2024/25 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 2024/25

Pre-requisite qualifications

Level 1 in Medicinal Chemistry or equivalent

Pre-requisites

CHEM1101

Chemistry 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; 
- 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.

Syllabus

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.

Teaching methods

Delivery type	Number	Length hours	Student hours
On-line Learning	10	1.00	10.00
Example Class	10	1.00	10.00
Independent online learning hours			15.00
Private study hours			65.00
Total Contact hours			20.00
Total hours (100hr per 10 credits)			100.00

Private study

80h (including 15h online study - quizzes, note-taking, additional reading)

Opportunities for Formative Feedback

Short online MCQs. Online workshops with in-class feedback

Methods 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 website

Last updated: 29/04/2024 16:12:08

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