Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones

A new series of oxazolidinones bearing N-linked 5-triazolylmethyl group have been synthesized and their in vitro antibacterial activities (MIC) were evaluated against a spectrum of resistant and susceptible Gram-positive organisms. Some of the analogues in this series displayed activity superior to linezolid and vancomycin. Furthermore, in vivo efficacies and pharmacokinetic properties of the selected compounds were also disclosed herein; the selected compounds showed reasonable bioavailability as well as in vivo efficacy comparable to that of linezolid.

Graphical abstractA new series of oxazolidinones bearing N-linked 5-triazolylmethyl group are disclosed. The selected compounds of this series display in vitro and in vivo activities comparable to linezolid. Compound 4e shows excellent activity against Gram-positive organisms.Figure optionsDownload full-size imageDownload as PowerPoint slide