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2021/22 Undergraduate Module Catalogue

CHEM3146 Medicinal Chemistry

10 creditsClass Size: 50

Module manager: Dr Martin McPhillie
Email: m.j.mcphillie@leeds.ac.uk

Taught: Semester 1 (Sep to Jan) View Timetable

Year running 2021/22

Pre-requisite qualifications

Level 2 in Chemistry or Medicinal Chemistry or Level 2 in Joint Honours (Science) with Chemistry or equivalent or Level 2 in MNatSci, BSc Natural Sciences.
For MSc candidates, undergraduate BSc level degree in Chemistry, Biochemistry or related subject.

Co-requisites

CHEM3126Strategy, Methods and Reaction Technology for Organic Synthe

Module replaces

CHEM3145 The Medicinal Chemistry of Drug Development

This module is not approved as a discovery module

Module summary

The module will serve as an introduction to medicinal chemistry and enable students to understand key aspects of drug discovery and development. We will cover the traditional medicinal chemistry processes of lead optimisation through to the filing of a marketable drug. We will use case studies in the area of anti-infective drug discovery to highlight the holistic nature of medicinal chemistry. The module is assessed via an exam (85%) and one piece of coursework (15%). Students will work independently to research and understand an aspect of anti-infective drug discovery, and to communicate their finding effectively via a written report.

Objectives

The objective of this module is to provide students with exposure to the key aspects of the drug development process, using examples from the pharmaceutical industry.
These key aspects include:
(a) an understanding of the medicinal chemistry processes required to optimise a drug candidate
(b) how a drug candidate progresses through late-lead optimisation to clinical trials
(c) a knowledge of anti-infective drug discovery with case studies from the pharmaceutical industry and academia.

Learning outcomes
On completion of this module, students should:
(1) be familiar with the drug discovery and development process, including preclinical development and clinical trials.
(2) be able to understand the pharmacokinetic and metabolic aspects of drug development and apply knowledge to unseen examples.
(3) be able to explain the process of multi-parameter lead optimisation and apply to unseen examples.
(4) be familiar with the field of anti-infective drug discovery.
(5) be able to work independently to research, understand and communicate aspects of anti-infective drug discovery.

Skills outcomes
Researching primary literature relating to medicinal chemistry


Syllabus

Unit 1: Traditional medicinal chemistry (Design-Make-Test cycles, classic reactions)
Unit 2: Metabolism (Phase I and II processes, AO metabolism, blocking strategies)
Unit 3: Multiparameter lead optimisation (‘traffic-light’ systems, selection criteria, balancing physicochemical properties)
Unit 4: Translation from late-lead to marketable drug (preclinical development, Phase I, II and III clinical trials, new drug approval)
Unit 5: An introduction to antiviral drug discovery
Unit 6: An introduction to antibiotic drug discovery

Teaching methods

Delivery typeNumberLength hoursStudent hours
Coursework Discussion Session11.001.00
Lecture31.003.00
Seminar51.005.00
Independent online learning hours25.00
Private study hours66.00
Total Contact hours9.00
Total hours (100hr per 10 credits)100.00

Private study

15 hours – preparing the report
31 hours – reading, independent study and preparation for workshops
20 hours - preparation for examination

Opportunities for Formative Feedback

1 x sessions to outline and advise on written work
5 x workshops throughout the module
2 x Minerva MCQs

Methods of assessment


Coursework
Assessment typeNotes% of formal assessment
ReportWritten Report, 2 pages of A415.00
Total percentage (Assessment Coursework)15.00

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


Exams
Exam typeExam duration% of formal assessment
Open Book exam2 hr 85.00
Total percentage (Assessment Exams)85.00

Will be replaced by an OTLA if necessary.

Reading list

There is no reading list for this module

Last updated: 10/08/2021

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