MChem Chemistry with Medicinal Chemistry

On successful completion of the course students should be able to:

1. Be able to understand and explain how medicinal chemistry has in the past approached drug           discovery and articulate the limitations of these approaches.

2. Describe and rationalize new approaches including HT, Fragment-Based Drug Discovery and virtual screening, and discuss and critically analyse HTS data outcomes.

3. Explain, calculate and apply drug physical characteristics such as ligand efficiency (LE) and lipid ligand efficiency (LipE). Define Lipinski’s rule and be able to apply to drug candidates.

4. Identify and explain examples of drug synthesis using reaction types that have been presented in lecture material or made available as on-line material, including providing mechanistic explanations for the outcome of synthetic schemes.

5. Suggest reaction processes, reagents and mechanisms, for specific drug synthetic steps provided.

6. Discuss specific drug development case histories articulating candidate selection criteria.

7. Describe and discuss importance of bioavailability, provide an account of processes for drug formulation, including aspects relevant to manufacture (tableting, particle size etc), as well as drug delivery.

8. Provide explanations of the key features of clinical trials, being able to explain important characteristics of trials.

9. Discuss the importance of drug-drug interactions and be able to explain case history examples.

Part 1: (Dr Allan Jordan and Dr. Ali Raoof): Historical perspective and failings of traditional medicinal chemistry, hit finding technologies (including fragment-based drug design, HT screening and virtual screening), target ID and target validation, Lipinski’s rules as guidelines/learnings from past failures, routes of Administration & Drug Delivery Systems, metabolism and its importance in drug design, SAR, personalized medicine and biomarkers, and oncology case studies showing contrasting use of technologies and timeline reduction
Part 2:    
Top Reactions (Dr. John Gardiner): Common Structural Types found in Medicinal Agents; Exemplification of most-used chemical transformations. The organic reactions that underpin contemporary medicinal chemistry will be discussed in detail. For example, the course will cover amide bond formation, metal-catalyzed cross-couplings, heterocycle synthesis and modification and approaches to the asymmetric synthesis of drug candidates where applicable. 
Part 3: 
Clinical and Preclinical development (Prof. Alex Galetin, Dr Doug Steinke, Dr. Katharina Edkins): This section will cover new directions in clinical development of medicines, covering aspects of drug absorption, drug-drug interactions and new drug delivery. The final journey in the drug development pathway is making sure that the medication works in humans. This section will describe clinical trials where the new medication is tested in humans to determine dose, adverse drug reactions and efficacy of the drug on a disease and provide a virtual experience of a clinical trial. Post marketing surveillance of the medication once available to the market will also be examined.