This medicinal chemistry case study is designed to introduce students to the development of antimalarial 4-aminoquinolines and the early stages of drug discovery and development. It focuses on antimalarial 4-aminoquinolines (4-AQs) and involves an introduction to malaria, its causes, societal impact and the need for new drugs. It then presents an overview of 4-AQs, their mode of action, structure activity relationships (SARs) and pharmacokinetics.