Synthesis and antibacterial activity of novel 7-substituted 6-fluoro-1- methylene-4-oxo-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives

Article abstract of DOI:10.3987/COM-99-8712

A series of 7-substituted 6-fluoro-1-methylene-4-oxo-4H- [1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives (2) and (3) was prepared and evaluated for antibacterial activity. These compounds were obtained by the treatment of the 1-methanesulfonyloxymethyl or 1-fluoromethyl thiazetoquinolone-3-carboxylates (12, 14 and 20) with potassium hydroxide. Compounds (2) and (3) showed excellent in vitro antibacterial activity against both gram-negative and gram-positive bacteria including quinolone and Methicillin-resistant Staphylococcus aureus.