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Classification and Structure-Activity Relationships of Fluoroquinolones

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Summary

Fluoroquinolones are potent broad spectrum antibacterial agents. Two classifications have been described: chemical and biological. Quinolones can be classified into 4 groups according to their chemical structures: monocyclic, bicyclic, tricyclic and tetracyclic derivatives. Each group can be subdivided into subgroups if a fluorine atom is fixed at the 6-position.

The biological classification recognised 4 groups. Groups 1 and 2 are composed of compounds showing limited spectra (Enterobacteriaceae) and groups 3 and 4 contain compounds displaying broad antibacterial spectra. Compounds that are highly metabolised fall into groups 1 and 3 and those poorly metabolised (< 5%) into groups 2 and 4.

The structure of fluoroquinolones may help to predict antibacterial activity, pharmacokinetics, physicochemical properties, toxicity and adverse events.

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Authors and Affiliations

  1. Department of Clinical Pharmacology, Roussel Uclaf, Domaine Antibiothérapie, 102 rue de Noisy, 93235, Romainville Cedex, France

    André Bryskier & Jean-François Chantot

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  1. André Bryskier
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  2. Jean-François Chantot
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Bryskier, A., Chantot, JF. Classification and Structure-Activity Relationships of Fluoroquinolones. Drugs 49 (Suppl 2), 16–28 (1995). https://doi.org/10.2165/00003495-199500492-00005

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