Macrolide Antibiotics

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There are only a few classes of antibiotics in medical use, developed over more than 60 years of research. Erythromycin, the first macrolide introduced nearly half a century ago, is a complex fermentation product from the soil bacterium Saccharopolyspora erythraea. Its success, due to efficacy and tolerability, spurred global research into macrolides, leading to improved compounds. The second generation of macrolides, derived from erythromycin, is widely used for respiratory infections. A new generation, the ketolides, is emerging to address rising resistance issues. This monograph provides an overview of "macrolide experience," encompassing essential areas from basic research to clinical application. It begins with a historical overview, highlighting key parameters such as efficacy, pharmacokinetics, pharmacodynamics, and pharmacology, which underpin the clinical use of macrolides. Subsequent chapters delve into the complex chemistry of macrolactone structures, offering historical context, structure-activity relationships, and insights into future discovery of new semisynthetic macrolide antibiotics.