65001 Medicinal Chemistry
Warning: The information on this page is indicative. The subject outline for a
particular session, location and mode of offering is the authoritative source
of all information about the subject for that offering. Required texts, recommended texts and references in particular are likely to change. Students will be provided with a subject outline once they enrol in the subject.
Subject handbook information prior to 2025 is available in the Archives.
Credit points: 6 cp
Result type: Grade and marks
Requisite(s): 65202 Organic Chemistry 1
Description
In this subject the entire process of drug discovery is discussed, from lead compounds to clinical trials. The multidisciplinary nature of medicinal chemistry is emphasised through lectures that explore the chemical, pharmacological and biological concepts that underlie drug development. Students learn about the macromolecules that drive cell behavior and disease, and how these can be targeted for therapeutic effect. The chemistry behind drug synthesis and design, including computational molecular modelling is introduced, and how the body’s metabolic processes impact on therapeutic success. This subject therefore provides students with the knowledge essential to the practice of medicinal chemistry.
Subject learning objectives (SLOs)
Upon successful completion of this subject students should be able to:
| 1. | Understand how drugs interact with biological molecules and the body, and apply these principles to drug design |
|---|---|
| 2. | Implement computational molecular modelling in drug design |
| 3. | Understand the role of clinical trials and intellectual property in drug development |
| 4. | Demonstrate laboratory skills relevant to medicinal chemistry, including synthetic chemistry and measurement of drug activity in a biological assay |
| 5. | Retrieve and analyse the scientific literature in the context of medicinal chemistry |
| 6. | Maintain an accurate record of practical work in the form of a laboratory notebook |
| 7. | Produce a high quality science journal article to convey the hypothesis and results of a research project |
| 8. | Demonstrate high level written communication skills to convey information to specific audiences |
| 9. | Work as an effective and reliable team member, demonstrating the necessary organisation and planning skills, collaboration and project management |
Course intended learning outcomes (CILOs)
This subject also contributes specifically to the development of following course intended learning outcomes:
- Demonstrate theoretical and technical knowledge of organic, inorganic, analytical, and physical chemistry and be able to explain specialised knowledge in one or more sub-disciplines. (1.1)
- Evaluate scientific evidence and apply effective experimental design, analysis and critical thinking to test current chemistry knowledge. (2.1)
- Work autonomously or in teams to address workplace or community problems utilising best scientific practice, and to act safely and responsibly in chemistry laboratory and practical settings. (3.1)
- Design creative solutions to contemporary chemistry-related issues by incorporating innovative methods, reflective practices and self-directed learning. (4.1)
- Effectively communicate concepts and scientific discovery in chemistry using different formats to present information in professional or public settings. (5.1)
Contribution to the development of graduate attributes
Graduate Attribute 1 – Disciplinary knowledge – you will understand of the principle, practice and application of medicinal chemistry in drug design. This subject will develop your knowledge through lectures, tutorials and quizzes, while practical skill and knowledge will be developed through the laboratory research project.
Graduate Attribute 2 – Research, Inquiry and Critical Thinking – you will develop skills in experimental design and the scientific method of knowledge acquisition that includes problem solving and critical thinking. These attributes are developed through the laboratory research project. Students will learn how to design and carry out a medicinal chemistry research, and record and interpret scientific results.
Graduate Attribute 3 - Professional, Ethical and Social Responsibility– you will learn to acquire, develop, employ and integrate a range of skills within a professional context, autonomously and collaboratively. In the laboratory research project students will need to manage and organise their time, accurately record and report data, and work effectively in teams. At the conclusion of the laboratory research project, students will write a formal report using the formatting and style found in journal publications.
Graduate Attribute 4 - Reflection, Innovation, Creativity – you will be provided with several opportunities to engage in reflection and develop the ability to make effective judgments about your own work. Opportunities to reflect and act on feedback will be available throughout the semester. Feedback on the laboratory notebook will be used to refine the journal article reporting the findings of the laboratory research project, and feedback from the quizzes will allow students to monitor their progression through the subject.
Graduate Attribute 5 – Communication – you will develop your written communication skills, including tailoring your message to the audience, in this subject. You will prepare a report in the form of a journal article that will provide experience in written communication to a scientific audience.
Teaching and learning strategies
This subject will be delivered through online and on-campus lectures, tutorials, and practical laboratory sessions
Online lectures and resource material: 12 x 1 hour. Each week students will need to view online material in the form of recorded lectures or other online content (youtube videos etc). The material delivered here will be built upon during the on-campus activities.
