混合型铁载体-甲氨蝶呤抗菌缀合物的设计、合成

In 2019, the first siderophore-antibiotic conjugated drug, Cefiderocol, was approved for marketing, which attracted widespread attention from many experts and pharmaceutical companies. This siderophore-antibacterial drug conjugate strategy provides a new idea for the development of novel antibiotics. Using this strategy, a conjugate of a mixed siderophore targeting Acinetobacter baumannii and the dihydrofolate reductase inhibitor methotrexate was designed and synthesized. It is expected to reduce the cytotoxicity of methotrexate and enhance the antibacterial activity against Acinetobacter baumannii. In the process of synthesizing mixed siderophore, a new synthetic route was designed in this paper. The route is simple and high in yield, which lays a foundation for the future research on mixed siderophore antibacterial conjugates.