CHEM 390 : Medicinal Chemistry
2020 Semester One (1203) (15 POINTS)
The concepts, principles and applications of medicinal chemistry will be examined and include: the drug discovery and development process, molecular recognition and structure-activity relationships in biological systems, drug-DNA interactions, enzymes as therapeutic targets, mechanisms of ligand-receptor interactions, combinatorial approaches to discovery of novel chemotherapeutic agents and drug metabolism and drug resistance.
Capabilities Developed in this Course
|Capability 1:||Disciplinary Knowledge and Practice|
|Capability 2:||Critical Thinking|
|Capability 3:||Solution Seeking|
|Capability 4:||Communication and Engagement|
|Capability 6:||Social and Environmental Responsibilities|
- Describe how antimicrobial peptides function understand the basic principles of peptide synthesis and be able to write the structure of a Peptide from constituent amino acids. (Capability 1, 2 and 3)
- Apply he principles of molecular recognition and intermolecular bonding interactions, to the development of enzyme inhibitors and receptor agonists and antagonists as drugs. (Capability 1, 2 and 3)
- Describe the mechanism of action and structure-activity-relationship of classic molecules like Penicillin, Morphine, Cisplatin, antigene and antisense oligonucleotides etc. (Capability 1, 2, 3, 4 and 6)
- Apply the "profit: need : threat" rationale for the drug discovery process using examples, describe How Lipinski’s 'rule of five' to determine 'drug-like molecules’ and Explain why halogens are often incorporated into pharmaceuticals, using examples. (Capability 1, 2 and 3)
- Apply he principles of combinatorial chemistry solid-phase organic synthesis (SPOS) in the drug discovery process to generating new drug leads. (Capability 1, 2 and 3)
- Apply the principles and ideas are behind QSAR studies, explain the concept of prodrugs, explain the importance of the molecular shape and flexibility (stereochemistry principles) and how the physicochemical properties of the drugs are important and can be incorporated in drug design. (Capability 1, 2, 3 and 4)
- Evaluate the influence of tissue pH, drug pKa and logP to the ability of the drug to cross membranes and enter cells as well as use the Henderson-Hasselbalch equation to determine the percentage of drug ionisation (known pKa) in tissue at a particular pH and understand the effect that pH has on solubility and hence therapeutic effectiveness (Capability 1, 2, 3 and 4)
- Describe the structural features of surfactants and liposomes that make them useful as drug delivery agents in order to overcome issues of drug solubility and metabolic stability and to improve drug targeting. (Capability 1, 2 and 3)
- Identify and explain metabolic reactions into phase I and II, relate these to the functional group or structure may undergo and predict the resultant metabolite; identify the types of enzymes and co-enzymes needed for the metabolic reaction and describe some examples where knowledge of the metabolic fate of a lead compound has been used to design a more effective drug. (Capability 1, 2 and 3)
- Describe he general mechanisms utilised by bacteria in drug resistance and give an example of an antibiotic that succumbs to each mechanism (Capability 1, 2, 3, 4 and 6)
|Final Exam||50%||Individual Examination|
|Assessment Type||Learning Outcome Addressed|
Electronic copy of lecture notes, lecture recordings, laboratory manual and lab report books and examples of previous test and exam papers with model answers
This course is a standard  point course and students are expected to spend 10 hours per week involved in each 15 point course that they are enrolled in.
For this course, you can expect  hours of lectures, a  hour tutorial,  hours of reading and thinking about the content and  hours of work on assignments and/or test preparation.
Course materials are made available in a learning and collaboration tool called Canvas which also includes reading lists and lecture recordings (where available).
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