Semisynthesis of Bioactive Compounds and their Biological Activities explores the potential benefits of semisynthetic derivatives obtained from nature. Sections cover the natural distribution of parent compounds, semisynthesis and biological properties of semisynthetic derivatives, the applications of semisynthetic derivatives in diverse fields such as drug delivery, food production and medicine, an explanation of the current resistance mechanisms of antibiotics, clinical applications of semisynthetic analogues, the functions of plant alkaloids on human health, potential agricultural biotechnology in semisynthetic derivatives, and semisynthesis of natural products under greener conditions, this book provides a comprehensive resource on the topics presented. Sections include information about alternative sources of energy and superior greener technologies (microwave, sonochemistry), alternative reaction media (water, supercritical CO2, ionic liquids) and alternative eco-friendly catalysts (biocatalysts). This book will be an excellent resource for academicians, researchers and students focusing on synthesis as well as the biological community and industry professionals in drug development. – Focuses on the current resistance mechanisms of antibiotics, chemical derivatization of antibiotics, and clinical applications of semisynthetic derivatives. – Includes discussion of the semisynthesis of natural products using green tools, green solvents, and eco-friendly catalysts. – Illustrates the concept of toxicity, the merits of transition-metal-free reactions, and the semisynthesis of natural products by introducing the oxygen atom(s) under transition-metal-free conditions.