Synthesis of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives as antituberculosis agents

In continuation of our research program for new antituberculosis drugs, we have designed, synthesized and evaluated antimycobacterial activity of new series of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives against different Mycobacterium species i.e. M. tuberculosis, M. avium and M. intracellulare in an agar dilution method. Compound 17 exhibited excellent antimycobacterial activity (in vitro) against drug sensitive and resistant clinical isolates of M. tuberculosis. Its MIC value is equivalent to linezolid and superior to isoniazid against all these strains.

Graphical AbstractPreliminary communicationSynthesis and in vitro antituberculosis activity of some new oxazolidinone-benzotriazole derivatives 11–20 has been described.Figure optionsDownload full-size imageDownload as PowerPoint slide