delivery can be an effective approach in combating antibiotic-resistant Acinetobacter infections.