Drug Discovery and Medicinal Chemistry for the Central Nervous System


Projects involve developing novel CNS drugs through applications of organic synthesis, medicinal chemistry and pharmacological screening.


Professor Michael Kassiou

Research Location

School of Chemistry

Program Type



The Drug Discovery Research Unit is located at the Brain and Mind Research Institute and the School of Chemistry at the University of Sydney. Research is interdisciplinary and built around the key themes of medicinal chemistry and drug discovery. In this domain understanding drug-protein and drug-binding site interactions is a key component which allows us to obtain structure-activity relationships of bioactive CNS molecules and therefore the rational design of more efficacious treatments for diseases of the brain We have an extensive medicinal chemistry program evaluating structure-activity relationships of a number of molecules varying from polycyclic to heterocyclic scaffolds that interact with specific targets we think are involved in brain disease. The purpose of these studies is to identify lead molecules that can be further developed into drug candidates for the treatment of disease. These projects involve the synthesis of a series a compounds that aid in the identification of structural motifs responsible for optimizing activity. There are opportunities for exciting and challenging PhD projects in: (1) The design and synthesis of new molecular entities for neuronal and non-neuronal cells; (2) Development of structure-activity relationships of bioactive molecules; (3) Use of novel molecules for studies of receptor biology; (4) Applications of radiolabelled CNS active drugs.

Additional Information

Techniques used:

  • Organic synthesis
  • Spectroscopic characterisation
  • Molecular modelling
  • In vitro binding
  • Cell based assays
  • Immunohistochemistry

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Medicinal chemistry, drug discovery, drug design, Structure-activity relationships, Pharmacology, Receptor biology, Neuroinflammation, Molecular imaging.

Opportunity ID

The opportunity ID for this research opportunity is: 220