The synthesis and in vitro antibacterial activity of conformationally restricted quinolone antibacterial agents Original Research Article

Two series of conformationally restricted quinolone antibacterials were synthesized. One series was restricted by formation of a tetrahydrofuran ring between the C-6 position and the C-7 position of the quinolone ring skeleton. The second series achieved conformational rigidity by formation of a tetrahydrofuran ring between the C-7 and the C-8 positions. These compounds were evaluated for their in vitro antibacterial activity. Compounds 19 and 20 were the most active compounds in either series and were about equipotent.