module specification

The aims of this module are aligned with the qualification descriptors within the Quality Assurance Agency’s Framework for Higher Education Qualifications.

This module will enable students to develop an understanding of the various strategies used in drug design and the molecular mechanisms by which drugs act in the body.

The module aims to: deepen students’ awareness of the major influence chemistry has had on the treatment of various diseases and debilitating conditions; enable students to assess critically the methodologies and strategies that govern whether or not a synthetic compound (i.e. new chemical entity, NCE) may be regarded as a good drug candidate.

CY5008

A brief survey of the history of medicinal chemistry from its origins in the use of natural products to molecules derived from computer-assisted design techniques. Use of data derived from approaches such as Hammet  and , QSAR/Hansch analysis, X-ray crystallography and computer modelling/bioinformatics, to determine whether a bioactive molecule may be a good lead candidate for clinical development. LO1,LO2,LO3,LO4

Examination of the individual steps needed to be taken, from the discovery of a potential new drug, to its approval and marketing. Themes such as: rational drug design (e.g. ‘Lipinski’s rule of 5’), targeted synthesis, early biological evaluation (e.g. pharmacokinetics), identification of structural leads and lead optimisation progressing to the identification of a clinically viable drug candidate, combinatorial chemistry and high throughput screening in drug discovery are examined. LO1,LO2,LO3,LO4

A number of drugs are chosen to exemplify their synthesis, mode of action and clinical impact. These include areas such as: centrally acting drugs, non-steroidal anti-inflammatory drugs and antibiotics. Special emphasis is also given to: anti-malarial agents such as artemisinin and its analogues, the anti-cancer drug Taxol and its Taxoid analogues, GPCR inhibitors such as the H2 histamine antagonists Cimetidine and Ranitidine for use in the treatment of peptic ulcer disease (PUD), HIV-reverse transcriptase inhibitors and anti-thrombotic peptidomimetics for use in the treatment of cardiovascular disease. LO1,LO2,LO3,LO4

Teaching and learning is based on lectures, tutorials and laboratory-based practical sessions. Lectures are used to set in context and deliver many aspects of the syllabus (16 hours). Other aspects are delivered through tutorials (incorporating guided study problems requiring formally presented solutions, 8 hours) and practical work (12 hours). Laboratory practical work also emphasises the importance of GLP and GMP in drug development. Pre-laboratory assignments are designed to help students prepare to work efficiently and safely in the laboratory.

On successful completion of this module students will be able to:
1. Demonstrate an understanding of the chemical synthesis, pharmacological action and clinical properties of drugs;
2. Demonstrate an understanding of the principles of pre-clinical and clinical development of a drug, and the criteria of assessment that are used to allow progression of a ‘safe’ drug into the market place;
3. Understand that as a result of incidents such as the ‘Thalidomide tragedy’, and the ‘VioxxTM perturbation’, the reasons why GLP, GMP and GCP govern the regulatory framework in which new drug candidates are developed for clinical use;
4. Survey the current literature in a given field, investigate current drug developments in this field and suggest possible future developments.

The module will be assessed by means of an end of module unseen examination (50%, 1.5 hours) which will assess the students’ abilities to think critically and solve problems, and by a practical coursework component (50%, 2000 words).
The coursework component will require completing the practical sessions and reporting
the results in an extended proforma. This constituent will also develop high level communication skills and facilitate engagement with the peer reviewed literature.
A minimum aggregate mark of 40% will be required to pass the module. If the module is
passed on reassessment, then the maximum mark awarded will be 40%.

Core Text: Patrick, G. L. (2017) An Introduction to Medicinal Chemistry, 6th Edition, OUP.

Other Texts: Patrick, G. L. (2015) An Introduction to Drug Synthesis, OUP.
Barber, J., Rostron, C. (2013) Pharmaceutical Chemistry, OUP.
Denton, P., Rostron, C. (2013) Pharmaceutics, OUP.
Davis, A., Ward, S. E. (2015) The Handbook of Medicinal Chemistry. RSC.

Journals: Students will be referred to specific papers in the peer reviewed literature.

Websites: Specific links to websites will given on Weblearn.