The increasing danger of methicillin-resistant Staphylococcus aureus (MRSA) and the limited therapeutic options for invasive MRSA infections make an urgent demand for the development of novel anti-MRSA agents. Oxazolidinone derivatives could inhibit protein synthesis by acting on the ribosomal 50S subunit of the bacteria and prevent the formation of a functional 70S initiation complex, so oxazolidinones are a novel class of antimicrobial agents with potential activity against a wide range of clinically significant multidrug-resistant Gram-positive pathogens. However, oxazolidinones such as linezolid are associated with significant adverse events, and myelosuppression represents the main unfavorable side effects. Moreover, MRSA isolates that are resistant to oxazolidinones have already emerged. Hybridization of oxazolidinone with other antibacterial pharmacophores has the potential to interact with multiple targets or to counterbalance the known side effects associated with each pharmacophore. Thus, oxazolidinone-containing hybrids are useful scaffolds for the development of novel anti-MRSA agents. This review covers the recent advances of oxazolidinonecontaining hybrids with anti-MRSA activity developed in the last decade to set up the direction for the design and development of oxazolidinone-containing hybrids with high efficiency and low toxicity.

耐甲氧西林金黄色葡萄球菌 (MRSA) 的危险性日益增加以及侵袭性 MRSA 感染的治疗选择有限，迫切需要开发新型抗 MRSA 药物。恶唑烷酮衍生物可通过作用于细菌的核糖体 50S 亚基来抑制蛋白质合成，并阻止功能性 70S 起始复合物的形成，因此恶唑烷酮是一类新型抗菌剂，对广泛的临床意义的多重耐药革兰氏具有潜在活性-阳性病原体。然而，利奈唑胺等恶唑烷酮类药物与显着不良事件相关，骨髓抑制是主要的不良副作用。此外，已经出现了对恶唑烷酮类耐药的 MRSA 分离株。恶唑烷酮与其他抗菌药效团的杂交有可能与多个靶标相互作用或抵消与每种药效团相关的已知副作用。因此，含恶唑烷酮的杂化物是开发新型抗 MRSA 药物的有用支架。本文综述了近十年来开发的具有抗MRSA活性的含恶唑烷酮杂化物的最新进展，为高效低毒的含恶唑烷酮杂化物的设计和开发指明了方向。