Medicinal Chemistry | CHEM3002 | University of Southampton

Module overview

Medicinal Chemistry is pivotal in the design, synthesis and evaluation of new medicines, and involves multidisciplinary research at the interface of Chemistry, Biology and Medicine. This module will introduce key molecular concepts and methods in Medicinal Chemistry, and the central role played by chemists in the development of drug candidates targeting diverse disease states and their associated biomolecular targets (for example proteins, DNA). Through important historical case studies, we will discuss the properties and modes of action of pharmaceuticals in biological systems, from “classical” inhibitors to more contemporary and cutting-edge bioactive compounds, such as protein degraders, pharmacological chaperones, and targeted covalent inhibitors. Students will have access to a broad range of resources, including recent specialist literature and software, along with additional recorded content that illustrate important concepts covered in the lectures.

Linked modules

Pre-requisite: CHEM2001 and CHEM2005

Aims and Objectives

Learning Outcomes

Having successfully completed this module you will be able to:

Predict the use of analytical methods to characterise specific materials and interpret the data in view of the material’s properties.
Describe the overall process of drug discovery, and the role played by medicinal chemistry in this process.
Demonstrate an understanding of concepts such as drug metabolism, bioavailability and pharmacokinetics and the role of medicinal chemistry in improving these parameters.
Describe the current challenges and opportunities in medicinal chemistry in light of contemporary developments in the field of drug discovery
Discuss examples of pharmaceutical drug discovery in detail, and relate patterns and lessons from discovery of these examples to other seen and unseen examples.
Relate the structure and physical properties of drugs to their pharmacological activity.

Syllabus

The course includes an introduction to the principles of medicinal chemistry:

Targets for drug discovery
Drug-receptor interactions
Controlling drug-target interactions
Lead optimisation
Pharmacokinetics and drug metabolism
High-throughput screening
Small molecule drug discovery; concepts of combinatorial and parallel synthesis

Case studies from classic and contemporary medicinal chemistry include:

G protein-coupled receptors as drug targets: adrenergic system (β-blockers and asthma), antihistamine and antiulcer drugs
DNA-targeting agents: intercalators, electrophiles/alkylating agents, and radicals
Screening technologies: Fragment Based Drug Discovery and biophysical methods
Mode of action and bioactivity of lead compounds targeting proteins: occupancy-based inhibitors, proteolysis targeting chimera, targeted covalent inhibitors
Discovery and development and drugs to treat of the migraine
AIDS and HIV: drug targets and therapeutics
Antibacterial agents history, development and resistance
Cardiovascular drugs: angiotensin converting enzyme inhibitors
Nucleoside drugs and prodrugs

The course also includes a guest lecture from the pharmaceutical sector.

Learning and Teaching

Teaching and learning methods

Lectures, workshops, problems sessions and revision classes including one industrial lecture

Study time
Type	Hours
Preparation for scheduled sessions	48
Follow-up work	60
Lecture	24
Practical classes and workshops	8
Revision	10
Total study time	150

Resources & Reading list

Textbooks

John Saunders. Top Drugs, Top Synthetic Routes. Oxford Primer.

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

Walter Sneader. Drug Discovery: A History. Wiley & Sons.

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

Graham L. Patrick. An Introduction to Medicinal Chemistry. Oxford University Press.

Tom Brown. Nucleic Acids Book.

Assessment

Summative

This is how we’ll formally assess what you have learned in this module.

Breakdown
Method	Percentage contribution
Final Assessment	100%

Referral

This is how we’ll assess you if you don’t meet the criteria to pass this module.

Breakdown
Method	Percentage contribution
Final Assessment	100%

Repeat Information

Repeat type: Internal & External