Chemistry and Mechanism of Action of the Quinolone Antibacterials

Katherine E. Brighty* and Thomas D. Gootz^

*Department of Medicinal Chemistry and ^Department of Respiratory, Allergy, Immunology, Inflammation, and Infectious Diseases, Central Research Division, Pfizer, Inc., Groton, Connecticut 06340

Introduction

Structural and Historical Background

General Structural Features of the Quinolones First-Generation Quinolones Second-Generation Quinolones Third- and Fourth-Generation Quinolones

In vitro Potency In vivo Activity

Selectivity: Activity against Mammalian Topoisomerase II

and Genetic Toxicity Chemical Properties Future Directions

Compounds Lacking the C-6 Fluorine 2-Pyridones

Alteration of Primary Enzymatic Target Mechanism of Action Replication of DNA Bacterial Topoisomerases Topoisomerase Sensitivity to Fluoroquinolones Killing of Bacterial Cells by Fluoroquinolones Conclusion References

The Quinolones, Third Edition

Copyright © 2000 by Academic Press. All rights of reproduction in any form reserved.

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