Medicinal chemistry and pharmacology are closely associated fields. They are concerned with the design and synthesis of drugs for the pharmaceutical industry. These drugs are generally organic compounds and can be divided into classes of biologics and small organic compounds. Medicinal chemistry is focused on the production of small organic molecules such as atorvastatin, fluticasone, clopidogrel, etc. The principles of synthetic organic chemistry, computational chemistry, enzymology, structural biology and chemical biology are integrated in medicinal chemistry. The study of drugs and their effects on the living body are explored in pharmacology. It involves the research, discovery and characterization of the chemicals that exhibit a biological effect. All therapies that are designed to target diseases, defects and pathogens and also advance preventive care, diagnostics and personalized medicine are a result of tremendous research in pharmacology. This book is a compilation of chapters that discuss the most vital concepts and emerging trends in the fields of medicinal chemistry and pharmacology. The various advancements in these fields are glanced at and their applications as well as ramifications are looked at in detail. This book is a vital tool for all researching and studying pharmaceutical science and medicinal chemistry.