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2021/22 Taught Postgraduate Module Catalogue

CHEM5106M Drug Discovery and Development

15 creditsClass Size: 20

Module manager: Prof Bruce Turnbull
Email: w.b.turnbull@leeds.ac.uk

Taught: Semester 1 (Sep to Jan) View Timetable

Year running 2021/22

Pre-requisite qualifications

None

This module is mutually exclusive with

CHEM3146Medicinal Chemistry

Module replaces

CHEM5105 Drug Discovery and Development

This module is not approved as an Elective

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 high throughput screening hit validation, 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.

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) a comprehensive understanding of the cutting edge medicinal chemistry processes and technologies 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 and a critical awareness of the role of contemporary types of biochemical and biophysical assay in the drug discovery process
(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 and
(6) be able to evaluate and critically discuss cutting edge technologies employed in contemporary drug development research

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
Unit 7: Colorimetric and fluorescence-based assays
Unit 8: Measuring binding kinetics and thermodynamics
Unit 9: Introduction to structural biology in hit validation

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
Coursework Discussion Session11.001.00
Lecture31.003.00
Seminar101.0010.00
Independent online learning hours50.00
Private study hours86.00
Total Contact hours14.00
Total hours (100hr per 10 credits)150.00

Private study

15 hours – preparing the written report
31 hours – reading, independent study and preparation for workshops
20 hours - preparation for examination
20 hours – research and preparation of oral presentation

Methods of assessment

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


Coursework
Assessment typeNotes% of formal assessment
Oral Presentation10 min presentation delivered live or as recording30.00
ReportWritten Report - 2 pages of A410.00
Total percentage (Assessment Coursework)40.00

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 60.00
Total percentage (Assessment Exams)60.00

If necessary the exam will be replaced by an OTLA

Reading list

There is no reading list for this module

Last updated: 02/07/2021

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