The synthesis and in vitro antibacterial activity of conformationally restricted quinolone antibacterial agents.
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.
Cooper
C S
CS
Anti-infective Research Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Tufano
M D
MD
Donner
P K
PK
Chu
D T
DT
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation
D000890:Anti-Infective Agents; D002939:Ciprofloxacin