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The University of Southampton

CHEM6092 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.
  • 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
  • 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

Lectures, workshops

Practical classes and workshops8
Follow-up work50
Assessment tasks10
Preparation for scheduled sessions48
Total study time150

Resources & Reading list

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

John Saunders. Top Drugs, Top Synthetic Routes. 

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

Graham L. Patrick. An Introduction to Medicinal Chemistry. 

Tom Brown. Nucleic Acids Book. 

Walter Sneader. Drug Discovery: A History. 


Assessment Strategy

Examination (70%) and Coursework (30%)


MethodPercentage contribution
Assignment  (1000 words) 30%
Final Assessment   (2 hours) 70%


MethodPercentage contribution
Assignment Marks carried forward 30%
Final Assessment   (2 hours) 70%

Linked modules

Pre-requisites: CHEM3038 or CHEM6095

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