Macrolide Antibiotics

1. Front Matter

   Pages I-X

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2. Introduction to the macrolide antibiotics

   • Herbert A. Kirst

   Pages 1-13

3. Macrolides: a clinical overview

   • Vito R. Iacoviello, Stephen H. Zinner

   Pages 15-24

4. Pharmacokinetics/pharmacodynamics of macrolides

   • Holly M. Mattoes, Charles H. Nightingale

   Pages 25-36

5. Cellular accumulation of macrolide antibiotics. Intracellular bioactivity

   • Marie-Thérèse Labro

   Pages 37-52

6. Clarithromycin and new derivatives of erythromycin

   • Takashi Adachi, Shigeo Morimoto

   Pages 53-72

7. Azithromycin and novel azalides

   • Wolfgang Schönfeld, Stjepan Mutak

   Pages 73-95

8. Ketolides: novel antibacterial agents designed to overcome resistance to erythromycin A within gram-positive cocci

   • André Bryskier, Alexis Denis

   Pages 97-140

9. Novel macrolide derivatives active against resistant pathogens

   • Ly T. Phan, Zhenkun Ma

   Pages 141-155

10. Polyketide diversity

    • Leonard Katz

    Pages 157-175

11. Biosynthesis of the macrolide antibiotic, tylosin

    • Eric Cundliffe

    Pages 177-184

12. In vitro activity of macrolides against traditional susceptible bacteria

    • Adel Ben Ali, Fred W. Goldstein, Jacques F. Acar

    Pages 185-200

13. Activity of macrolides against mycobacteria

    • Lowell S. Young, Luiz E. Bermudez

    Pages 201-213

14. Chlamydia pneumoniae and asthma and atherosclerosis: role of macrolides

    • Margaret R. Hammerschlag

    Pages 215-228

15. Activity of macrolides in sexually transmitted diseases

    • Geoffrey L. Ridgway

    Pages 229-241

16. Helicobacter pylori and macrolides

    • Francis Mégraud

    Pages 243-260

17. Effects of macrolide antibiotics on ribosome function

    • Norris E. Allen

    Pages 261-280

18. Mechanisms of resistance to macrolides, lincosamides, and ketolides

    • Joyce A Sutcliffe, Roland Leclercq

    Pages 281-317

19. Back Matter

    Pages 319-323

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There are only very few chemical classes of antibiotics in medical use, and these have originated over a span of more than 60 years of research. Almost half a century ago, the first member of the macrolides, erythromycin, was introduced as a treatment option for bacterial infections. Erythromycin is a very complex fermentation product obtained from the soil bacterium Saccharopolyspora ery­ thraea (originally named Streptomyces erythreus). The success of erythromycin, based on its efficacy and tolerability, stimulated researchers throughout the world to undertake intense efforts to understand the biology and chemistry of macrolides and to use this experience to improve the properties of this compound class. The second generation of macrolides, based on chemical modifications of erythromy­ cin, is currently being in broad use, especially for treatment of respiratory tract infections. We presently foresee the introduction of a new generation of macro­ lides, i. e. the ketolides, which have the potential to overcome rising resistance problems. This monograph is intended to give the interested reader an overview on "macrolide experience", covering important areas from basic research to clinical use. Starting from a historic overview, the essential basic parameters - efficacy, pharmacokinetics, pharmacodynamics, and pharmacology - are highlighted in order to introduce the reader to the rationale for clinical use of macrolides. The following group of chapters cover the complex chemistry of the macro­ lactone structures, giving historic background, basic structure-activity relation­ ships of various derivatization strategies, and perspectives for future discovery of new semisynthetic macrolide antibiotics.

• Antibiotika
• Infektionskrankheiten
• Sexually Transmitted Diseases
• antibiotics
• asthma
• bacteria
• bacterial infection
• bacterial infections
• infection
• infections
• infectious disease
• tissue
• infectious diseases

• PLIVA Research Antiinfective Research, Zagreb, Croatia

  Wolfgang Schönfeld

• Elanco Animal Health Research & Development, Greenfield, USA

  Herbert A. Kirst

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