Medicinal chemistry is an interdisciplinary field of study combining aspects of organic chemistry, physical chemistry, pharmacology, microbiology, biochemistry, as well as computational chemistry. Medicinal chemistry is concerned with the discovery, design, synthesis, and interactions of a pharmaceutical agent (drug) with the body. Medicinal chemistry is mainly concerned with small organic molecules both natural and synthetic. Compounds in clinical use are primarily small organic compounds. Organometallic compounds, biopharmaceuticals, and inorganic compounds are also used in medicine as therapeutics. This book aims to provide you with a comprehensive understanding of the fundamental principles and concepts that underpin medicinal chemistry. Whether you are a student embarking on a career in pharmaceutical sciences, a researcher seeking to broaden your knowledge, or a healthcare professional interested in the intricacies of drug discovery, this book will serve as a valuable resource. Throughout the chapters, the book delves into the key aspects of medicinal chemistry, exploring various topics including drug targets, drug design, structure-activity relationships, synthesis techniques, pharmacology, and toxicology. By examining the intricate relationships between chemical structures and biological activities, the authors aim to unravel the strategies employed to optimize drug efficacy while minimizing adverse effects.