2021/22 Undergraduate Module Catalogue
CHEM2215 Introduction to Drug Design
10 creditsClass Size: 80
Module manager: Dr Richard Foster
Email: r.foster@leeds.ac.uk
Taught: Semester 1 (Sep to Jan) View Timetable
Year running 2021/22
Pre-requisite qualifications
Level 1 in Medicinal Chemistry or equivalentPre-requisites
CHEM1101 | Chemistry 1: Bonding and Behaviour |
Module replaces
CHEM2115 Introduction to Drug DesignThis module is not approved as a discovery module
Objectives
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.
Syllabus
Lead Generation (3 lectures)
- 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. (9 lectures 2.5 workshops)
- 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.
Receptors as Targets (1 lectures 1 workshop)
- Cell signalling pathways and receptor mechanisms. Receptor Subtypes
- Agonists Antagonists
Quantification of structure activity relationships (2 lectures 0.5 workshop)
- The role of QSAR
- QSAR analysis
- Independence of parameters and the Craig plot
- Simplifying QSAR: the Topliss model.
Case Studies (1 lecture)
- Drug development case studies
Teaching methods
Delivery type | Number | Length hours | Student hours |
Workshop | 8 | 1.00 | 8.00 |
e-Lecture | 1 | 1.00 | 1.00 |
Private study hours | 91.00 | ||
Total Contact hours | 9.00 | ||
Total hours (100hr per 10 credits) | 100.00 |
Private study
51 hours - working though online material, making notes and background reading.20 hours - completion of workshop assignments
20 hours - preparation for examination.
Opportunities for Formative Feedback
Short online MCQs. Online workshops with in-class feedbackMethods of assessment
Exams
Exam type | Exam duration | % of formal assessment |
Open Book exam | 2 hr 00 mins | 100.00 |
Total percentage (Assessment Exams) | 100.00 |
Normally resits will be assessed by the same methodology as the first attempt, unless otherwise stated
Reading list
The reading list is available from the Library websiteLast updated: 02/07/2021 10:55:13
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