Macrolide antibiotics

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Only a few chemical classes of antibiotics are in medical use, developed over more than 60 years of research. Erythromycin, the first macrolide introduced nearly half a century ago, is derived from the soil bacterium Saccharopolyspora erythraea. Its success due to efficacy and tolerability spurred global research into macrolides, leading to improvements in this compound class. The second generation of macrolides, modified from erythromycin, is widely used, particularly for respiratory infections. A new generation, the ketolides, is anticipated to address rising resistance issues. This monograph provides an overview of "macrolide experience," detailing essential areas from basic research to clinical application. It begins with a historical overview and highlights key parameters such as efficacy, pharmacokinetics, pharmacodynamics, and pharmacology to explain the rationale for clinical use. Subsequent chapters delve into the complex chemistry of macrolactone structures, offering historical context, structure-activity relationships of various derivatization strategies, and future prospects for discovering new semisynthetic macrolide antibiotics.