Undergraduate Course: Advanced Medicinal Chemistry (CHEM10072)
|School||School of Chemistry
||College||College of Science and Engineering
|Credit level (Normal year taken)||SCQF Level 10 (Year 4 Undergraduate)
||Availability||Not available to visiting students
|Summary||A course of lectures on how medicines are designed and developed, with emphasis on the key properties required for developing a successful medicine. This course will discuss how physicochemical properties affect drug design and activity, the use of computational and structure-based drug design, common reactions that are widely used in medicinal chemistry, the different types of drug targets that are currently ¿druggable¿, emerging new drug classes that can expand the types of disease targets we can modulate, consideration of the pharmacokinetic properties of a drug and how a drug can be translated from the lab to clinic.
The course comprises six individual five-lecture courses that describe common and emerging approaches in drug discovery and design. The course will afford an appreciation of the importance of mode of action, structure-activity relationships, pharmacokinetics and physicochemical properties in successful drug design; as well as the methods that are key to their optimisation.
Physicochemical Properties in Drug Design - the role of physical organic chemistry in understanding the relationships between the physicochemical and biological properties of pharmaceutical agents. A discussion of the role of structure-activity relationships in modern-day drug design and development.
Computational Drug Design - the driving forces of protein-ligand association and current strategies to optimise the potency or selectivity of a small molecule ligand. An introduction to the main computational methods currently used to support rational approaches to drug design in academia and industry.
Synthetic Methods in Medicinal Chemistry - the common synthetic organic methods that are widely used in the synthesis of drug-like compounds e.g. Suzuki coupling, amide bond formation, fluorination, C-H activation. An explanation of the key features of these reactions, including reagents, curly arrow mechanisms and selectivities.
Therapeutic Targets and Classes - how different types of drug molecule can modulate specific classes of biological molecule such as nucleic acids, transcription factors, enzymes, membranes and cell-surface receptors. A discussion of these target classes illustrated with specific examples from MHRA and FDA approved drugs and drugs in clinical trials.
Emerging Modalities in Medicinal Chemistry - alternative approaches to drug design including ¿non-traditional¿ small molecules such as PROTACs and peptides, biologics including antibody-drug conjugates, and theranostic agents. An overview of some of the most promising emerging modalities in medicine under investigation by the pharmaceutical industry.
Translational Aspects of Drug Design and Development - target identification, key drug target classes and their mechanisms of action, understanding of pharmacokinetic (ADME) properties of drug molecules and how these may differ between drug classes and biological targets; as well as the safety/toxicity profiles of candidate molecules. Translation of drugs from the lab to clinic.
Entry Requirements (not applicable to Visiting Students)
||Other requirements|| None
Course Delivery Information
|Academic year 2022/23, Not available to visiting students (SS1)
|Learning and Teaching activities (Further Info)
Lecture Hours 30,
Seminar/Tutorial Hours 9,
Summative Assessment Hours 3,
Revision Session Hours 6,
Programme Level Learning and Teaching Hours 4,
Directed Learning and Independent Learning Hours
|Assessment (Further Info)
|Additional Information (Assessment)
||Written Exam 100 %
||Each lecture module has an associated small-group tutorial. This will provide students with practice at problem-solving and tackling exam-like questions. It is also an opportunity for students to discuss any issues pertaining to the lecture course. Additional pre-exam revision sessions and/or individual meetings will be offered by the lecturers.
||Hours & Minutes
|Main Exam Diet S2 (April/May)||Advanced Medicinal Chemistry||3:00|
On completion of this course, the student will be able to:
- Show an understanding of the principal theories and concepts behind the application of chemistry to medicine, including the discovery of new therapeutic targets, the development of drugs, prodrugs and drug-like lead compounds, and common routes to drug delivery and administration.
- Apply this chemical knowledge to: explain the properties of, propose synthetic routes to, explain the mode of action of, and propose new targets for, a range of drugs and drug-like lead compounds.
- Critically review current practices in the application of chemistry to medicine and demonstrate an ability to analyse or assess complex problems based on diverse, or limited, datasets.
- Interpret and use a wide range of numerical, graphical and schematic (including chemical structures and curly arrows) data and communicate this effectively.
- Show an appreciation of complex ethical and professional issues relating to the application of chemistry to medicine in accordance with current professional and/or ethical codes or practices.
|Any good medicinal chemistry textbook; e.g. Medicinal Chemistry 6th Ed (Patrick), An Introduction to Drug Synthesis (Patrick), The Organic Chemistry of Drug Design and Drug Action 3rd Ed (Silverman), Drug Design and Development (Rostron)|
Computational methods covered by "Drug Design - Structure and Ligand Based Approaches" Kenneth M Merz Jr, Dagmar Ringe, Charles H. Reynolds, Cambridge University Press 2010
Reading lists pertaining to each course unit will be given by the lecturers.
|Graduate Attributes and Skills
||1. Note-taking skills.
2. Numerical data interpretation and analysis.
3. Unseen problem solving skills.
|Keywords||medicinal chemistry,chemical biology,pharmacology,computational drug design,drug discovery
|Course organiser||Prof Alison Hulme
Tel: (0131 6)50 4711
|Course secretary||Mr Craig Smith
Tel: (0131 6)50 4710