University of the West of England

MODULE SPECIFICATION

Code: USSJ8A-20-2 Title: MEDICINAL CHEMISTRY Version: 4

Level: 2 UWE credit rating: 20 ECTS credit rating: 10

Module type: STANDARD

Owning Faculty: Health and Life Sciences Field: Applied Sciences

Valid from: October 2007 Discontinued from:

Pre-requisites: USSJR9-20-1 Chemical Principles, USSJRA-20-1 Chemistry in Context

Co-requisites: None

Excluded combinations: None

Learning outcomes:

Students will be able to:

      • identify potential targets for drugs;

      • apply chemical knowledge to the principles of drug design and development;

      • illustrate the role of molecular modelling in drug design and development;

      • explain the action and related development of selected examples of antimicrobial agents, cholinergic and anticholinergic drugs and antihypertensive agents.

Syllabus outline:

Targets for Drugs

      Enzymes, review of induced fit theory, survey of types of catalysis, introduction to design of inhibitors. Receptors, release of neurotransmittors, interaction with receptors, effect on ion channels, membrane bound enzymes. Agonists and antagonists, an introduction to their design. Partial agonists, desensitization. Tolerance and dependence

Drug Development

      Lead compound, structure-activity relationships. Strategies for development of synthetic analogues; substitutents, structure extension/contraction, isosteres, rigidification, receptor interaction. Stability of drugs, absorption, prodrugs, bioisosteres. Introduction to quantitative structure-activity relationships.

Molecular Modelling

    Examples of experiments to study sites of reactivity, energies of reaction, rates of reactivity or modification of drug structure.

Case Studies.

Application of the above principles to a selection of the following case studies:

Antimicrobial agents - ome mechanisms of action. Inhibition of cell metabolism, sulphonamides. Inhibition of cell wall synthesis, development and action of the penicillins and cephalosporins.

Drugs acting on the peripheral nervous system: Cholinergic and anticholinergic drugs. Effects of production of acetyl choline. Development of agonists at the cholinergic receptor. Antagonists of the muscarinic and nicotinic cholinergic receptors. Antihypertensives: Mechanisms of action and development of important examples.

Teaching and learning methods:

The module will be presented as lectures, tutorial and workshop sessions.

Reading Strategy

All students will be encouraged to make full use of the print and electronic resources available to them through membership of the University. These include a range of electronic journals and a wide variety of resources available through web sites and information gateways. The University Library’s web pages provide access to subject relevant resources and services, and to the library catalogue. Many resources can be accessed remotely. Additional useful texts can be accessed at shelf marks 615.1 and 541.22. Students will be presented with opportunities within the curriculum to develop their information retrieval and evaluation skills in order to identify such resources effectively.

This guidance will be available either in the module handbook, via the module information on UWEonline or through any other vehicle deemed appropriate by the module/programme leaders.

      • Patrick, G L, An introduction to Medicinal Chemistry, Oxford University Press (2001)

      • Thomas, G, Medicinal Chemistry – an introduction, Wiley (2000)

      • Silverman, R B, The Organic Chemistry of Drug Design and Drug Action, Academic Press (1992)

      • Rang M P, Dale M M, Ritter J M, Pharmacology, Churchill Livingstone (1995)

      • Hinchliffe, A, Modelling Molecular Structures, Wiley (1996)

Assessment

Weighting between components A and B (standard modules only) A: 50% B: 50%

ATTEMPT 1

First Assessment Opportunity

Component A Element weighting

EX1

Examination (2 Hours)

1

     
     
 

 

Component B

Description of each element Element weighting

PO

Poster presentation

1

PF

Portfolio of worksheets

1

     
 

 

Second Assessment Opportunity (further attendance at taught classes is not required)

Component A

Description of each element Element weighting

EX1

Examination (2 Hours)

1

     
     
 

 

Component B

Description of each element Element weighting

CT

Critical Review

1

PF

Portfolio of Worksheets

1

     
 

 

SECOND (OR SUBSEQUENT) ATTEMPT Attendance at taught classes is required.

Specification confirmed by …………………………………………………Date ……………………………

(Associate Dean/Programme Director)

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