Medicinal Chemistry

Overview

Summary of Lecture Content:
The purpose of this module is to provide students with the knowledge of the inception of a biopharmaceutical product, its chemical composition and how it will act in the body. The module is split into three lecture series, Biomacromolecules, Pharmacology, and Drug Discovery. Each of the series is comprised of 5 lectures which will deal with topics in significant detail. As there will be some organic chemistry associated with the first lecture series relevant workshops will aid understanding and provide students with a space to discuss or raise queries with the academic. One of the marked assessments will be written reports by the students on journal articles aligned with each of the lecture series subjects, e.g. the first report will be on a journal article about drug discovery. Another assessed aspect is the literature review - each student will be given a topic and a period of time to perform a literature search. Following this, the student will compile their findings and provide a report which must include critical analysis and a short presentation detailing the major findings from the review.

Series 1: Proteins- Uses, Structure and Function
The content of this series will be mainly involved with macromolecules which are found naturally and also synthesised in vivo. The initial focus concerns the basic building blocks of proteins with an in-depth look at the type of bonding and interactions between amino acids, what the key features are and how they potentially react with each other. This series will be challenging for students from a non-chemistry background and as such will be supported by relevant workshops to reinforce learning and enhance understanding of theoretical organic chemistry. This block will include two seminars where questions will be uploaded and worked through during the classes.

Series 1 Lectures:
• Lecture 1: Amino acids - Structure and bonding
• Lecture 2: Amino Acid Sequence
• Lecture 3: Proteins-Structure
• Lecture 4: Proteins-Uses
• Lecture 5: Protein interactions

Series 2: Pharmacology Introduction
This series will introduce the theories behind pharmacology and their importance when thinking about designing a drug for administration. The emphasis in this block is the consideration of pharmacokinetics and pharmacodynamics of a drug’s effects on the human body. These topics will involve the interpretation and understanding of curves showing effect vs time and concentration vs time and students will also be expected to apply mathematical knowledge with regard to the determination of models which apply to drug administration and distribution. Also discussed is the use of prodrugs for the treatment of illness affecting the human body, why these are important and their mechanism of liberation. Workshops will facilitate and reinforce learning in these new topics including the application of specific mathematical models.
Series 2 Lectures:
• Lecture 6: Biopharmacology
• Lecture 7: Pharmacokinetics
• Lecture 8: Pharmacodynamics
• Lecture 9: Mechanisms of action
• Lecture 10: Receptors and systems

Series 3: Drug Discovery
This series will look at the processes behind the discovery of drugs, both in a traditional manner and also through the discovery of biopharmaceutical products. Students will gain knowledge and understanding of target ID and validation within a biological system, why this is necessary and the techniques involved in this process. Other aspects of the drug discovery regime are discussed in detail, including lead generation, optimisation and candidate selection. Throughout the discussion around these themes within drug discovery, there will be a detailed consideration of relevant ethical standards. This block will include a seminar where questions will be uploaded and worked through during class.

Series 3 Lectures:
• Lecture 11: Target ID & Validation
• Lecture 12: Lead Generation
• Lecture 13: Lead Optimisation
• Lecture 14: Candidate Selection
• Lecture 15: Ethics


Summary of Workshops:
• Workshop 1: Amino acids and their Chemistry
• Workshop 2: Bonding and Structure in Proteins
• Workshop 3: Pharmacokinetics and pharmacodynamics
• Workshop 4: Mechanisms and receptors
• Workshop 5: Drug discovery breakdown, processes and guidelines

Summary of Module Delivery:
The three lecture series described above will be delivered in a blended fashion, over a period of twelve weeks. All workshops will be held either in person or via Teams so discussion of points and questions can be facilitated, ideally this will be done with a PDRA or PhD student who can move between break-out rooms when group work is underway.

Learning Objectives

At the end of the module students will be able to:
• Create a structure from a given name of a biomacromolecule including the key bonding pattern and features
• Given appropriate structures, give rationale for reactivity
• Understand and explain the structures of a protein and the bonding both inter- and intramolecularly
• Understand and apply knowledge of the key principles of pharmacology
• Recall the principles of ADME
• Categorise and evaluate a drug in terms of Lipinski’s rule of 5
• Understand and extract data from graphs relating pharmacokinetics and pharmacodynamics
• Using rationale, provide mechanisms of action for a given pharmaceutical
• Understand and describe the processes in a system in terms of receptor and ligand etc.
• Understand the need for the processes in drug discovery
• Critically evaluate the drug discovery process
• Rationally describe the ethics of the drug discovery process

Skills

Skills associated with this module:
• Core skills in STEM
• Critical evaluation
• Analytical skills
• Communication and report writing skills
• Logical understanding
• Problem solving ability

Assessment

Course Requirements:
Coursework submission 100 %
Total Coursework elements must be passed at 50%

Assessment Profile
Element type Element weight (%)
1. Workshop Questions 40
2. Short essays on journals 60