Oxazolidinone: A promising scaffold for the development of antibacterial drugs

Due to the long-term and widespread use of antibiotics in clinic, the problem of bacterial resistance is increasingly serious, and the development of new drugs to treat drug-resistant bacteria has gradually become the mainstream direction of antibiotic research. The oxazolidinone-containing drugs linezolid, tedizolid phosphate and contezolid have been approved to the market, which are effective against a variety of Gram-positive bacterium infections. Moreover, there are also many antibiotics containing oxazolidinone fragment under clinical investigation that show good pharmacokinetic and pharmacodynamic properties with unique mechanism of action against resistant bacteria. In this review, we summarized the oxazolidinone-based antibiotics already on the market or in clinical trials and the representative bioactive molecules, and mainly focused on their structural optimizations, development strategies and structure-activity relationships in hope of insight into the reasonable design for medical chemists to develop new oxazolidinone antibiotics with highly potency and fewer side effects.

Automated summary

Due to the long-term and widespread use of antibiotics in clinical practice, bacterial resistance has become an increasingly serious problem. The development of new drugs to combat drug-resistant bacteria has become the mainstream direction of antibiotic research. This review summarizes the current oxazolidinone-based antibiotics on the market or in clinical trials and their structural optimizations, development strategies, and structure-activity relationships, providing insights for the rational design of new oxazolidinone antibiotics with higher potency and fewer side effects.