Introductory description

The module provides an introduction to medicinal chemistry at Year 2 UG level, with case studies of drug discovery from the pharmaceutical industry, and three guest lectures from external speakers.

Module web page

Module aims

Outline syllabus

This is an indicative module outline only to give an indication of the sort of topics that may be covered. Actual sessions held may differ.

1. Introduction to drug discovery process (3 lectures, 1 workshop). Overview of drug discovery process, source of lead compounds. Drug metabolism, pharmacokinetics, introduction to toxicology.
2. Enzyme catalysis & inhibition (6 lectures, 1 workshop, 1 guest lecture). Principles of protein structure, enzyme catalysis and enzyme kinetics. Examples of enzyme mechanisms, and enzymes using coenzymes (NAD, PLP). Case studies of medicinally relevant enzyme inhibitors and mechanism-based inhibitors. Beta-lactam antibiotics and antibiotic resistance.
3. Receptor agonists and antagonists (4 lectures, 1 workshop, 1 guest lecture). Case studies of drugs acting as receptor agonists and antagonists, inclusing salbutamol (asthma drug), beta-blockers (treatment for high blood pressure) and ranitidine (anti-ulcer drug).
4. Computational approaches to drug discovery (3 lectures, 1 workshop). Case studies on lead optimisation via docking, and other computational approaches to drug discovery.
5. Antibody-based drugs & molecular diagnostics (6 lectures, 1 guest lecture). Introduction to antibody structure and monoclonal antibody selection. Case studies of antibody-based drugs. Molecular diagnostics used in COVID pandemic. Discussion on ethical issues from bioactive compounds.

Learning outcomes

By the end of the module, students should be able to:

• Understand the different stages of the drug discovery process
• Apply knowledge of drug metabolism to understand why certain drug candidates might be metabolised rapidly or slowly, and how this might lead to toxicity or the design of prodrugs.
• Understand the principles of enzyme catalysis, applied to classes of drug targets such as proteases, and the mechanism of action of beta-lactam antibiotics
• Understand the mechanisms of NAD- and PLP-dependent enzymes, and be able to predict mechanisms of inactivation by mechanism-based enzyme inhibitors
• Explain receptors as drug targets, and major classes of receptor agonists and antagonists used as chemotherapeutic drugs
• Understand how computational approaches can be used in drug development
• Understand how antibody-based drugs work, and how antibodies can be used for medical diagnostics
• Critically analyse structure-activity data for drug candidates, and be able to suggest further potential chemical structures for testing.
• Present the discovery/development of a pharmaceutical drug, involving literature searching and creative presentation skills (assessed work)

Indicative reading list

“Introduction to Medicinal Chemistry”, G. Patrick, Oxford University Press (copies in Library).
“Introduction to Enzyme and Coenzyme Chemistry”, T.D.H. Bugg, Wiley (copies in Library, eBook chapters available).

Interdisciplinary

The module teaches at the chemistry/biology interface, including topics from biochemistry, pharmacology, toxicology, and immunology. Students will have an opportunity to explore these topics more through the assessed work assignment.

Subject specific skills

1. Understanding of principles of drug discovery, different types of drug targets, and case studies, used in pharmaceutical industry.
2. Understanding of protein structure and enzyme catalysis, underpinning knowledge for advanced modules and used in pharmaceutical and biotech industries.
3. Understanding of the application of computational methods for drug discovery, used in pharmaceutical industry.
4. Understanding of antibody technology, used in pharmaceutical and biotech industries.

Transferable skills

1. Critical analysis of structure-activity data for drug candidates, design of further potential chemical structures for testing. Used in pharmaceutical industry.
2. Written presentation of the discovery/development of a pharmaceutical drug.
3. Literature searching for discovery/development of a pharmaceutical drug.