PH4S020 - Advanced Medicinal Chemistry 01 Apr 2025 - 31 Aug 2027 | Version 2

Associated Module Information

Module Code: PH4S020
Module Title: Advanced Medicinal Chemistry
Faculty: Faculty of Computing, Engineering and Science
Faculty Group: Chemical and Environmental Sciences
Faculty Sub Group:
Module Leader: Andrew Graham, Suzanna Kean
Module Team: Rehana Karim
First Intended Intake: SEP 2024 Final Year of Intake:
Date Closed:
Credit Value: 20 Credit Level: 7
Language: English
Percentage of Module Taught in Welsh:
Equivalent Module:
HECOS codes: 100420 - medicinal chemistry
HECOS Code Weighting: 100

Document Version Information

Version 2
Valid From 01 Apr 2025
Valid To 31 Aug 2027

Module Aims

To apply chemical principles to illustrate and understand the mechanisms of drug action, small molecule drug design and synthesis. 

To understand the biological, physicochemical and physiological principles involved in drug adsorption and distribution and the importance of pharmacokinetic principles and their influence on drug action. 

To develop knowledge of antibacterial agents, their mode of action, structure-activity-relationships (SAR) and syntheses. 

To appreciate the chemical reactivity, synthesis, and structure of amino acids, proteins and peptides, and their role in medicine. 

 

Content Summary

1. Introduction to Drug Design 

An introduction to fundamental aspects of medicinal and pharmaceutical chemistry.  

Development of pharmaceutical chemistry and future directions. 

 Basic structural requirements for pharmaceutical activity (Lipinski rule of 5) including physicochemical, stereoisomeric and electronic properties of drug molecules and intermolecular forces.  

Drug targets including drug receptors, enzymes and non-specific interactions, and drug binding interactions.  

Fundamentals of pharmacokinetics and pharmacodynamics including partitioning of drugs and drug transport and routes of administration.  

Basic drug design, development and lead compound identification.  

Fundamentals of structure-activity relationships and quantitative structure-activity relationships including case studies on the design and development of salbutamol, propranolol and cimetidine. 

2. Antibiotics and Protein Chemistry 

Antibiotics chemistry focuses on the germ theory of disease and bacteria, history of antibiotics, sulfonamide drugs and ß-lactam antibiotics. The early development of sulfanilamide and the sulfonamide drugs, mode of action, synthesis of sulfanilamide, structure-activity-relationships (SAR), the N-heterocyclic sulfonamide drugs and the problem of drug-resistance. 

History of penicillin, structure and biosynthesis, mode of action, structure-activity-relationships (SAR), and related synthetic aspects and drug-resistance to ß-lactam antibiotics and the future of antibiotics.   

Protein chemistry focuses on the structure and properties of a-amino acids. Proteins structure/organization. Peptides, structure and synthesis (solution phase/solid phase peptide synthesis strategies). 

Learning and Teaching Methods

Activity Type Hours
Lecture? 9
Practical Classes and Workshops 24
Independent Study? 100
Problem/Challenge based learning 3
Directed Study 64
Total Hours Selected 200

Learning Outcomes

# Learning Outcome
LO1 Demonstrate knowledge of basic drug design, development, synthesis, and approaches to lead compound identification and the individual factors required for effective drug action, biology and pharmacology, and their interdependence (with a focus on biologics, e.g., proteins/peptides and traditional ‘small’ molecules).
LO2 Apply diagnostic and creative skills to review, analyse and interpret fundamental aspects of medicinal and pharmaceutical chemistry.

Module Requisites

N/A

Assessment Criteria

Assessment Category Assessment Type Description Duration Word Count Weight (%) Best of? Pass Mark
Asynchronous Assessment Report 1 Written assignment covering the topics presented in the module 0 3000 80 No 40
Asynchronous Assessment Practical Written Work 1 Written report on practical exploration of modern methods for determination of physicochemical parameters 0 1000 20 No 40

Assessment Matrix

Assessment Type Learning Outcomes
LO1 LO2
Report 1
Practical Written Work 1

Reading List

  1. G. L. Patrick,  An Introduction to Medicinal Chemistry,  Oxford University Press, Oxford, 5th edn., 2013. 

  1. G. L. Patrick,  An Introduction to Drug Synthesis, Oxford University Press, Oxford, 2014. 

  1. J. M. Ritter, R. Flower, G. Henderson, Y. K. Loke, D. MacEwan, H. P. Rang, Rang & Dales’s Pharmacology, Elsevier, Edinburgh, 9th edn., 2020. 

  1. J. Barber, C. Rostron, Pharmaceutical Chemistry, Oxford University Press, Oxford, 2013. 

  1. J. Jones, Amino Acid and Peptide Synthesis, Oxford University Press, Oxford, 1992.