Medicinal Chemistry teaches essential concepts by focusing on how the field is actually practiced, melding real-world research experience with basic principles and modern methods. Written by practicing medicinal chemists, this textbook is intended for advanced undergraduates and first-year graduate students in biology, chemistry, and biochemistry. Pre-medical or pre-pharmacy students and professionals entering the drug discovery field will also find it a useful reference. Building on a foundation of synthetic organic chemistry and structural biology, the book interweaves therapeutics, case studies, historical context, and techniques for discovering, developing, and optimizing new drugs. Chapters are richly illustrated and include problems and annotated journal references with accompanying exercises and answers.