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Microsoft word - as140_abct462 medicinal chemistry_tye_9 jan 2013
Subject Description Form
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.
Upon completion of this subject, the students will be able to
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
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
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.
Basic chemical and biochemical concepts:
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
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 anti-inflammatory 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; anti-inflammatory 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.
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.
Explanation of the appropriateness of the assessment methods in assessing the intended learning outcomes:
(reading on textbooks, reference books, notes etc)
Reading List and
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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