Download ABCT462

Subject Description Form
Subject Code
ABCT462
Subject Title
Medicinal Chemistry
Credit Value
3.0
Level
4
Pre-requisite /
Co-requisite/
Exclusion
Organic Chemistry II (ABCT342)
Objectives
After taking this subject, students will have a systematic understanding of the
basic chemical and biochemical basis of drug research and development in the
pharmaceutical industry; the analytical skill in evaluate the benefits and
limitations of therapeutic agents currently in use or understanding; and a
stronger interest in the discipline of chemical technology and applied biology.
Intended Learning
Outcomes
Upon completion of this subject, the students will be able to
Subject Synopsis/
Indicative Syllabus
Basic chemical and biochemical concepts:
a. discuss and contrast the chemical and biochemical basis of drug
development in the pharmaceutical industry.
b. recognise the concepts of enzyme inhibition, receptors and ligands, agonists
and antagonists.
c. optimize the various chemical and physical parameters which affect the
development and use of therapeutic agents.
d. analyze the benefits and criticize the limitations of therapeutic agents
currently in use or in development.
e. develop a greater interest in the field of synthetic chemistry and chemical
biology, and a better understanding of the potential of the field in the
pharmaceutical industry.
Stereochemistry; chemistry of lipids, steroids, carbohydrates, amino acids, and
nucleic acids; biochemistry of proteins, DNA and RNA, glycolipids and
glycoproteins.
The process of drug development--a brief outline:
Screening and bioassays; the lead compounds; synthetic analogues; molecular
modeling; physiochemical properties and drug design, structure-activity
relationships; pharmacodynamics; clinical testing;
Combinatorial Chemistry in drug development:
Parallel synthesis; mix and split technique; deconvolution and encoding methods;
dynamic combinatorial chemistry; click chemistry;
The antibiotics:
The bacterial cell wall biosynthesis; the-lactam antibiotics; the chemistry of
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penicillins, cephalosporins and carbapenams; the -lactamases and drug resistance;
the tetracyclines; the aminoglycosides; the macrolides; chloramphenicol; the
quinolones; the superbugs!
The anti-parasitic, anti-fungal and anthelmintic drugs:
Chemotherapy of malaria and resistance; the discovery of quinghaosu and recent
developments; anti-fungal drugs; anthelmintics;
Anti-viral drugs:
How viruses reproduce; amantadine and analogs; the nucleoside analogs; the
protease inhibitors; treatment of HIV by combination therapy; the development of
zanamivir as anti-influenza drug;
Analgesics and Nonsteroidal anti-inflammatory drugs (NSAIDs):
Pain and analgesics; prostaglandins and the arachidonic acid cascade; new antiinflammatory drugs; morphine and narcotics; opiate receptors and endorphins;
Drugs affecting cholinergic and adrenergic neurotransmitters:
The neurotransmitters; cholinesterase inhibitors; cholinomimetics and Alzheimer's
disease; anticholinergics; adrenoreceptors; selective a- and ß-blockers;
Selected topics through guided study:
Chemistry and biochemistry of steroids; cholesterol and coronary heart disease;
drugs based on inhibition of cholesterol biosynthesis; the corticosteroids; antiinflammatory steroids; the sex hormones; contraceptive drugs; the anabolic
steroids; the cell cycle; cause of cancer; cancer chemotherapy; alkylating agents;
anti-metabolites; intercalating agents; mitotic inhibitors; multidrug resistance;
The content of this subject is subject to change with reference to Patrick, G. L.’s
book - An Introduction to Medicinal Chemistry.
Teaching/Learning
Methodology
Assessment
Methods in
Alignment with
Intended Learning
Outcomes
The students are encouraged to develop an independent approach of learning the
subject matters. Lecture notes will be given to students one week ahead and the
students can participate in the discussion of lecture materials. The students are
also required to undertake an independent study of an existing drug and give an
oral presentation to the class.
Specific assessment
methods/tasks
Intended subject learning outcomes to
be assessed (Please tick as
appropriate)
a
b
c
d
e
1. Examination
70
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√
√
√
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2. Test
30
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Total
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%
weighting
100 %
Explanation of the appropriateness of the assessment methods in assessing the
intended learning outcomes:
Student Study
Effort Required
Class contact:

Lecture
36 Hrs.

Tutorial
6Hrs.
Other student study effort:

Self Study
108 Hrs.
(reading on textbooks, reference books, notes etc)
Total student study effort
Reading List and
References
150 Hrs.
Essential
An Introduction to Medicinal Chemistry Patrick, G. L. Oxford University Press,
Oxford, 2005
Supplementary
Medicinal Chemistry: Principles and Practice, 2nd Ed. King, F. D. Ed. Royal
Society of Chemistry, Cambridge, 2002
Fundamentals of Medicinal Chemistry Thomas, G. Wiley, West Sussex, 2003
Burger’s Medicinal Chemistry and Drug Discovery, 6th Edition Abraham, D. J.
Ed. Wiley, Hoboken, 2003
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