Design, synthesis and antibacterial evaluation of oxazolidinone derivatives containing N-methylglycyl or quaternary ammonium salts.

The continuous evolution of multidrug-resistant (MDR) bacteria to existing antibiotic treatment regimens poses a serious threat to human health, so the discovery of new and potent antimicrobial drugs that are less likely to develop resistance is of great clinical significance. As a result, oxazolidinone antibiotics have emerged as a significant class of bacterial protein synthesis inhibitors, with particular success in the treatment of MDR Gram-positive infections. Herein, a series of novel C-ring modified oxazolidinone derivatives with the introduction of N-methylglycyl groups or quaternary ammonium salts were synthesized and evaluated for their antibacterial efficacy, among which most of the N-methylglycyl derivatives showed significant activity against E.