Oxazolidinone is an important class of antibiotic used for treatment of infections caused by Gram-positive pathogens, being the drug linezolid the main representative of this class . This scaffold acts through the inhibition of protein synthesis by binding to the 50S ribosomal subunit and blocking the binding of transfer RNA (tRNA) . Researchers from AstraZeneca® (AstraZeneca R&D, Bangalore, India) have identified an oxazolidinone derivative, namely AZD5847 (5) (Figure 2), with outstanding antitubercular activity against a panel of several clinical isolates of Mtb with different resistance profiles, including single drug-resistant strains. AZD5847 showed improved extracellular and intracellular activity compared to linezolid, exhibiting MIC90 values in a range of 0.13 and 1 μM in the tested strains and a reduction of 1-log-unit in macrophage intracellular bacilli. Furthermore, the authors also demonstrated that this compound (5) also acts through the inhibition of protein synthesis . AZD5847 was clinically tested as an antimycobacterial drug in a phase 2; however, several adverse effects were observed, including serious hepatic and haematological toxicities . Wei and coworkers also reported a series of bis-oxazolidinone derivatives with antitubercular activity. Compound (6) (Figure 2) exhibited MIC90 values at values ranging from 2 to 8 μM against several clinical MDR and XDR-TB strains. In addition, the authors demonstrated the low cytotoxicity of this compound against monkey fibroblast-like kidney cell (VERO) with IC50 above 5000 μM and high selectivity against mycobacteria .