Medicinal Chemistry

Learning Outcomes

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.
• 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
• Relate the structure and physical properties of drugs to their pharmacological activity.
• Describe the overall process of drug discovery, and the role played by medicinal chemistry in this process.
• Discuss examples of pharmaceutical drug discovery in detail, and relate patterns and lessons from discovery of these examples to other seen and unseen examples.

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.

Teaching and learning methods

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

Resources & Reading list

Textbooks

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.

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

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

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

Summative

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

Referral

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

Repeat Information

Repeat type: Internal & External