The 4-Quinolones: Anti Bacterial Agents in Vitro

1. Front Matter

   Pages i-xiv

   PDF

2. Quinolones as Broad-spectrum Agents

   1. Quinolones as Broad-spectrum Agents

      • H. C. Neu

      Pages 1-13

3. Effects of Physiological Cation Concentration on 4-Quinolone Absorption and Potency

   1. Effects of Physiological Cation Concentration on 4-Quinolone Absorption and Potency

      • J. T. Smith

      Pages 15-21

4. The Influence of Oxygen upon Bactericidal Potency

   1. The Influence of Oxygen upon Bactericidal Potency

      • I. Morrissey, C. S. Lewin, J. T. Smith

      Pages 23-36

5. Interactions of 4-Quinolones with Other Agents — The Importance in Assessing Practical Antibacterial Potency

   1. Interactions of 4-Quinolones with Other Agents — The Importance in Assessing Practical Antibacterial Potency

      • C. S. Lewin, J. T. Smith

      Pages 37-51

6. Molecular Effects of 4-Quinolones upon DNA Gyrase: DNA Systems

   1. Molecular Effects of 4-Quinolones upon DNA Gyrase: DNA Systems

      • G. C. Crumplin

      Pages 53-68

7. Mechanisms of Killing of Bacteria by 4-Quinolones

   1. Mechanisms of Killing of Bacteria by 4-Quinolones

      • J. S. Wolfson, D. C. Hooper

      Pages 69-85

8. Use of an In Vitro DNA Strand-Breakage Assay to Monitor Compound Interactions with DNA Gyrase

   1. Use of an In Vitro DNA Strand-Breakage Assay to Monitor Compound Interactions with DNA Gyrase

      • L. P. Elwell, L. M. Walton, J. M. Besterman, A. Hudson

      Pages 87-102

9. Comparisons of DNA Gyrases from Different Species

   1. Comparisons of DNA Gyrases from Different Species

      • N. J. Robillard, B. L. Masecar, B. Brescia, R. Celesk

      Pages 103-114

10. Structure-Activity Relationships of Fluoro-4-Quinolones

    1. Structure-Activity Relationships of Fluoro-4-Quinolones

       • L. A. Mitscher, P. V. Devasthale, R. M. Zavod

       Pages 115-146

11. Aspects of Quinolone-DNA Interactions

    1. Aspects of Quinolone-DNA Interactions

       • L. L. Shen, J. Baranowski, M. Nuss, J. Tadanier, C. Lee, D. T. W. Chu et al.

       Pages 147-158

12. Selective Toxicity: The Activities of 4-Quinolones against Eukaryotic DNA Topoisomerases

    1. Selective Toxicity: The Activities of 4-Quinolones against Eukaryotic DNA Topoisomerases

       • T. D. Gootz, J. F. Barrett, H. E. Holden, V. A. Ray, P. R. McGuirk

       Pages 159-172

13. In Vitro Genotoxicity Assessment and the Effects of 4-Quinolones upon Human Cells

    1. In Vitro Genotoxicity Assessment and the Effects of 4-Quinolones upon Human Cells

       • G. C. Crumplin

       Pages 173-200

14. Mechanisms of Resistance to 4-Quinolones

    1. Mechanisms of Resistance to 4-Quinolones

       • D. C. Hooper, J. S. Wolfson

       Pages 201-214

15. In Vitro and In Vivo Mutation Frequencies to Resistance — do they Correlate in the Long Term?

    1. In Vitro and In Vivo Mutation Frequencies to Resistance — do they Correlate in the Long Term?

       • J. T. Smith

       Pages 215-227

16. Measurement of the Frequency of Mutation to Resistance: The Importance of Testing under Physiological Conditions

    1. Measurement of the Frequency of Mutation to Resistance: The Importance of Testing under Physiological Conditions

       • M. Odell, G. C. Crumplin

       Pages 229-239

17. Plasmid-Borne Resistance to 4-Quinolones a Real or Apparent Absence?

    1. Plasmid-Borne Resistance to 4-Quinolones a Real or Apparent Absence?

       • P. Courvalin, C. Poyart-Salmeron, E. Derlot

       Pages 241-248

18. Poster Presentations

    1. Anaerobiosis and Staphylococcal Resistance to Certain 4-Quinolones

       • D. J. C. Knowles, G. T. Grimes, L. S. Holmes

       Pages 249-255

    2. Gram Negative Mutants Resistant to 4-Quinolones: Are they Competent Pathogens?

       • G. C. Crumplin

       Pages 257-268

    3. Quinolone-Resistant E. Coli Mutants Overproduce a 60 kDa Protein Highly Homologous to GroEL

       • P. Hallett, A. Mehlert, A. Maxwell

       Pages 269-273

The 4-quinolone antibacterial agents have been under development and in use for over 25 years, but despite an enormous body of research work there are still many basic questions that remain unanswered. For example, we do not know how these agents kill susceptible cells - or even how the drugs interact with the target mol- ecule(s). However, we do know that the 4-quinolones display many properties which are not shared with any other group of antibacterial agents. This book raises the unanswered questions and assesses the potential significance to future chemotherapy of their unique features. The book also raises matters which are significant for physicians as well as for the pharmaceutical industry and the assessment of these agents by legislative bodies concerned with drug safety.

• bacteria
• chemotherapy
• development
• drug
• drug safety
• research

• Department of Biology, University of York, York, UK

  Geoff C. Crumplin

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