RESUMO
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.
Assuntos
Antituberculosos/síntese química , Oxazolidinonas/síntese química , Tioureia/análogos & derivados , Tioureia/síntese química , Antituberculosos/química , Antituberculosos/farmacologia , Testes de Sensibilidade Microbiana , Estrutura Molecular , Mycobacterium/classificação , Mycobacterium/efeitos dos fármacos , Oxazolidinonas/química , Oxazolidinonas/farmacologia , Tioureia/farmacologiaRESUMO
A series of novel (un)substituted benzotriazolyl oxazolidinone derivatives has been synthesized and tested for in vitro antibacterial activities by MIC determination against a panel of susceptible and resistant Gram-positive and Gram-negative microorganisms, some of which are resistant to methicillin and vancomycin. Compounds 20, 21, 24, 29 and 30 from this series were found to be equipotent or more potent than linezolid in vitro.
