The synthesis and antibacterial activity evaluation of oxazolidinone - deferasirox conjugates.

We reported herein the synthesis and antibacterial activity evaluation of two oxazolidinone-deferasirox conjugates with different linkers that were designed based on the "Trojan horse" strategy. The conjugates could combine with Fe³⁺ ions as the deferasirox. However, both conjugates were inactive against tested bacteria, including S. aureus, E. coli, A. baumannii, and P. aeruginosa. The results suggested that the synthesized iron chelator deferasirox was not suitable as a siderophore of the bacteria to transport the antibiotic, or the coupling linker of the synthesized conjugates could not be hydrolyzed to release the oxazolidinone in the cytoplasm. Therefore, the design and synthesis of oxazolidinone-deferasirox conjugates need further exploration. Keywords: Oxazolidinone; Deferasirox; Antibacterial; Siderophore; "Trojan horse" strategy [ABSTRACT FROM AUTHOR]