CH2MMP-Medicinal Chemistry for Pharmacists (Drug targets)

Module Provider: Chemistry, School of Chem, FoodBi and Pharm
Number of credits: 20 [10ECTS credits]
Level: I (Intermediate)
Terms in which taught: Autumn and Spring
Module Convenor: Dr AJA Cobb
Pre-requisites: PM1DS1
Co-requisites:
Modules excluded:
Module version for: 2008/9

Email: a.j.a.cobb@reading.ac.uk

Aims:
To provide pharmacy students with an overview of the drug discovery and development process. Students are taught how modern synthetic chemistry can be used to make compounds of medicinal importance and are introduced to new processes in synthetic organic chemistry. They are also introduced to concepts within pharmacokinetics; how drugs are taken up and distributed throughout the body. They are also given an overview of modern methods in drug discovery. This course 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:
• Explain how a variety of chemical mechanisms work and show an appreciation of their use within drug synthesis.
• Explain how an understanding of drug targets at the molecular level facilitates the development of drugs and understanding of their mode of action.
• Describe the interlocked nature of biosynthetic pathways and its implications for selective drug action.
• Explain the relationship of endogenous and xenobiotic metabolism.
• Describe and assess the various strategies for drug discovery.
• Describe aspects of the drug development process.
• 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 modules PM1DS1 and CH2A4, pharmacy students to understand the issues surrounding provision of pure pharmaceuticals. Presentation skills will be developed during tutorials and workshops.

Outline content:
Part a: The Nature of Drug Targets (20 Lectures)
A. J. A. Cobb (8) + H. M. I . Osborn (2) Molecules of Medical Significance
An overview of the diversity of molecular structures that are used as therapeutic agents and common methods used in their synthesis. This will include the importance of pKa and enolate chemistry and will be exemplified throughout with drug syntheses. Heterocyclic chemistry is then introduced and the synthesis and reactivity of selected classes are shown. An introduction to carbohydrate chemistry is then given and the lectures will conclude with nucleotide chemistry and its importance in drug discovery.

A.T. Russell (10) Drug Discovery
A study of the pathways for administration, distribution, metabolism and excretion (ADME) of drugs. Methods for studying and affecting a drug’s ADME will be examined, e.g. prodrugs, Log P etc.


Part b: Development of Pharmaceuticals: Active Compounds and Drugs, is there a Difference? (20 Lectures)

A. J. A. Cobb (10) Methods of Drug Discovery
An introduction to drug discovery covering ‘me-too’ compounds, screening for natural products, mineral drugs, ethnopharmacology, clues from clinical side-effects, the role of synthesis, combinatorial methods and high throughput screening. The use of bioisosteres in drug development and the use of feedback from pharmacokinetics data.

J.E. McKendrick (10) 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.

Reading List:
An Introduction to Medicinal Chemistry, 2nd or 3rd Edition, G.L. Patrick
The Organic Chemistry of Drug Design and Drug Action, R.B. Silverman
Foye’s Principples of Medicinal Chemistry, 5th Edition, D.A. Williams and T.L. Lemke
The Organic Chemistry of Biological Pathways, J. McMurry and T. Begley

Brief description of teaching and learning methods:
Two one-hour lectures per week with approximately one workshop on related material every four weeks. In response to student needs lecturers have the discretion to change one lecture to an extra workshop. Students attend 20 hours of Practical Work over the duration of the module.

Contact hours:

	Autumn	Spring	Summer
Lectures	20	20
Tutorials/workshops	2	2
Practicals			20
Preparation and analysis for tutorials/ seminars/ practicals	10	10	40
Directed private study: reading for practicals	10	10	10
Private study	14	15	16
Total hours	57	57	86
Number of essays or assignments
Other (eg major seminar paper)

Assessment:
Coursework
Students attend tutorials and workshops on the material covered in this module. Attendance is compulsory at both and both 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 20%

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. 70%

Requirements for a pass
A mark of 40% overall and a mark of 50% plus attendance in the practical classes.

Reassessment arrangements
By examination in August/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 August/September.

Last updated: 18 July 2008