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2019/20 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 View Timetable

Year running 2019/20

Pre-requisite qualifications

Level 1 in Medicinal Chemistry or equivalent

Pre-requisites

CHEM1000Introduction to Modern Chemistry

Module replaces

CHEM2115 Introduction to Drug Design

This 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 typeNumberLength hoursStudent hours
Workshop41.004.00
Lecture161.0016.00
Private study hours80.00
Total Contact hours20.00
Total hours (100hr per 10 credits)100.00

Private study

40 hours - preparation for lectures
20 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 typeNotes% of formal assessment
In-course AssessmentWorkshop Assessment12.00
Total percentage (Assessment Coursework)12.00

Normally resits will be assessed by the same methodology as the first attempt, unless otherwise stated


Exams
Exam typeExam duration% of formal assessment
Standard exam (closed essays, MCQs etc)2 hr 00 mins88.00
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 website

Last updated: 18/02/2019

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