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The University of Southampton

CHEM3002 Medicinal Chemistry

Module Overview

Aims and Objectives

Learning Outcomes

Learning Outcomes

Having successfully completed this module you will be able to:

  • Describe the overall process of drug discovery, and the role played by medicinal chemistry in this process.
  • 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.
  • Discuss examples of pharmaceutical drug discovery in detail, and relate patterns and lessons from discovery of these examples to other seen and unseen examples.
  • Predict the use of analytical methods to characterise specific materials and interpret the data in view of the material’s properties.
  • Describe the current challenges and opportunities in medicinal chemistry in light of contemporary developments in the field of drug discovery


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

Lectures, workshops

Follow-up work60
Practical classes and workshops8
Preparation for scheduled sessions48
Total study time150

Resources & Reading list

Walter Sneader. Drug Discovery: A History. 

Richard B. Silverman. The Organic Chemistry of Drug Design and Drug Action. 

Tom Brown. Nucleic Acids Book. 

Graham L. Patrick. An Introduction to Medicinal Chemistry. 

John Saunders. Top Drugs, Top Synthetic Routes. 

Jie Jack Li. Blockbuster Drugs: The Rise and Fall of the Pharmaceutical Industry. 



MethodPercentage contribution
Final Assessment   (2 hours) 100%


MethodPercentage contribution
Final Assessment   (2 hours) 100%

Repeat Information

Repeat type: Internal & External

Linked modules

Pre-requisite: CHEM2001 and CHEM2005

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