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MChem Chemistry with Medicinal Chemistry / Course details

Year of entry: 2021

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Course unit details:
Advanced Drug Discovery

Unit code CHEM30441
Credit rating 10
Unit level Level 3
Teaching period(s) Semester 1
Offered by Department of Chemistry
Available as a free choice unit? No

Overview

This course unit detail provides the framework for delivery in 21/22 and may be subject to change due to any additional Covid-19 impact. 

Lectures from staff from the Department of Division of Pharmacy & Optometry, The Paterson Institute for Cancer Research and Signature Discovery Ltd. will discuss new strategies for drug discovery, the clinical and preclinical evaluation of drug candidates and the chemical tools most commonly used to build drug candidates.

The following topics will be discussed in this unit:

1. Review the failings of traditional medicinal chemistry and the new concepts behind contemporary drug discovery

2. To study the top reactions used by medicinal chemists.

3. Look behind the scene of the Phase I, II and II trials of drug candidates, new directions in preclinical development and              understand issues related to drug-drug interactions.

 

Pre/co-requisites

Unit title Unit code Requirement type Description
Fundamentals of Biochemistry BIOL10551 Pre-Requisite Compulsory
Properties of Medicines PHAR10102 Pre-Requisite Compulsory
Fundamentals of Drug Discovery CHEM20421 Pre-Requisite Compulsory
The Big Killers PHAR20302 Pre-Requisite Compulsory

Aims

This unit aims to provide insights into how new medicinal lead compounds are identified, provide an understanding of the synthetic strategies that are deployed in their synthesis and discuss how these molecules are evaluated in order to arrive at new medicinal agents.

 

Learning outcomes

On successful completion of the course students should be able to:

1. Be able to understand and explain how medicinal chemistry has in the past approached drug           discovery and articulate the limitations of these approaches.

2. Describe and rationalize new approaches including HT, Fragment-Based Drug Discovery and virtual screening, and discuss and critically analyse HTS data outcomes.

3. Explain, calculate and apply drug physical characteristics such as ligand efficiency (LE) and lipid ligand efficiency (LipE). Define Lipinski’s rule and be able to apply to drug candidates.

4. Identify and explain examples of drug synthesis using reaction types that have been presented in lecture material or made available as on-line material, including providing mechanistic explanations for the outcome of synthetic schemes.

5. Suggest reaction processes, reagents and mechanisms, for specific drug synthetic steps provided.

6. Discuss specific drug development case histories articulating candidate selection criteria.

7. Describe and discuss importance of bioavailability, provide an account of processes for drug formulation, including aspects relevant to manufacture (tableting, particle size etc), as well as drug delivery.

8. Provide explanations of the key features of clinical trials, being able to explain important characteristics of trials.

9. Discuss the importance of drug-drug interactions and be able to explain case history examples.

Transferable skills and personal qualities

  • Problem-solving skills
  • Communications skills
  • Numeracy and mathematical skills
  • Analytical skills
  • ICT skills
  • Time management and organisational skills
  • Interpersonal Skills
  • Ethical behaviour
  • Entrepreneurial Skills

 

Assessment methods

Method Weight
Written exam 100%

Feedback methods

Students will be given problem sheets and example exam questions; outline solutions will be uploaded to BlackBoard.  Staff will be available to answer queries during the course, especially during the workshop sessions.

 

Recommended reading

Lecture material, case studies and required reading will be available on the CHEM30441 website.

General Reading:

“An Introduction to Mecinial Chemistry, 5th Edn.” by G. L. Patrick.  Oxford University Press, 2013.  ISBN 978-0-19-969739-7.  Main library, 3rd floor, blue area: 615.19 PAT

“An Intoduction to Drug Synthesis”, by G. L. Patrick.  Oxford University Press, 2015.  ISBN 978-0-19-870843-8.  Main Library, 3rd floor, blue area: 615.19 PAT

 

Study hours

Scheduled activity hours
Assessment written exam 2
Lectures 24
Independent study hours
Independent study 74

Teaching staff

Staff member Role
Peter Quayle Unit coordinator

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