Macquarie University

Medicinal Chemistry - CBMS606

Medicinal chemistry is the application of chemistry to the discovery, design and synthesis of new drugs. This unit is of value to all chemistry, biomolecular sciences and medical sciences students. The central core of the unit is the description of methods used for the discovery of new drugs, how these are modified to produce more active compounds, transportation to and from their points of action and how they are cleared from the body. Topics include: the structure and function of biological targets (proteins and DNA); sources of new drugs from nature; and lead generation and methods of lead modification to make more active, selective or less toxic drugs. This is followed by a study of structure – activity relationship methods; pharmacokinetics, drug metabolism and prodrugs, and chemical genetics. Case studies are also provided, including antibacterial and anticancer agents, and nucleic acid therapies. The theory is complemented by a discovery-based laboratory project incorporating synthetic chemistry, spectroscopic methods and bioassays to elucidate the essential structural features necessary for the sulfonamide class of antibacterial agents.