Pre-requisite: CHEM2001 and CHEM2005
Aims and Objectives
Having successfully completed this module you will be able to:
- Discuss examples of pharmaceutical drug discovery in detail, and relate patterns and lessons from discovery of these examples to other seen and unseen examples.
- Describe the overall process of drug discovery, and the role played by medicinal chemistry in this process.
- Describe the current challenges and opportunities in medicinal chemistry in light of contemporary developments in the field of drug discovery
- Demonstrate an understanding of concepts such as drug metabolism, bioavailability and pharmacokinetics and the role of medicinal chemistry in improving these parameters.
- Relate the structure and physical properties of drugs to their pharmacological activity.
- Predict the use of analytical methods to characterise specific materials and interpret the data in view of the material’s properties.
Section 1: Introduction to medicinal chemistry:
Development of medicinal chemistry, modern small molecule drug discovery, targets for drug discovery, drug-receptor interactions, controlling drug-target interactions, examples of lead optimisation, pharmacokinetics and drug metabolism, high-throughput screening.
Examples from classic and contemporary medicinal chemistry:
This will include examples of drug discovery in the following fields: Adrenergic system (bronchodilators, β-blockers), cholinergic system (antagonists, anticholinesterases), antiulcer drugs, DNA-drug interactions (drug types - intercalators, electrophiles/alkylating agents, radicals), nucleoside drugs and prodrugs, HIV therapeutics, discovery of the migrane drug sumatriptan, antibacterials.
Tools and technology in drug discovery:
This will include an introduction to the concepts of combinatorial and parallel synthesis, along with current trends and issues in the discovery of small molecules
Learning and Teaching
Teaching and learning methods
|Practical classes and workshops||8|
|Preparation for scheduled sessions||48|
|Total study time||150|
Resources & Reading list
Richard B. Silverman. The Organic Chemistry of Drug Design and Drug Action. Academic Press.
John Saunders. Top Drugs, Top Synthetic Routes. Oxford Primer.
Walter Sneader. Drug Discovery: A History. Wiley & Sons.
Graham L. Patrick. An Introduction to Medicinal Chemistry. Oxford University Press.
Tom Brown. Nucleic Acids Book.
Jie Jack Li. Blockbuster Drugs: The Rise and Fall of the Pharmaceutical Industry. Oxford University Press.
This is how we’ll formally assess what you have learned in this module.
This is how we’ll assess you if you don’t meet the criteria to pass this module.
Repeat type: Internal & External