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2011/2 Provisional Module Catalogue - UNDER CONSTRUCTION & SUBJECT TO CHANGE
 Module Code: CHE2029 Module Title: MEDICINAL CHEMISTRY 1
Module Provider: Chemical Sciences Short Name: CHE2029
Level: HE2 Module Co-ordinator:
Number of credits: 15 Number of ECTS credits: 7.5
 
Module Availability
Semester 1
Assessment Pattern

Coursework 30%

Formal Examination 70%
Module Overview
Prerequisites/Co-requisites
Module Aims

To develop an understanding of biomolecules and natural products.

To understand how drugs interact with biomolecules and gain a strong grounding in the drug discovery, design and development process.
Learning Outcomes
  • On successful completion of this module you should, or should be able to:  
  • understand the history of drug discovery  
  • describe modern methods of drug discovery, design and development.  
  • develop an awareness of the pharmacodynamic and pharmacokinetic aspects of molecules that must be considered throughout the drug discovery process.
  • explain the chemistry of lipids, amino acids, peptides and proteins, carbohydrates, nucleic acids and alkaloids.
  • be aware of the important classes of natural products and aspects of their biosynthesis.
Module Content

DAM

 

 

1-6

 

 

 

 

Drug discovery: historical perspective

 

 

The acetate pathway: Fatty acids, prostagalandins, anthraquinones, aflatoxins, cannabinoids, tetracyclines, macrolides, polyenes and polyethers of medicinal importance

 

 

The shikimate pathway: Lignans, coumarins and flavonoids of medicinal importance. Phytoestrogens and vitamin E

 

 

DKW

 

 

7-26

 

 

 

 

Basic model of drug mechanism, medicinal chemistry introduction, modern drug discovery process. Diseases, disease mechanisms, drugs target part of the mechanism, examples: HIV, malaria, TB, MRSA, diabetes, cancer, hypertension, ischaemic heart disease, obesity.

 

 

The cell membrane: lipids, fatty acids, membrane proteins, crossing the cell membrane, drugs which target the cell membrane

 

 

Amino acids, peptides, proteins: 1°, 2°, 3°, 4° structure, peptide synthesis, gel electrophoresis, Western blotting, peptide/protein analysis.

 

 

Carbohydrates: mono, oligo, polysaccharides, carbohydrate (sugar) chemistry/synthesis.  Drugs that target carbohydrates.

 

 

Nucleic acids: DNA, RNA, replication, transcription, translation.  Drugs that target DNA/RNA.

 

 

Drug targets: receptors, enzymes, other proteins (structural, transporters), nucleic acids, membranes.  Target identification.  Introduction to target validation.

 

 

Drug-target binding interactions: electrostatic, H-bonding, dipole-dipole, repulsive, van der Waals, hydrophobic. 

 

 

Lead finding: ligand and target based: bioassay introduction, natural products, HTS, fragment-based drug discovery, virtual screening, ‘me-too’, hit validation, parallel chemistry, combinatorial chemistry.

 

 

SAR and structure based design.  Pharmacophore, introduction to computer aided drug design.  Selectivity, toxicity.

 

 

Pharmacokinetics: ADME: bioavailability, introduction to absorption, log P, distribution, metabolism, excretion, Lipinski’s ‘rules’, drug administration

 

 

Getting a drug to market: Toxicology testing, clinical trials, formulation and stability, regulatory affairs.

 

 

Drugs acting on the adrenergic system

 

 

Cancer therapeutics

 

 

Antiviral agents

 

 

DAM

 

 

27-33

 

 

 

 

The chemistry of the alkaloids: structures, biosynthesis, medicinally important examples

 

 

The recreational drugs. Opiates, morphine, heroin, cocaine. Phenylalkylamines. Ecstasy. Hallucinogens. Tryptamines. LSD. Drug abuse

 

 

Traditional medicine systems.  Ethnopharmacology

 

 
Methods of Teaching/Learning
Formal lecture and tutorial sessions.
Selected Texts/Journals

Essential: 

 

Bruice, P.Y., Organic Chemistry, 6th Edition, 2011, Pearson

 

Patrick, G. L., An Introduction to Medicinal Chemistry, 4th Edition, 2008,  Oxford University Press

 

Dewick, P.M., Medicinal Natural Products. A Biosynthetic Approach, 3rd Edition, 2009, Wiley

 

Recommended:

 

Clayden, J.P., Greeves, N., Warren, S., Wothers, P., Organic Chemistry, 1st Edition, 2001, Oxford University Press
Last Updated
20 April 2011