Aims

To provide an overview of the methods and approaches used in modern drug discovery. To introduce the key stages of a project i.e. target identification and validation, hit discovery, hit validation, hit-to-lead optimisation and lead optimisation. To familiarise students with the most commonly used synthetic methods in medicinal chemistry. To provide students with an understanding of the role of medical imaging in drug discovery, synthetic methods for the incorporation of radioisotopes into biologically active molecules and the quality control requirements for clinical production.

Outline Of Syllabus

Methods in Drug Discovery
Dr IR Hardcastle

1 Overview of drug discovery - Peptide synthesis 1
2 Target identification and validation - Peptide synthesis 2
3 Hit identification technologies - Nucleophilic aromatic substitution (SNAr)
4 Hit identification technologies - Heterocycle formation
5 Hit-to-lead strategies and methods - Microwave synthesis
6 Seminar: Fragment-based drug discovery
7 Lead optimisation challenges - Multicomponent reactions
8 Lead optimisation - Reductive amination
9 In vitro and vivo DMPK - Mitsunobu reactions
10 Metabolism-directed design - Palladium coupling
11 Modern drug synthesis

Isotopes and Imaging in Drug Discovery
Dr MA Carroll

1 Introduction to radioactivity
2 Positron Emission Tomography - PET
3-4 Preparation of 11C labelled compounds
5 Preparation of 18F labelled compounds - electrophillic
6 Preparation of 18F labelled compounds - nucleophilic
7 Radiochemistry automation
8 Clinical production
9 Other PET radioisotopes - e.g. 68Ga, 64Cu, 89Zr
10-11 Key PET imaging agents

Teaching Rationale And Relationship

Key concepts and supporting examples are delivered by lectures.

Assessment Rationale And Relationship

The formal examination will test the student's acquisition and understanding of the lecture material.

Study Abroad students may request to take their exam before the semester 1 exam period, in which case the format of the paper may differ from that shown in the MOF. Study Abroad students should contact the school to discuss this.