CHEM 390 : Medicinal Chemistry

Science

2024 Semester One (1243) (15 POINTS)

Course Prescription

Nature of cellular targets for drug action – lipids, proteins, enzymes, DNA. Principles of molecular recognition. Enzymes and receptors as targets for drug action. DNA as a target for drug action. An overview of approaches to drug discovery and development. Structure-activity relationships, stereochemistry and drug action, prodrugs, drug solubilisation and delivery, drug metabolism and antibiotic resistance. Laboratories focus on the synthesis, computer modelling and biological testing of drugs.

Course Overview

Want to be at the forefront of designing and discovering new compounds that are suitable for use as new drugs? Want to learn about how a substance operates in the body and its suitability for use as a drug? Medicinal chemistry is for you. It is one of the most rapidly developing areas within the disciplines of pharmaceutical science and chemistry and connects synthetic chemistry, pharmaceuticals, and healthcare. As a medicinal chemistry student, you will learn the art of drug discovery and development which will lead to employment in a wide range of institutions such as biomedical and pharmaceutical companies, private research institutions, and Crown Research Institutes.

Course Requirements

Prerequisite: CHEM 110 and a minimum of 165 points passed

Capabilities Developed in this Course

Capability 1: People and Place
Capability 3: Knowledge and Practice
Capability 4: Critical Thinking
Capability 5: Solution Seeking
Capability 7: Collaboration
Capability 8: Ethics and Professionalism
Graduate Profile: Bachelor of Science

Learning Outcomes

By the end of this course, students will be able to:
  1. Apply the principles of molecular recognition and intermolecular bonding interactions, to the development of enzyme inhibitors and receptor agonists and antagonists as drugs. (Capability 3, 4 and 5)
  2. Describe the mechanism of action and structure-activity-relationship of classic molecules like Penicillin, Morphine, Cisplatin (Capability 3, 4 and 5)
  3. Understand and explain the various steps of the drug development process from initial discovery, synthetic modification of candidates all the way to product marketing. (Capability 1, 3, 4, 5, 7 and 8)
  4. Explain the importance of the atomic/molecular structure, shape and flexibility and the various strategies medicinal chemists use to maximise drug interactions and control the physicochemical properties of drugs. (Capability 3, 4 and 5)
  5. Interpret qualitative and quantitative experimental data (and be able to make predictions about experimental outcomes) to draw conclusions about the efficacy and mode of action of drug leads, including ligand binding behaviour and enzyme kinetics. (Capability 3, 4 and 5)
  6. Understand and describe the differences between biologics and small molecule medicines with regards to their chemical makeup, regulation, development, production, and formulation. (Capability 3, 4 and 5)
  7. 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 3, 4 and 5)
  8. Describe the general mechanisms utilised by bacteria in drug resistance and give an example of an antibiotic that succumbs to each mechanism (Capability 3, 4 and 5)

Assessments

Assessment Type Percentage Classification
Laboratories 30% Individual Coursework
Test 1 15% Individual Test
Test 2 15% Individual Test
Quizzes 10% Individual Coursework
Final Exam 30% Individual Examination
Assessment Type Learning Outcome Addressed
1 2 3 4 5 6 7 8
Laboratories
Test 1
Test 2
Quizzes
Final Exam

A student must pass both the theory component and the practical component to gain an overall pass (gain at least 50% in the laboratory component to pass the course). The theory component is composed of quizzes, term tests, and final exams. The practical component is composed of laboratory experiments.

Tuākana

Tuākana Science is a multi-faceted programme for Māori and Pacific students providing topic specific tutorials, one-on-one sessions, test and exam preparation and more. Explore your options at
https://www.auckland.ac.nz/en/science/study-with-us/pacific-in-our-faculty.html
https://www.auckland.ac.nz/en/science/study-with-us/maori-in-our-faculty.html

As part of the University-wide Tuākana community, The School of chemical sciences aims to provide a welcoming learning environment for and enhance the success of, all of our Māori and Pacific students. We are led by the principles of tautoko (support) and whanaungatanga (connection) and hope you find a home here at the School. Students who have identified as Māori and/or Pacific will receive an invitation to our online portal introducing the Programme, the resources we have available, and how you can get involved.

Tuākana Chemistry runs a range of activities for students enrolled in this class. This includes weekly workshops, social activities, and opportunities to engage with senior students and researchers within the School of Chemical Sciences. Tuākana-eligible students will be added automatically to the Tuākana Chemistry program when they enroll in this course. For more information, please see the Tuākana program website or email scstuakana@auckland.ac.nz.

Key Topics

(8 lectures): Cellular targets for drug action: Introduction, Lipids as the target for drug action, Protein structure, Principles of molecular recognition, Enzymes as targets for drug action, Receptors as targets for drug action. DNA structure and function and DNA as a target for drug action.
(8 lectures): An overview of approaches to drug discovery and development (including computational and combinatorial approaches).
(8 lectures): Biologics, antibodies as medicines, experimental methods, mode-of-action studies, basic models of ligand binding and enzyme kinetics, interpretation of qualitative and quantitative data.
(8 lectures): Drug absorption and metabolism, and antimicrobial drug mechanism of action and mechanisms of antimicrobial resistance.

