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The synthesis and in vitro antibacterial activity of conformationally restricted quinolone antibacterial agents
C S Cooper1, M D Tufano, P K Donner
1Anti-infective Research Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Bioorganic & Medicinal Chemistry
|August 1, 1996
Abstract:
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.