Antibiotic Discovery and Development

Transcription

1 Thomas J. Dougherty Michael J. Pucci Editors Antibiotic Discovery and Development ringer

2 VOLUME I Part I Introductory History of Antimicrobial Drugs 1 The Early History of Antibiotic Discovery: Empiricism Ruled Richard J. White 2 Rational Approaches to Antibacterial Discovery: Pre-Genomic Directed and Phenotypic Screening Lynn L. Silver Part Marketed Major Classes of Compounds 3 Antibiotics 79 Malcolm Page 4 Review of the Quinolone Family George A. Jacoby and David Hooper Tetracyclines 147 Patricia A. Bradford and C. Hal Jones Macrolides and 181 Xu, Michael T. Flavin, and David A. 7 Aminoglycosides 229 S. Armstrong, Corwin F. Robert T. Cass, Heinz E. Moser, W. Serio, and George H. Miller Oxazolidinone Antibacterial Agents Michael Barbachyn

3 Contents 9 Glycopeptides and Lipoglycopeptides 301 F.F. Arhin, A. Belley, A. Rafai Far, D. Lehoux, G. Moeck, and T.R. Parr Jr. Part III The Rise of Antibiotic Resistance/Resistance Mechanisms to Major Classes 10 Efflux-Mediated Antimicrobial Resistance 349 Keith Poole Structural Mechanisms of P-Lactam Antibiotic Resistance in Penicillin-Binding Proteins 397 Robert A. Nicholas and Christopher Davies 12 Evolution of p-lactamases: Past, Present, and Future 427 Karen Bush 13 Inducible Resistance to Macrolide Antibiotics 455 Sai Lakshmi Subramanian, Haripriya and Alexander S. Mankin 14 Fluoroquinolone Resistance: Mechanisms, Restrictive Dosing, and Anti-Mutant Screening Strategies for New Compounds 485 Karl Drlica, Zhao, Muhammad Malik, and Robert Kerns 15 Glycopeptide Resistance 515 Bruno Perichon and Patrice Courvalin 16 Acquired Tetracycline Resistance Genes 543 Marilyn C. Roberts Part IV Clinical Issues of Resistance: "Worst Offenders" List of Problematic Microbes Gram-positives 17 Evolution of Molecular Techniques for the Characterization Clones 571 Duarte C. Oliveira, de Lencastre, and Alexander 18 Mechanisms of Penicillin Resistance in Streptococcus pneumoniae: Targets, Gene Transfer and Mutations 593 Regine Hakenbeck, Denapaite, and Patrick Maurer 19 Clinical Aspects of Multi-Drug Resistant Enterococci 617 German A. Contreras and Cesar A. Arias

4 Contents Part V Gram-negatives 20 Clinical Issues of Resistance: Problematic Microbes: Enterobacteriaceae David F. Briceno, Julian A. Torres, Jose D. Tafur, John P. Quinn, and Maria V. Villegas 21 aeruginosa: A Persistent Pathogen in Cystic Fibrosis and Hospital-Associated Infections 679 Kristen N. Schurek, Elena B.M. Breidenstein, and Robert E.W. Hancock Part VI Mycobacteria 22 Drug Resistant and Persistent Tuberculosis: Mechanisms and Drug Development 719 Ying Zhang VOLUME II Part VII Antibiotic Discovery 23 Resistance Trends and Susceptibility Profiles in the US Among Prevalent Clinical Pathogens: Lessons from Surveillance 753 Chris Pillar and Dan 24 Chemical Properties of Antimicrobials and Their Uniqueness 793 Mark J. Macielag 25 Natural Products in the 21st Century 821 Sheo B. Singh 26 Permeability of Bacteria to Antibacterial Agents 849 Wright W. Nichols 27 Novel Antibacterial Targets/Identification of New Targets by Comparative Genomics 881 Sarah M. McLeod, Thomas J. Dougherty, and Michael J. Pucci 28 Cell-Based Screening in Antibacterial Discovery 901 Scott D. Mills and Thomas J. Dougherty 29 Enzyme-Based Screens in HTS 931 David E. and Stewart L. Fisher

5 xii Contents 30 Antibacterial Inhibitors of the Essential Cell Division Protein FtsZ 957 Lloyd G. Czaplewski, Neil R. Stokes, Steve Ruston, and David J. Haydon 31 Structure-Guided Discovery of New Antimicrobial Agents 969 Molly B. 32 NMR in Infection Research 985 Jun Hu and Gunther Kern 33 A Review of Animal Models Used for Antibiotic Andrea Marra 34 In Vivo Pharmacodynamic Modeling for Drug Discovery Jared L. Crandon and David P. Nicolau 35 Applications of Pharmacokinetic/Pharmacodynamic Models for the Development of Antimicrobial Agents 1055 April Barbour and Hartmut Derendorf Part VIII Antibiotic Drug Development 36 Antibiotic Drug Development: Moving Forward into the Clinic 1071 Jane E. Ambler and Greg G. Stone Part IX The Economics and Incentives of Antibiotic Drug Discovery 37 Stimulating Antibacterial Research and Development: Sense and Sensibility? Steven J. Index 1107