A detailed account of information regarding the discovery of drugs and their development has been highlighted in this book. Utilization of plants, microorganisms and animals for medicinal purposes has been an integral part of human evolution. Is it possible that this knowledge can be employed to formulate effective novel drugs and solve some of the human health problems that we are facing presently? This book attempts to explore the answers to this question with insightful researches in various domains of drug discovery and development. It is a compilation of contributions from a veteran team of biologists, agronomists, policy makers and chemists who have elucidated some of the procedures concerned with the development of a naturally occurring bioactive compound into a drug therapy. They have attempted to define a naturally occurring compound as well as describe the procedures needed to find, extract and outline a naturally-derived bioactive molecule. Also, they have emphasized on the need for comprehending the elementary mechanisms of disease before using bioactive molecules in bioassay-guided drug discovery platforms.