Using current research and real-life scenarios to motivate students to understand chemistry principles is a key strategy in learning and teaching. An illustration of psychoactive drugs referred to as "legal highs" used in the U.K. and Europe is presented to highlight key chemistry principles and relate the importance of chemistry research in healthcare. Specific topics include stereochemistry, 1 H NMR characterization, organic synthesis, and functional groups, which can be used in chemistry curricula for high school students and also in higher education programs. A contextualized example focused on mephedrone is used during an interpretative spectroscopy exercise in a second-year bioscience program. Student evaluations on the use of this case study approach were very positive. This topic on psychoactive drugs integrates chemistry in social and legal issues relating to patient safety. It highlights public awareness of "legal highs" and the generalized perception that "natural products" are safe and nontoxic.