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This book, “Phytochemistry and Pharmacological Basis of Medicinal Plants,” has been carefully designed to provide undergraduate and postgraduate pharmacy students, research scholars, academicians, and professionals with a comprehensive understanding of medicinal plants from both classical and modern scientific perspectives. The contents have been organized systematically to bridge the gap between traditional knowledge and contemporary pharmaceutical sciences. The book begins with the fundamental principles of Pharmacognosy and Phytochemistry, followed by an in-depth discussion of the biosynthesis of plant secondary metabolites. Subsequent chapters comprehensively explain the chemistry, biosynthesis, pharmacological activities, and structure–activity relationships of major classes of phytochemicals, including alkaloids, glycosides, flavonoids, tannins, terpenoids, and essential oils. Considerable emphasis has been placed on the relationship between chemical constituents and their biological activities to help readers appreciate the scientific basis of medicinal plants.