The fluoroquinolone antibacterial agents.
In summary, the last decade has been a highly fertile and productive period in quinolone medicinal chemistry, resulting in major improvements in potency, antibacterial spectra, oral absorption and pharmacokinetic properties as well as an increased knowledge of the molecular features important to conferring these various properties. Very recent discoveries concerning replacements for the 3-carboxylic acid moiety, previously thought to be uniquely essential for activity, to give highly potent antibacterials such as (83) illustrate the potential for new breakthroughs in this field. Among the major goals for future research remains the understanding of the potential cartilage toxicity associated with this class of agents, such that an agent useful for pediatric indications may be developed. Future studies can also be expected to further enhance and refine the level of current insight into the manner by which these agents inhibit the target enzyme on a molecular level.
Rosen
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Department of Medicinal Chemistry, Pfizer Central Research, Groton, CT 06340.
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000627:therapeutic use*; D001419:Bacteria / Q000187:drug effects*; D006801:Humans; D013329:Structure-Activity Relationship
D042462:4-Quinolones; D000890:Anti-Infective Agents