Module manager: Dr Richard Foster
Email: r.foster@leeds.ac.uk
Taught: Semester 1 (Sep to Jan) View Timetable
Year running 2024/25
Level 1 in Medicinal Chemistry or equivalent
| CHEM1101 | Chemistry 1: Bonding and Behaviour |
CHEM2115 Introduction to Drug Design
This module is not approved as a discovery module
On completion of this module, students should be able to:
- understand the principle modes of binding of small drug molecules to biological macromolecules;
- identify key recognition features in drug molecules;
- identify the pharmacophore and design new potential drug molecules using the principles of rational structure modification;
- interpret structure activity relationships in terms of binding models and bioavailability;
- understand basic cell signalling pathways and the role of receptor agonists and antagonists in medicinal chemistry;
- use the principles of quantitative structure activity relationships to increase the efficiency of the drug design process;
- understand the principles of drug absorption and distribution and use these to optimise the pharmacokinetics of drug candidates;
- understand the origin of toxicity and recognise simple toxicophores in drug candidates.
Lead Generation:
- Selection of therapeutic areas for drug development; Measures of drug activity in vivo and in vitro.
- Interactions of drugs with biomolecules including H-bonding and Hydrophobic interactions.
- Pharmacophore Identification.
Structure Optimisation:
- Activity optimisation by: Conformational restriction, Bioisosteric replacement, exploring the binding site.
- Other factors to be optimised, Pharmacokinetics, The journey of a drug through the body, selectivity.
- Structure Activity Relationships.
Absorption and Distribution:
- Solubility, permeability, plasma protein binding.
- Lipinski's rule, Veber's rule.
- Recognising acidic and basic groups. pKa and extent of ionisation at variable pH.
Receptors as Targets:
- Cell signalling pathways and receptor mechanisms. Receptor Subtypes.
- Agonists Antagonists.
Quantification of structure activity relationships:
- The role of QSAR.
- QSAR analysis.
Case Studies:
- Drug development case studies.
| Delivery type | Number | Length hours | Student hours |
|---|---|---|---|
| On-line Learning | 10 | 1 | 10 |
| Example Class | 10 | 1 | 10 |
| Independent online learning hours | 15 | ||
| Private study hours | 65 | ||
| Total Contact hours | 20 | ||
| Total hours (100hr per 10 credits) | 100 | ||
80h (including 15h online study - quizzes, note-taking, additional reading)
Short online MCQs. Online workshops with in-class feedback
| Exam type | Exam duration | % of formal assessment |
|---|---|---|
| Open Book exam | 2.0 Hrs 0 Mins | 100 |
| Total percentage (Assessment Exams) | 100 | |
Normally resits will be assessed by the same methodology as the first attempt, unless otherwise stated
The reading list is available from the Library website
Last updated: 4/29/2024
Errors, omissions, failed links etc should be notified to the Catalogue Team