CBMS842 is a 4 credit point, half year unit and will require an average of 12 hours of work per week (contact hours plus self study time).  For students with weak chemistry backgrounds, more time than the average 12 hours per week will probably be necessary to perform satisfactorily in this unit. CBMS842 is run with three hours of lectures/tutorials per week, along with 4 hour blocks of laboratories/workshops.  Additional time (~5 x 4 hr slots) will also be needed to conduct computational chemistry workshops.  Students are required to attend all lectures, tutorials, laboratory classes and computational chemistry workshops.  Active participation by the students in all of these fora is expected.

• Lectures will be presented as a combination of formal lectures and interactive tutorial sessions. Some lecture material will be available on the unit web site, while other material will be provided in the lecture class.  Learning is an active process, and as such, you must engage with the material. This means reading the textbook (and beyond) before and after lectures and studying the computational chemistry notes after each workshop, attempting the assignment questions and other questions, discussing the concepts with your classmates and lecturers.  Do not be afraid to ask questions – everyone benefits from a robust and open discussion of the topics.
• Assignment questions are issued so that you will have the opportunity to use the information provided in the lectures and textbook and to test your degree of understanding of those topics as well as further explore the literature to extend your knowledge in contemporary medicinal chemistry.
• Spot tests and a mid session test will also be run in the lecture session.  The spot tests will cover any material prior to that day’s lecture, therefore all students are expected to keep up to date with lecture material through revision each week.  The spot tests and mid session test are designed to allow you to continuously learn and to identify what you understand and the areas that you need to spend more time on, with minimal assessment penalty.  
• The computational chemistry workshops will allow you to develop skills in visualisation and explaining of specific properties of drugs and drug development methods. 
• To develop communication skills, a short oral on a research topic related to chemical biology will be assessed.  You will also be asked for an oral defence of your first assignment (pharmaceutical agent profile) to both determine your true understanding of specific concepts and to further develop your communication skills.
• All laboratory experiments will be conducted in groups.  These have a highly collaborative and investigative approach, where you will be designing and synthesising a series of sulfonamides and subsequently testing them for antibacterial activity to determine the important features for their antibacterial activity.  In addition, the program MOE will be used to derive a QSAR relationship for the class results in conjunction with published data on a wide range of sulfonamides.  The laboratory work is designed to give real life experiences in research by involving students in the design of the experiments, using literature procedures as a guide, and trouble shooting to identify the best experimental conditions.  It will emphasise the importance of being highly prepared for all experiments and being fully aware of all safety procedures, proper recording and reporting of all data and interpreting of all results, and having an analytical and inquisitive approach.

Unit Web Page

The web page for this unit can be found at ilearn.mq.edu.au. Just login and follow the prompts to CBMS842. You can use any web browser such as Firefox, Internet Explorer or Safari to login.  iLearn is the name for Macquarie University’s new Learning Management System (LMS). The iLearn online learning environment enables learning, teaching, communication and collaboration. It is used to make lecture notes, laboratory notes, discussion forums, digital lecture recordings and other learning resources available to students online.

Technology Used

You are expected to access the unit web site frequently  This contains important information including notes on the topics to be covered; the laboratory manual; What You Need to Know Sheets; your marks for practicals, quizzes and the mid-session exam; and past exam papers, including with answers.  Additionally, the web site will also be used to post important messages and links to internet facilities and sites of relevance to the course, downloadable software, and lots of other interesting material. If you do not have your own computer you may wish to access the Medicinal Chemistry web resources on campus using the PC computers in the Library or in the C5C computer laboratories.  To view notes on all the topics and past exams on the unit web site, you will require Adobe Acrobat Reader Version 9 or later to be installed on your computer. Acrobat Reader can be downloaded from the Adobe web site http://get.adobe.com/uk/reader/. If you are using the computers in the library, then Acrobat has already been installed.  Please note information will also be sent by email to your student email account so please look at your email account on a frequent basis. You are expected to access SciFinder Scholar and Reaxys to assist in searching the literature. These are available through the library web site. Hand-held calculators will be occasionally used in tutorials and practicals, for tests and in the final examination. Note that text-retrieval calculators are not allowed in the in-semester tests or final examination.

Lectures/tutorials: 

The first 3/4 of CBMS842 will provide an overview of the important concepts in medicinal chemistry and the last 1/4 will concentrate on a series of case studies (e.g. penicillins). CBMS842 has three hours/week allocated to lectures/tutorials. While formal lectures will be presented, discussion sessions will also form a major part of the classes. This will be supplemented by practical classes utilising synthetic chemistry, spectroscopic methods and bioassays and workshops on computational chemistry methods.

The laboratory classes will be run in groups and students are required to, in part, design the experiments, using literature procedures as a guide.  Considerable preparation is therefore needed. Past students have found this a valuable experience as it gives them a realistic approach to conducting research.  The laboratory classes will run every week, Friday 1-5 pm except Good Friday, the mid-session break and week 13.

Topics          Lect/Tut  Lecturer

• Overview of Medicinal Chemistry         wk 1-2       JJ
• Cellular targets (‘receptors’) for drug action
• Binding of drugs to ‘receptors’
• Interaction of ‘receptors’ with agonists and antagonists

• Protein structure and function            wk 2-3      JJ
• Enzyme kinetics
• Interaction of enzymes with inhibitors (competitive, non-competitive)
• Nucleic acids              wk 4      JJ

• Drug discovery from nature wk 4-6 JJ
• Drugs from synthesis
• Optimisation of lead compound, structure-activity relationships
• Physicochemical properties of drugs           
• Drug absorption, distribution, metabolism and excretion 
• Prodrugs     

• Quantitative structure-activity relationships          wk 7-10      PK
• Combinatorial synthesis
• Case Studies (G-coupled protein receptors)

• Case studies (e.g. antibacterial agents) wk 10-12                         JJ
• Chemoinformatics (Guest lecture)

• Discussion of sulfonamide antibacterial assays and lab report wk 12/13     JJ/PK
• Revision wk 13    JJ/PK

This  unit is essentially the same as last year.