Pre-requisites: CHEM3038 or CHEM6095
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 synthesis of important target compounds.
- Describe the current challenges and opportunities in medicinal chemistry in light of contemporary developments in the field of drug discovery
- Relate the structure and physical properties of drugs to their pharmacological activity.
- Demonstrate an understanding of concepts such as drug metabolism, bioavailability and pharmacokinetics and the role of medicinal chemistry in improving these parameters.
- Describe the overall process of drug discovery, and the role played by medicinal chemistry in this process.
- Analysis of the high impact scientific literature relating to Medicinal Chemistry
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
|Preparation for scheduled sessions||48|
|Practical classes and workshops||8|
|Total study time||150|
Resources & Reading list
Graham L. Patrick. An Introduction to Medicinal Chemistry. Oxford University Press.
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.
Tom Brown. Nucleic Acids Book.
Jie Jack Li. Blockbuster Drugs: The Rise and Fall of the Pharmaceutical Industry. Oxford University Press.
Examination (70%) and Coursework (30%)
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.
|Assignment Marks carried forward||30%|