ADVANCED MEDICINAL CHEMISTRY - 2024/5
Module code: CHEM037
The module brings students to a position of knowledge, understanding and skills which would facilitate a new role in drug discovery research. It covers the most important aspects of modern medicinal chemistry in detail and also teaches developments in radioisotope medicinal chemistry, antibiotics and nanotherapeutics.
Chemistry and Chemical Engineering
WHELLIGAN Daniel (Chst Chm Eng)
Number of Credits: 15
ECTS Credits: 7.5
Framework: FHEQ Level 7
Module cap (Maximum number of students): N/A
Overall student workload
Independent Learning Hours: 86
Lecture Hours: 15
Seminar Hours: 2
Tutorial Hours: 7
Guided Learning: 12
Captured Content: 28
Prerequisites / Co-requisites
Indicative content includes:
- Target validation using genetic engineering molecular biology tools.
- An introduction to X-ray crystallography and structure based design.
- Advanced binding interactions: ΔG, binding role of functional groups and amino acids, the hydrophobic effect.
- Structure-Activity Relationships (SARs), medicinal chemistry strategy and synthesis.
- Enzymes: methods of catalysis, inhibitor design and discovery.
- Antibiotics, their discovery. Natural and semisynthetic β–lactams (penicillins and cephalosporins), their mechanism of action. Other antibiotics, the problem of drug resistance (MRSA etc).
- Receptors: agonists, antagonists, partial agonists, GPCRs, kinase-linked receptors, ligand gated ion-channels, signal transduction, affinity, efficacy, potency.
- Pharmacokinetics and strategies for improvements: solubility, permeability, blood-brain barrier, pKa, log P, metabolism, toxic metabolites, excretion.
- Nucleic acids as drug targets: DNA intercalation, alkylation, chain terminators, nucleic acid therapeutics.
- Metal ions and chelating agents in therapy. Ligand design, choice of metal ion and targeting strategies.
- Radioisotopes for biological imaging and therapy. Ligand design and targeting strategies.
- Radioisotope production, radioloabelling and radioimmunoassay
- Process chemistry, scale-up.
- The pharmaceutical industry. Generic drugs. Ethical aspects. Clinical trials. Patents
|Assessment type||Unit of assessment||Weighting|
|Oral exam or presentation||PRESENTATION||10|
|Examination Online||ONLINE OPEN BOOK EXAM (4 hours)||70|
The assessment strategy is designed to allow students to demonstrate:
- through coursework, the ability to use electronic databases (pillar: digital capabilities) and peer-reviewed literature to research and understand a specified target protein, evaluate an imaginary hit molecule (with reference to published target ligands) in terms of possible binding interactions, and propose analogues with improved efficacy along with routes to their synthesis with reference to the literature. It utilises skills gleaned from lectures and tutorial problem-solving as described above.
- through written examination, all learning outcomes
Thus, the summative assessment for this module consists of:
- coursework incorporating a written research proposal and oral presentation to the class including the answering of questions from the audience (~30 h, assesses learning outcomes 1-4)
- online examination (4 h, assesses learning outcomes 1-5)
Problem sets mimicking exam questions and taken from medicinal chemistry literature are provided in tutorials and in some lectures. While working towards the summative coursework, students are encouraged to discuss with the lecturer queries about their proposal and literature they have read and receive verbal feedback before completing the presentation and review.
The research proposal oral presentation takes place approximately one week before the deadline for the written proposal to allow the students to act on (and therefore better internalise) immediate feedback. During the presentation, some feedback is given immediately in the form of questions and suggestions for improvement of the proposed research. Formal written feedback is given 1-2 days later including marks, why they were awarded and what could be done to improve in time to edit the written proposal. Feedback to the written research proposal consists of annotations on the returned document and general comments on the mark sheet indicating why the given marks have been assigned and what could be done to improve
- Give students an advanced understanding of how drugs work and are designed, discovered and developed
- Provide students with the ability to critically evaluate published medicinal chemistry programmes and make suggestions for novel drug design
- Enhance students' abilities to propose molecules likely to have improved properties in the context of medicinal chemistry and design syntheses of such those molecules and analogues
|001||Review, critically evaluate and present background material from current topics in medicinal chemistry||KCT|
|002||Apply medicinal chemistry knowledge to suggest analogues of molecules, and their synthesis, to test structure-activity relationships, improve potency or alter pharmacokinetics||KCP|
|003||Have a critical awareness of the natural function of major drug targets and the action of drugs upon them at the molecular level||KC|
|004||Understand, critically evaluate and suggest late-stage and modern drug development strategies including process chemistry and the design of nanotherapeutics||KC|
|005||Critically appreciate the role of metal complexes in diagnostics and therapy and solve problems related to choice of isotope and ligands||KC|
C - Cognitive/analytical
K - Subject knowledge
T - Transferable skills
P - Professional/Practical skills
Methods of Teaching / Learning
The learning and teaching strategy is designed to:
- Through lectures and pre-recorded material, provide a graduate-level understanding of medicinal chemistry and the pharmacodynamic and pharmacokinetic facets involved, augmented through the use of examples and case studies
- Build on compulsory level 4 and 5 organic chemistry modules, and level 5 optional module Bioorganic Chemistry and Drug Discovery by reviewing in lectures those reactions most relevant to medicinal chemistry and, in tutorials, designing synthetic routes to desired molecular analogues for drug discovery
- Invest in students the ability to critically evaluate medicinal chemistry programmes from the literature by answering questions, sometimes in groups, on such programmes in tutorials.
- In tutorials and short in-lecture questions, encourage students to design molecular entities with improved medicinal properties compared to previous iterations and thus feed into the coursework
Indicated Lecture Hours (which may also include seminars, tutorials, workshops and other contact time) are approximate and may include in-class tests where one or more of these are an assessment on the module. In-class tests are scheduled/organised separately to taught content and will be published on to student personal timetables, where they apply to taken modules, as soon as they are finalised by central administration. This will usually be after the initial publication of the teaching timetable for the relevant semester.
Upon accessing the reading list, please search for the module using the module code: CHEM037
The School of Chemistry and Chemical Engineering is committed to developing graduates with strengths in Employability, Digital Capabilities, Global and Cultural Capabilities, Sustainability, and Resourcefulness and Resilience. This module is designed to allow students to develop knowledge, skills, and capabilities in the following areas:
An ability to design novel drug test compounds and propose routes to their synthesis will increase employability in the pharmaceutical industry as well as any industry involving organic synthesis. In the coursework, resourcefulness is developed when proposing novel test compounds and extensive reference to the literature to back up the proposals will rely on digital capabilities. Oral presentation of the proposal gives an opportunity to develop confidence and therefore improve resilience, particularly when answering questions. The cost of drug discovery and consideration of animal trials raise ethical issues and help develop students’ global and cultural capabilities. An understanding of considerations during process chemistry will generate a deeper awareness of sustainability.
Although it is not a pre-requisite, this module is a specialization of the drug discovery side of L5 CHE2037 Bioorganic Chemistry and Drug Discovery.
Please note that the information detailed within this record is accurate at the time of publishing and may be subject to change. This record contains information for the most up to date version of the programme / module for the 2024/5 academic year.