Handbook

This course will provide students with an understanding of what medicinal chemistry is and how it is carried out. It will describe the interdisciplinary process of how small-molecule drugs are designed and developed. The course begins with an introduction to different classes of drug targets (e.g. DNA, enzymes, receptors). The various sources of small-molecule lead compounds are then examined, including examples from Australian traditional medicine. The concepts of pharmacodynamics and pharmacokinetics are investigated, building upon earlier studies of intermolecular forces and structure determination. Several valuable computational tools for drug development are introduced (e.g. docking, logP prediction). Strategies for lead optimisation are examined (e.g. isosteric replacements; metabolic fixes; rigidification; simplification; extension). Finally, an introduction to clinical trials is provided. Throughout the course, many examples of contemporary drug development (e.g. antiviral drugs to treat COVID-19) will be presented, and a strong emphasis will be placed on peer learning through a series of student-led workshops.