Discovery of a novel nitroimidazolyl–oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation

A number of linezolid analogues containing a nitroaryl-1,3,4-thiadiazole moiety, were prepared and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Among synthesized compounds, nitrofuran analogue 1b exhibited more potent inhibitory activity, with respect to other synthesized compounds and reference drug linezolid. The target compounds were also assessed for their cytotoxic activity against normal mouse fibroblast (NIH/3T3) cells using MTT assay. The results indicated that compound 1c exhibit potent antibacterial activity against Gram-positive bacteria at non-cytotoxic concentrations. Novel linezolid analogues containing a nitroaryl-1,3,4-thiadiazole moiety, were synthesized and evaluated against a panel of Gram-positive and Gram-negative bacteria. [Display omitted] ►Antibiotic resistance to Gram-positive pathogens is a major problem in hospitals. ►The oxazolidinones, e.g. linezolid, are a relatively new class of orally active, totally synthetic antibacterial agents active against Gram-positive bacteria. ►The synthesis and in vitro antibacterial activity of novel oxazolidinones containing a nitro-heteroaryl core with potent activity against Gram-positive bacteria have been described.