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.
Dixit
Prasad P
PP
Medicinal Chemistry Division, New Chemical Entity Research, Lupin Research Park, Village Nande, Taluka Mulshi, Pune, Maharashtra, India.
Patil
Vijaykumar J
VJ
Nair
Prathap S
PS
Jain
Sanjay
S
Sinha
Neelima
N
Arora
Sudershan K
SK
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009161:Mycobacterium / Q000145:classification / Q000187:drug effects; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013890:Thiourea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
D000995:Antitubercular Agents; D023303:Oxazolidinones; D013890:Thiourea