Synthesis and antibacterial evaluation of isoxazolinyl oxazolidinones: Search for potent antibacterial

A series of (5S) N-(3-{3-fluoro-4-[4-(3-aryl-4,5-dihydro-isoxazole-5-carbonyl)-piperazin-1-yl]-phenyl}-2-oxo-oxazolidin-5-ylmethyl)-acetamide(6a–o) were synthesized and their in vitro antibacterial activity against various resistant Gram-positive and Gram-negative bacteria were evaluated. Most of the synthesized compounds showed 2 to 10 fold lower MIC values compared to linezolid against Staphylococcus aureusATCC 25923, ATCC 70069, ATCC 29213,Bacillus cereusMTCC 430,Enterococcus faecalisMTCC439,Klebsiella pneumoniaeATCC 27736, and Streptococcus pyogens.

The synthesis and antibacterial activity of novel oxazolidinone analogues (6a–o) has been reported with 6i being the most potent compound of the series showing MIC at 0.0866–0.7039 μM.Figure optionsDownload as PowerPoint slide