Integrated lectures and workshops: 12 x 2 hours on-campus with recordings available on Canvas. In these sessions there will be a mixture of lectures covering key concepts and problem solving exercises. Students will be expected to engage with pre-lecture material in Canvas. Questions and lectures will consolidate concepts learnt in the online material. Students will receive on-going feedback during the classes in the form of discussion of the solutions to quiz and tutorial questions both as a full class and in small student-led groups.
Laboratory: 8 x 3 hour. Students will conduct a laboratory research project in groups that runs over 8 weeks. To successfully complete the research project students must familiarise themselves with the assigned pre-lab reading- this material will be used to design the first series of compounds. Consideration of ‘real-world’ issues such as price and commercial availability of regents is included in the project to give students an authentic experience of medicinal chemistry research. Throughout the project students will keep records in their laboratory notebooks that will be assessed at regular intervals during the lab sessions via written and verbal feedback. Students can incorporate this feedback into their final written report.
In the laboratory sessions students are required to work in groups. Team work is a vital skill for a medicinal chemist, as all drug discovery requires a team of researchers.
If you cannot attend a scheduled practical class, please contact your subject coordinator as soon as possible to discuss your situation.
Content (topics)
Specific topics to be presented throughout the semester will include:
- Drug targets- structure, function and targeting of receptors, enzymes and DNA.
- Pharmockinetics- drug adsorption, distribution, metabolism and excretion. Drug half life, oral bioavailability.
- Drug-receptor binding- bonding forces, binding modes.
- Drug design- structure-activity relationships, pharmacophores, design strategies, pro-drugs.
- Assays- assay types, high-throughput screening.
- Drug formulation- tablets, coatings, emulsions.
- Molecular modelling- ligand and structure based drug design.
- Toxicology- sources, screening for toxicity.
- Drug to market- patents, clinical trials.
Assessment
Assessment task 1: In-class quizzes
| Intent: | This assessment contributes to the development of Graduate Attribute: 1. Disciplinary knowledge |
|---|---|
| Objective(s): | This assessment task addresses subject learning objective(s): 1, 2 and 3 This assessment task contributes to the development of course intended learning outcome(s): 1.1 |
| Type: | Quiz/test |
| Groupwork: | Individual |
| Weight: | 45% |
| Criteria: | Students will be assessed based on the correctness of their responses. |
Assessment task 2: Laboratory Research Project
| Intent: | This assessment contributes to the development of Graduate Attributes: 1. Disciplinary knowledge 2. Research, Inquiry and Critical Thinking 3. Professional, Ethical and Social Responsibility 4. Reflection, Innovation and Creativity |
|---|---|
| Objective(s): | This assessment task addresses subject learning objective(s): 1, 2, 4, 5, 6 and 9 This assessment task contributes to the development of course intended learning outcome(s): 1.1, 2.1, 3.1 and 4.1 |
| Type: | Laboratory/practical |
| Groupwork: | Group, group and individually assessed |
| Weight: | 25% |
| Criteria: | The laboratory notebook will be assessed based on the validity of the SAR set, quality of the experimental results, and the correctness of answers to the questions. |
Assessment task 3: Laboratory Research Project-Journal Article
| Intent: | This assessment contributes to the development of Graduate Attributes: 1. Disciplinary knowledge 2. Research, Inquiry and Critical Thinking 4. Reflection, Innovation, Creativity 5. Communication |
|---|---|
| Objective(s): | This assessment task addresses subject learning objective(s): 1, 2, 4, 5, 7 and 8 This assessment task contributes to the development of course intended learning outcome(s): 1.1, 2.1, 4.1 and 5.1 |
| Type: | Laboratory/practical |
| Groupwork: | Individual |
| Weight: | 30% |
| Criteria: | The journal article will be assessed based on the content and flow of ideas, quality of the writing, formatting, presentation and appropriate use of literature references. A rubric will be provided on Canvas. |
Minimum requirements
Practical classes in subjects offered by the School of Mathematical and Physical Sciences are an important and integral part of each subject in which they run. In addition to assisting students’ understanding of concepts, practical classes develop laboratory skills and experience, including safety skills, that are essential graduate attributes desired by employers. Thus, students are strongly encouraged to attend all scheduled practical sessions.
If you cannot attend a scheduled practical class, please contact your subject coordinator as soon as possible to discuss your situation.
You must obtain an overall mark of 50 or greater to pass the subject.
Required texts
Graham L. Patrick, An Introduction to Medicinal Chemistry, 5th edition, Oxford University Press 2013
Recommended texts
Benjamin E. Blass, Basic Principles of Drug Discovery and Development, Elsevier 2015
Camille Georges Wermuth, The Practice of Medicinal Chemistry, 4th edition, Elsevier 2015