Special Requirements

Attendance at the laboratories is a compulsory part of this course. Students must be wearing safety glasses, covered footwear, and a lab coat before entering the laboratory and must keep these on until after exiting the laboratory. Jandals or other open shoes are not satisfactory footwear. Students who wear prescription spectacles are required to wear safety glasses over their spectacles. Students must comply with all health and safety regulations whilst working in the laboratories.

Workload Expectations

This course is a standard 15-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 36 hours of lectures, 18 hours of laboratory work (6 x 3 hours), 55 hours of reading and thinking about the content, and 41 hours of work on assignments/lab report writing and/or test preparation.

Delivery Mode

Campus Experience

Attendance is required at scheduled activities including labs/tutorials to receive credit for components of the course.
Lectures will be available as recordings. Other learning activities will not be available as recordings.
The course will not include live online events.
Attendance on campus is required for the test and exam.
The activities for the course are scheduled as a standard weekly timetable.

Learning Resources

Course materials are made available in a learning and collaboration tool called Canvas which also includes reading lists and lecture recordings (where available).

Please remember that the recording of any class on a personal device requires the permission of the instructor.

Electronic copy of lecture notes, lecture recordings, laboratory manual and lab report books, and examples of previous test and exam papers with model answers.

Student Feedback

During the course Class Representatives in each class can take feedback to the staff responsible for the course and staff-student consultative committees.

At the end of the course students will be invited to give feedback on the course and teaching through a tool called SET or Qualtrics. The lecturers and course co-ordinators will consider all feedback.

Your feedback helps to improve the course and its delivery for all students.

No changes requried

Other Information

 

Academic Integrity

The University of Auckland will not tolerate cheating, or assisting others to cheat, and views cheating in coursework as a serious academic offence. The work that a student submits for grading must be the student's own work, reflecting their learning. Where work from other sources is used, it must be properly acknowledged and referenced. This requirement also applies to sources on the internet. A student's assessed work may be reviewed for potential plagiarism or other forms of academic misconduct, using computerised detection mechanisms.

Class Representatives

Class representatives are students tasked with representing student issues to departments, faculties, and the wider university. If you have a complaint about this course, please contact your class rep who will know how to raise it in the right channels. See your departmental noticeboard for contact details for your class reps.

Copyright

The content and delivery of content in this course are protected by copyright. Material belonging to others may have been used in this course and copied by and solely for the educational purposes of the University under license.

You may copy the course content for the purposes of private study or research, but you may not upload onto any third party site, make a further copy or sell, alter or further reproduce or distribute any part of the course content to another person.

Inclusive Learning

All students are asked to discuss any impairment related requirements privately, face to face and/or in written form with the course coordinator, lecturer or tutor.

Student Disability Services also provides support for students with a wide range of impairments, both visible and invisible, to succeed and excel at the University. For more information and contact details, please visit the Student Disability Services’ website http://disability.auckland.ac.nz

Special Circumstances

If your ability to complete assessed coursework is affected by illness or other personal circumstances outside of your control, contact a member of teaching staff as soon as possible before the assessment is due.

If your personal circumstances significantly affect your performance, or preparation, for an exam or eligible written test, refer to the University’s aegrotat or compassionate consideration page https://www.auckland.ac.nz/en/students/academic-information/exams-and-final-results/during-exams/aegrotat-and-compassionate-consideration.html.

This should be done as soon as possible and no later than seven days after the affected test or exam date.

Learning Continuity

In the event of an unexpected disruption, we undertake to maintain the continuity and standard of teaching and learning in all your courses throughout the year. If there are unexpected disruptions the University has contingency plans to ensure that access to your course continues and course assessment continues to meet the principles of the University’s assessment policy. Some adjustments may need to be made in emergencies. You will be kept fully informed by your course co-ordinator/director, and if disruption occurs you should refer to the university website for information about how to proceed.

The delivery mode may change depending on COVID restrictions. Any changes will be communicated through Canvas.

Student Charter and Responsibilities

The Student Charter assumes and acknowledges that students are active participants in the learning process and that they have responsibilities to the institution and the international community of scholars. The University expects that students will act at all times in a way that demonstrates respect for the rights of other students and staff so that the learning environment is both safe and productive. For further information visit Student Charter https://www.auckland.ac.nz/en/students/forms-policies-and-guidelines/student-policies-and-guidelines/student-charter.html.

Disclaimer

Elements of this outline may be subject to change. The latest information about the course will be available for enrolled students in Canvas.

In this course students may be asked to submit coursework assessments digitally. The University reserves the right to conduct scheduled tests and examinations for this course online or through the use of computers or other electronic devices. Where tests or examinations are conducted online remote invigilation arrangements may be used. In exceptional circumstances changes to elements of this course may be necessary at short notice. Students enrolled in this course will be informed of any such changes and the reasons for them, as soon as possible, through Canvas.

Published on 31/10/2023 10:51 a.m.