MEDICINAL CHEMISTRY - 2023/4
Module code: CHE3062
The module provides well-rounded knowledge and understanding of the chemistry and molecular considerations and assays involved in drug discovery. Students who opted to study Bioorganic Chemistry and Drug Discovery at level 5 will find this module gives a deeper understanding of the medicinal chemistry aspect of drug discovery. Through its employment of example drug discovery projects from the research areas of viruses, antibiotics, diabetes, adrenergic receptors, cancer, including nuclear medicine, nanotherapeutics and inorganic medicinal chemistry, it provides students with an appreciation of design and discovery strategies which will allow them to critically evaluate unseen medicinal chemistry projects as well as suggest new research directions and ideas for improvements.
Chemistry and Chemical Engineering
WHELLIGAN Daniel (Chst Chm Eng)
Number of Credits: 15
ECTS Credits: 7.5
Framework: FHEQ Level 6
Module cap (Maximum number of students): N/A
Overall student workload
Independent Learning Hours: 85
Lecture Hours: 17
Tutorial Hours: 7
Guided Learning: 10
Captured Content: 31
Prerequisites / Co-requisites
Indicative module content:
Advanced binding interactions: ΔG, binding role of functional groups and amino acids, the hydrophobic effect.
Structure-Activity Relationships (SARs), medicinal chemistry strategy and synthesis
Viruses and antiviral drugs. Vaccines and antiviral drugs. DNA chain terminators. Enzymes: kinases, peptidases, reversible inhibitors.
Adrenergic receptors: GPCRs, agonists, antagonists, partial agonists, affinity, efficacy, potency. Associated drugs, their mechanisms of action 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).
Diabetes, mechanisms of action of insulin and drugs. Discovery of new therapeutics. Kinase-linked receptors, ligand gated ion-channel receptors, signal transduction.
Cancer and chemotherapy. Nucleic acids as drug targets. The design of modern targeted 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.
|Assessment type||Unit of assessment||Weighting|
|Examination Online||ONLINE OPEN BOOK EXAM (4 hours)||70|
The assessment strategy is designed to allow students 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 and employing online digital databases;
- through written examination, all learning outcomes
Thus, the summative assessment for this module consists of:
- coursework incorporating a review of a medicinal chemistry programme on a given target (~30 h, assesses learning outcomes 1-3)
- online examination (4 h, assesses learning outcomes 1-5)
Problem sets mimicking exam questions and taken from medicinal chemistry literature are provided in tutorials. After discussion in groups, students provide answers and feedback is given immediately by the lecturer. The ability to come up with solutions under mild pressure and work in groups will increase employability and resourcefulness. .
Feedback to the written review consists of annotations on the returned document and a breakdown of marks into specific headings along with written general feedback giving justifications for the marks and suggestions for improvement
- Give students an in-depth understanding of how small molecule, and polymer, therapeutics and diagnostics work and the processes and considerations involved in their design, discovery and development
- Provide students with a strong awareness of the biomacromolecular target classes and therapeutic design strategies involved in several diseases to provide them with a skill set applicable to other diseases and new drug discovery programmes
|001||Understand example and new rationales for the targeting of specific biological pathways with drugs to treat several major disease classes||KC|
|002||Review and critically evaluate material describing the mode of action, discovery and development of known drugs||CPT|
|003||Apply medicinal chemistry methods for the determination of structure-activity relationships and improvement of drug pharmacodynamics and pharmacokinetics and suggest synthetic routes||KCP|
|004||Understand and critically evaluate late-stage and modern drug development strategies including process chemistry and the design of nanotherapeutics||KC|
|005||Conceptually rationalise the role of metal complexes in diagnostics and therapy and be able to solve problems related to their use||KCP|
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:
- Provide in-depth knowledge of medicinal chemistry in the context of several diseases, each of which will highlight specific strategies, through lectures and pre-recorded material
- Furnish students with a specialism in the organic / medicinal side of chemistry by building on compulsory level 4 and 5 organic chemistry modules, and level 5 optional Bioorganic Chemistry and Drug Discovery, with those reactions most useful to medicinal chemists
- In tutorials, give students an opportunity to practice designing synthetic and medicinal chemistry strategies towards new molecular classes. In some tutorials, group work is facilitated for answering questions thus providing an opportunity to work on inclusivity.
- Train students in the ability to understand and critically evaluate medicinal chemistry programmes through highlighting parts of the literature in lectures and tutorials before setting coursework requiring review of such literature aided by database.
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: CHE3062
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 in-depth understanding of the drug discovery process, as well as the knowledge of typical synthetic reactions used in the field, will enhance employability in the pharmaceutical industry along with any industry involving organic synthesis. In the coursework, resourcefulness and digital capabilities are developed when seeking out and critically evaluating the literature on 1-2 medicinal chemistry programmes. 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.
Programmes this module appears in
|Chemistry with Forensic Investigation BSc (Hons)||2||Optional||A weighted aggregate mark of 40% is required to pass the module|
|Chemistry 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 2023/4 academic year.