2018/19 Undergraduate Module Catalogue
CHEM2215 Introduction to Drug Design
10 creditsClass Size: 80
Module manager: Dr R Foster
Email: r.foster@leeds.ac.uk
Taught: Semester 2 (Jan to Jun) View Timetable
Year running 2018/19
Pre-requisite qualifications
Level 1 in Medicinal Chemistry or equivalentPre-requisites
CHEM1000 | Introduction to Modern Chemistry |
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 | 4 | 1.00 | 4.00 |
Lecture | 16 | 1.00 | 16.00 |
Private study hours | 80.00 | ||
Total Contact hours | 20.00 | ||
Total hours (100hr per 10 credits) | 100.00 |
Private study
40 hours - preparation for lectures20 hours - completion of workshop assignments
20 hours - preparation for examination.
Opportunities for Formative Feedback
- 4 workshops- Workshop assignments distributed in advance and handed in prior to review in workshop environment.
Methods of assessment
Coursework
Assessment type | Notes | % of formal assessment |
In-course Assessment | Workshop Assessment | 12.00 |
Total percentage (Assessment Coursework) | 12.00 |
Normally resits will be assessed by the same methodology as the first attempt, unless otherwise stated
Exams
Exam type | Exam duration | % of formal assessment |
Standard exam (closed essays, MCQs etc) | 2 hr 00 mins | 88.00 |
Total percentage (Assessment Exams) | 88.00 |
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: 18/02/2019
Browse Other Catalogues
- Undergraduate module catalogue
- Taught Postgraduate module catalogue
- Undergraduate programme catalogue
- Taught Postgraduate programme catalogue
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