CH2MMP: Medicinal Chemistry for Pharmacists (Drug targets and how to access them)

Module Provider:

Chemistry, School of Chem, FoodBi and Pharm

Number of credits:

20 [10 ECTS credits]

Level:

I (Intermediate)

Terms in which taught:

Autumn, Spring and Summer

Module Convenor:

Dr JB Sweeney

Pre-requisites:

Co-requisites:

Modules excluded:

Module version for:

2007/8

Aims:
To provide pharmacy students with an overview of the drug discovery and development process. Particular emphasis is placed on understanding the nature of drug targets at the molecular level, namely receptors, enzymes, ion channels and nucleic acids, how these fit into overall cellular processes and how selective intervention by drugs can be achieved. This will enable students, dependant upon career pathway, to work as part of a multidisciplinary team in the pharmaceutical industry or in their role in a pharmacy to appreciate the origins of drugs and why there are therapeutic limitations to particular drugs e.g. lack of selectivity in action.

Assessable learning outcomes:
Students should be able to:
(i) Describe and discuss the key targets for drug action.
(ii) Explain how an understanding of drug targets at the molecular level facilitates the development of drugs and understanding of their mode of action.
(iii) Describe the interlocked nature of biosynthetic pathways and its implications for selective drug action.
(iv) Explain the relationship of endogenous and xenobiotic metabolism.
(v) Describe and assess the various strategies for drug discovery.
(vi) Describe aspects of the drug development process.
(vii) Be able to work within COSHH guidelines.
.

Additional outcomes:
Students will gain experience in problem solving via workshops and during these they will be encouraged to work in groups to promote team working. Experience in laboratory synthesis, purification and characterisation of drugs will allow, in conjunction with the analytical module CH2A4, pharmacy students to understand the issues surrounding provision of pure pharmaceuticals. Presentation skills will be developed during tutorials and workshops.

Outline content:
A T Russell (10 lectures) Introduction to Medicinal Chemistry
A study of the pathways for absorption, distribution, metabolism and excretion (ADME) of drugs paying particular attention to how this relates to their action at the appropriate cellular targets. Methods for studying and affecting a drug’s ADME will be examined, e.g. prodrugs, Log P etc.
A J A Cobb (10 lectures) Molecules of Medicinal Significance
This course will discuss the structures and chemistry of some key classes of compounds utilised/targeted in Medicinal Chemistry. In particular, the chemistry of amino acids, peptides, proteins, carbohydrates and nucleic acids will be outlined. This will set the scene for understanding the role of proteins, carbohydrates and nucleic acids as drug targets. Some basic topics in carbonyl group and heteroaromatic chemistry, relevant to drug synthesis, will also be covered.
A J A Cobb (10 lectures) Drug Discovery and Development
An introduction to drug discovery covering ‘me-too’ compounds, screening of natural products, mineral drugs, ethnopharmacology, clues from clinical side-effects, the role of synthesis, combinatorial methods and high throughput screening will be given. The use of bioisosteres in drug development and the use of feedback from pharmacokinetics data will be examined and discussed.
J E McKendrick (10 lectures) Key Cellular Processes and Health
A study of selected primary metabolic pathways of the cell with particular reference to disease and drug action. The relationship between endogenous and xenobiotic metabolism e.g. the role of CYP450’s in hormone production from cholesterol, the origin and metabolism of glucose - a key compound for phase II metabolism of xenobiotics. Understanding glucose metabolism will lead to an appreciation of diabetes in its various forms etc. The interrelationship of biochemical pathways, interdiction with drugs after the first committed step of a pathway and the problems and advantages of biochemical feedback e.g. 6-mercaptopurine.

Brief description of teaching and learning methods:
Two one hour lectures per week with approximately two tutorials in the spring and autumn term on related material. Additional directed private study will be given (26 hours over three terms). Twenty hours of practicals will be carried out in the summer term.

Contact hours:

Assessment:
Coursework
Students attend tutorials and workshops on the material covered in this module. Attendance is compulsory at both but only the former will contribute to the assessment of this module. Practical work is assessed through both work in the laboratory and the resultant reports. The tutorial and practical reports must be submitted by the date identified.

Relative percentage of coursework: Tutorials 10%; Practical work 25%

Penalties for late submission
In accordance with Faculty policy 10% of marks will be deducted from practical work which is submitted up to one week late. Work submitted later than this will receive no credit unless there are extenuating circumstances. Tutorial work that is submitted late will receive no credit unless there are extenuating circumstances and the relevant form is completed. Penalties for late submission of other coursework will be in accordance with University policy.

Examinations
One two-hour written paper during the Part 2 examination period. 65%

Requirements for a pass
A mark of 40% overall and a mark of 50% in the practical class plus at least a 75% attendance record in the practical classes (but see progression requirements in programme specifications).

Reassessment arrangements
By examination only in August or September.
If the practical element is not passed at the first attempt the student will have to sit and pass a seven-hour practical examination in September [in which case the maximum mark carried forward into the overall assessment of this unit will be 50%].