Bioactive Polyphenols in Drug Discovery

Plant polyphenols are a broad class of phytoconstituents showing a potential research interest because of their potential health benefits. This chapter presents an extensive overview of biologically active polyphenols in drug discovery, covering their classification, chemical properties, synthesis, and pharmacological effects. The evolution of polyphenol chemistry is traced from early uses in leather tanning to modern applications in medicine and materials science. Key structural classes, like condensed tannins, hydrolyzable tannins, and flavonoids, are described, along with their characteristic chemical reactions and biosynthetic pathways. Synthetic approaches for accessing complex polyphenolic scaffolds are reviewed, including oxidative coupling, biomimetic transformations, and total synthesis of natural products. Structure—activity relationships and molecular mechanisms of action are examined. Overall, this chapter highlights the continuing importance of polyphenols as lead compounds and inspiration for drug discovery efforts across multiple therapeutic areas.