ADVANCED MEDICINAL CHEMISTRY - 2019/0
Module code: CHEM032
The module brings undergraduates to a position of knowledge which would facilitate strong understanding and skills in a new role in drug discovery research. It covers knowledge and skills required for all aspects of the modern drug discovery process and also teaches developments in inorganic medicinal chemistry, antibiotics and polymer therapeutics.
WHELLIGAN Daniel (Chemistry)
Number of Credits: 15
ECTS Credits: 7.5
Framework: FHEQ Level 7
JACs code: F150
Module cap (Maximum number of students): N/A
Overall student workload
Workshop Hours: 3
Independent Learning Hours: 116
Lecture Hours: 30
Tutorial Hours: 1
Prerequisites / Co-requisites
Satisfactory completion of FHEQ Level 5 and 6 Chemistry
Indicative content includes:
Photodynamic therapy. Porphyrin and phthalocyanine complexes, their mode of action.
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.
Target validation: genetic engineering, RNAi.
X-ray crystallography (crystallisation, soaking, X-ray), structure based design.
Advanced binding interactions: DG, binding role of functional groups and amino acids, the hydrophobic effect.
Enzymes: methods of catalysis, inhibitors. Examples.
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. Examples.
Nucleic acids as drug targets: DNA intercalation, alkylation, chain terminators, nucleic acid therapeutics. Examples.
Structure-Activity Relationships (SARs), medicinal chemistry strategy and synthesis.
Pharmacokinetics and strategies for improvements: solubility, permeability, blood-brain barrier, pKa, log P, metabolism, toxic metabolites, excretion.
Polymer therapeutics: Polymer-protein and polymer-drug conjugates. Polymer backbones: linear and branched polymers. Conjugation strategies. Targeting strategies. Cancer therapy with polymers: the Enhanced Permeation and Retention effect (EPR).
Process chemistry, scale-up.
The pharmaceutical industry. Generic drugs. Ethical aspects. Clinical trials. Patents
|Assessment type||Unit of assessment||Weighting|
|Examination||EXAMINATION: 2 hours||70|
The assessment strategy is designed to provide students with the opportunity to demonstrate,
through coursework, the ability to:
research and understand a drug discovery target, propose and rationalise analogues of a given molecule which should show improved medicinal chemistry properties, and propose syntheses of those analogues with reference to the literature [LOs 2, 3, 4]
through written examination, all learning outcomes, including those not covered by the coursework [LOs 1, 2, 3, 4, 5]
Thus, the summative assessment for this module consists of:
· coursework incorporating oral and written presentation of a research proposal for a medicinal chemistry programme, and attendance at all students’ presentations [LOs 2, 3, 4] (20+3 h, 30%)
· examination [LOs 1, 2, 4, 5] (2 h, 70%)
Formative assessment and feedback
Small problem-solving tasks are included in some lectures. During the task, the lecturer moves amongst the groups commenting and guiding the students’ starting points and answering strategies. Common difficulties are highlighted to the whole class and the final solution is given on the board/visualiser.
Feedback to the presentation includes general comments explaining the given marks and what could be done to improve. Feedback to written coursework consists of annotations on the returned proposal and a general comment indicating why the given marks have been assigned and what could be done to improve.
- To give students an advanced understanding of how drugs work and are designed, discovered and developed.
- To provide students with the ability to critically evaluate published medicinal chemistry programmes and make suggestions for drug design
|1||Critically appreciate the role of metal complexes in diagnostics and therapy and solve problems related to choice of isotope and ligands||KC|
|2||Review, critically evaluate and present material from current topics in medicinal chemistry||KCPT|
|3||Apply medicinal chemistry knowledge to suggest original alterations to molecules to test structure-activity relationships, improve potency or alter pharmacokinetics||KC|
|4||Have a critical awareness of the natural function of major drug targets and the action of drugs upon them at the molecular level||KC|
|5||Understand, critically evaluate and suggest late-stage drug development steps including formulations and process chemistry||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:
- Build on students’ knowledge of the basic drug discovery process and characteristics of drugs by providing them with a fuller understanding of considerations during their design. This is bolstered by many examples and case studies of small molecule drugs, inorganic agents, antibiotics and polymer therapeutics.
- Provide students with medicinal chemistry tools which can be applied to new drug discovery programmes and permit critical evaluation of published programmes.
The learning and teaching methods include:
- Formal lectures which contain occasional group problem-solving tasks. (32 h)
- Coursework: a written critical summary of an aspect of medicinal chemistry not discussed in lectures as well as a short oral presentation on the topic to the class followed by questions. (20 h)
- All students attend all coursework presentations so gain brief insights into these additional aspects of medicinal chemistry. (3 h)
- Independent learning (reading (some directed) and revision). (92 h)
- Revision tutorial (1 h)
- Written exam (closed book, 2 h)
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: CHEM032
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 2019/0 academic year.