MEDICINAL CHEMISTRY II - 2019/0
Module code: CHE3049
The module provides a well-rounded knowledge of medicinal chemistry. Through its employment of example drug discovery projects from the research areas of viruses, antibiotics, diabetes, adrenergic receptors, cancer, nanotherapeutics and inorganic medicinal chemistry, it provides students with an understanding of design and discovery strategies which should allow them to critically evaluate new medicinal chemistry projects as well as suggest new research directions and ideas for improvements.
WHELLIGAN Daniel (Chemistry)
Number of Credits: 15
ECTS Credits: 7.5
Framework: FHEQ Level 6
JACs code: F150
Module cap (Maximum number of students): N/A
Overall student workload
Independent Learning Hours: 120
Lecture Hours: 30
Indicative content includes:
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.
Adrenergic receptors: GPCRs, agonists, antagonists, partial agonists, GPCRs, affinity, efficacy, potency. Associated drugs, their mechanisms of action and discovery.
Viruses and antiviral drugs. Vaccines and antiviral drugs. DNA chain terminators. Enzymes: kinases, peptidases, reversible inhibitors.
Antibiotics, their discovery. Natural and semisynthetic β–lactams (penicillins and cephalosporins), their mechanism of action. Other antibiotics, the problem of drug resistance (MRSA etc).
Diabetes, mechanisms of action of insulin and drugs. Discovery of new therapeutics. Receptors: kinase-linked receptors, ligand gated ion-channel receptors, intracellular receptors, signal transduction.
Cancer and chemotherapy. Nucleic acids as drug targets: DNA intercalation, alkylation. The design of modern targeted therapeutics.
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.
Process chemistry, scale-up.
The pharmaceutical industry. Generic drugs. Ethical aspects. Clinical trials. Patents
|Assessment type||Unit of assessment||Weighting|
|Examination||EXAMINATION: 1.5 hours||70|
The assessment strategy is designed to provide students with the opportunity to demonstrate,
through coursework, the ability to:
- research, understand and critically evaluate drug discovery programmes reported in the literature, against a target not met in lectures, by applying knowledge gained in the module [LOs 2, 3, 4]
through written examination, all learning outcomes [LOs 1-5]
Thus, the summative assessment for this module consists of:
- coursework incorporating a review of medicinal chemistry programmes on a given target [LOs 3, 5] (25 h, deadline week 9, 30%)
- examination [LOs 1-5] (1.5 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 written review consists of annotations on the returned document and a breakdwon of marks into specific headings along with written general feedback giving justifications for the marks and suggestions for improvement.
- To give students an advanced understanding of how drugs work and are designed, discovered and developed.
- To provide students with a conceptual understanding of drug discovery, for several disease classes, through medicinal chemistry examples
|1||Analyse classes of medicinally important natural products (antibiotics, terpenes) in terms of their biosynthesis and mode of action|
|2||Conceptually rationalise the role of metal complexes in diagnostics and therapy and be able to solve problems related to their use|
|3||Understand the targeting of biological pathways with drugs to treat several major diseases|
|4||Review and critically evaluate material describing the mode of action, discovery and development of known drugs|
|5||Apply medicinal chemistry methods for the determination of structure-activity relationships and improvement of drug pharmacodynamics and pharmacokinetics|
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 drug discovery process, methods and characteristics of drugs by providing them with a fuller understanding of considerations during their design through the use of case studies in several specific areas.
Provide students with an ability to understand new drug discovery programmes, critically evaluate them and suggest future work or improvements.
The learning and teaching methods include:
Formal lectures which contain occasional group problem-solving tasks. (30 h)
Coursework: a written critical review of published medicinal chemistry programmes for a given biomolecular target, not discussed in lectures, followed by suggested future directions. (25 h)
Independent learning (reading (some directed) and revision).(92.5 h)
Revision tutorial (1 h)
Written exam (closed book, 1.5 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: CHE3049
Programmes this module appears in
|Chemistry BSc (Hons)||2||Optional||A weighted aggregate mark of 40% is required to pass the module|
|Chemistry with Forensic Investigation BSc (Hons)||2||Optional||A weighted aggregate mark of 40% is required to pass the module|
|Medicinal Chemistry BSc (Hons)||2||Compulsory||A weighted aggregate mark of 40% is required to pass the module|
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.