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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.
List of contents
1 Quinolones as Broad-Spectrum Agents.- 2 Effects of Physiological Cation Concentration on 4-Quinolone Absorption and Potency.- 3 The Influence of Oxygen upon Bactericidal Potency.- 4 Interactions of 4-Quinolones with Other Agents - the Importance in Assessing Practical Antibacterial Potency.- 5 Molecular Effects of 4-Quinolones upon DNA Gyrase.- 6 Mechanisms of Killing of Bacteria by 4-Quinolones.- 7 Use of an in vitro DNA Strand-Breakage Assay to Monitor Compound Interactions with DNA Gyrase.- 8 Comparisons of DNA Gyrases from Different Species.- 9 Structure-activity Relationships of Fluoro-4-Quinolones.- 10 Aspects of Quinolone-DNA Interactions.- 11 Selective Toxicity: the Activities of 4-Quinolones against Eukaryotic DNA Topoisomerases.- 12 In vitro Genotoxity Assessment and the Effects of 4-Quinolones upon Human Cells.- 13 Mechanisms of Bacterial Resistance to 4-Quinolones.- 14 In vitro and in vivo Mutation Frequencies to Resistance - do they Correlate in the Long Term?.- 15 Measurement of the Frequency of Mutation to Resistance - the Importance of Testing under Physiological Conditions.- 16 Plasmid-borne Resistance to 4-Quinolones - a Real or an Apparent Absence?.- Poster Presentations.- Anaerobiosis and staphylococcal resistance to certain 4-quinolones.- Gram Negative Mutants Resistant to 4-Quinolones: Are they Competent Pathogens?.- Quinolone-Resistant E. Coli Mutants Overproduce a 60 kDa Protein Highly Homologous to GroEL.
