Medicinal Chemistry begins with the history of the field, starting from the serendipitous use of plant preparations to current practice of design- and target-based screening methods. Written from the perspective of practicing medicinal chemists, the text covers key drug discovery activities such as pharmacokinetics and patenting, as well as the classes and structures of drug targets (receptors, enzymes, nucleic acids, and protein-protein and lipid interactions) with numerous examples of drugs acting at each type. Selected therapeutic areas include drugs to treat cancer, infectious diseases, and central nervous system disorders. Throughout the book, historical and current examples illustrate the progress to market and case studies explore the applications of concepts discussed in the text. Each chapter features a Journal Club, as well as review and application questions to enhance and test comprehension. This textbook is ideal for upper-level undergraduates and graduate students taking a one-semester survey course on medicinal chemistry and/or drug discovery, as well as scientists entering the pharmaceutical industry.