Oxazolidinone scaffolds in drug discovery and development

Oxazolidinone scaffolds have a significant role in drug discovery and development. Compounds with an oxazolidinone skeleton have a wide range of pharmacologic effects and are used to treat bacterial infection. The fully synthetic oxazolidinone antibacterial drugs linezolid and tedizolid have proven clinical therapeutic benefits with the emergence and evolution of resistant bacteria. Antibacterial drugs containing oxazolidinone have several advantages, including favorable pharmacokinetics and pharmacodynamics, novel antibacterial pathways, and druggability. Here, we focus on oxazolidinones derived from structural modifications of linezolid and other possible oxazolidinone drugs, describing their structure–activity relationships, druggability, and safety, and providing a unique idea for improving more potent and safer oxazolidinone drugs.