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This book provides perspectives on the combinatorial approach of plant-based compounds for drug discovery to achieve better disease-curing outcomes introducing the evolution of ethnobotany and traditional medicine in modern drug development. It covers the biotechnological interventions for the identification and screening of compounds and their optimization to enhance affinity, selectivity, bioavailability, and metabolic stability. While overviewing how essential compounds are successfully identified from herbal/ medicinal plants and utilized in the form of effective drugs which eventually have helped in combating long-term diseases in humans, the book also provides a better understanding of how infection and the diseases caused are regulated at the molecular and physiological stages. The book also highlights the importance of bioactive compounds in modern drug discovery and the perspectives for a potential industrial application. The chapters are developed by eminent subject experts with due care and clarity and cover an up-to-date literature review with relevant illustrations. The book would cater to the needs of undergraduate and graduate students, researchers, and scientists, and may attract the attention of pharmaceutical companies/industrialists and health policymakers.