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Abstract：
Pseudomonas aeruginosa is a Gram-negative pathogenic bacterium responsible for severe infections, and it is naturally resistant to many clinically approved antibiotic families. Oxazolidinone antibiotics are active against many Gram-positive bacteria, but are inactive against P. aeruginosa. Increasing the uptake of oxazolidinones through the bacterial envelope could lead to an increased antibiotic effect. Pyochelin is a siderophore of P. aeruginosa which delivers external iron to the bacterial cytoplasm and is a potential vector for the development of Trojan Horse oxazolidinone conjugates. Novel pyochelin-oxazolidinone conjugates were synthesized using an unexpectedly regioselective peptide coupling between an amine functionalized pyochelin and oxazolidinones functionalized with a terminal carboxylate.
摘要：
铜绿假单胞菌是导致严重感染的革兰氏阴性致病菌，它对许多临床批准的抗生素家族具有天然抗性。恶唑烷酮抗生素对许多革兰氏阳性细菌具有活性，但对铜绿假单胞菌不活跃。通过细菌包膜增加恶唑烷酮的摄取可导致增加的抗生素作用。Pyochelin是铜绿假单胞菌的铁载体，可将外部铁输送到细菌细胞质，并且是开发特洛伊木马恶唑烷酮偶联物的潜在载体。使用胺官能化的pelchelin和用末端羧酸酯官能化的恶唑烷酮之间的出乎意料的区域选择性肽偶联来合成新型pelchelin-恶唑烷酮缀合物。
