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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 equivalent

Pre-requisites

CHEM1101Chemistry 1: Bonding and Behaviour

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

Due to COVID-19, teaching and assessment activities are being kept under review - see module enrolment pages for information

Delivery typeNumberLength hoursStudent hours
Workshop81.008.00
e-Lecture11.001.00
Private study hours91.00
Total Contact hours9.00
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 feedback

Methods of assessment

Due to COVID-19, teaching and assessment activities are being kept under review - see module enrolment pages for information


Exams
Exam typeExam duration% of formal assessment
Open Book exam2 hr 00 mins100.00
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 website

Last updated: 02/07/2021 10:55:13

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