MEDICINAL CHEMISTRY 1 - 2017/8
Module code: CHE2029
WHELLIGAN DK Dr (Chemistry)
Number of Credits
FHEQ Level 5
Module cap (Maximum number of students)
Overall student workload
Independent Study Hours: 116
Lecture Hours: 36
|Assessment type||Unit of assessment||Weighting|
|Examination||EXAM - 1.5 HRS||70%|
|Coursework||COURSEWORK PROBLEM SHEET||30%|
Prerequisites / Co-requisites
This module builds on general organic chemistry knowledge in the context of biomolecules including proteins, carbohydrates, nucleic acids and natural products from common biosynthetic pathways. It covers the biomolecules’ natural and synthetic chemistry and uses this foundation to support a basic understanding of drug action and the drug discovery process.
To provide students with an understanding of the chemistry of biomolecules and natural products and their interaction with drugs.
To provide students with a strong grounding in the drug discovery, design and development process
|Understand modern and historical drug discovery strategies|
|Explain the bonding and reactivity of proteins, lipids, carbohydrates, nucleic acids and selected classes of natural products|
|Solve basic problems set on the classification, synthesis, biosynthesis or synthetic manipulation of biomolecules and natural products|
|Identify pharmacophores and structure-activity relationships from medicinal chemistry datasets|
|Suggest and/or apply basic drug discovery methods and principles to taught and new examples|
C - Cognitive/analytical
K - Subject knowledge
T - Transferable skills
P - Professional/Practical skills
Indicative content includes:
Drug discovery: historical perspective
Basic model of drug mechanism, medicinal chemistry introduction, modern drug discovery process and examples
Drug-target binding interactions: electrostatic, H-bonding, dipole-dipole, repulsive, van der Waals, hydrophobic.
Drug targets: receptors, enzymes, other proteins (structural, transporters), nucleic acids, membranes. Target identification. Target validation.
Amino acids, peptides, proteins: 1°, 2°, 3°, 4° structure, peptide synthesis, gel electrophoresis, Western blotting, peptide/protein analysis.
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.
The cell membrane: lipids, fatty acids, membrane proteins, crossing the cell membrane, drugs which target the cell membrane
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, regulatory affairs.
Carbohydrates: mono, oligo, polysaccharides, carbohydrate (sugar) chemistry/synthesis. Drugs that target carbohydrates.
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
The mevalonate pathway: the terpenoids, classes, nomenclature, steroid hormones and other medicinally important terpenoids
Traditional medicine systems. Ethnopharmacology
The chemistry of the alkaloids: structures, biosynthesis, medicinally important examples, recreational drugs and drug abuse
Nucleic acids: DNA, RNA, replication, transcription, translation. Drugs that target DNA/RNA.
Methods of Teaching / Learning
The learning and teaching strategy is designed to:
introduce chemists to drug discovery and provide them with a foundation in biomolecules for understanding more advanced drug discovery concepts and biochemistry in the future.
The learning and teaching methods include:
Formal lectures (32 h) and tutorial sessions (2 h), directed reading of the literature for question sets.
The assessment strategy is designed to provide students with the opportunity to demonstrate,
through coursework, the ability to:
apply knowledge and skills from lectures to answer problems on related examples of biomolecule identification, biosynthesis and medicinal uses
the use of knowledge from lectures and, where necessary, further background reading to comprehend a drug discovery paper from the peer-reviewed literature and answer a set of questions on it
through written examination, those learning outcomes not covered by the coursework [LOs 1-5]
Thus, the summative assessment for this module consists of:
two coursework problem sets based on lecture material and a drug discovery publication. The first provides an opportunity for mid-module feedback before the final, higher value piece. [LOs 1-5] (10-15 h, deadlines week 7 and week 10, 10+20=30%).
examination [LOs 1, 2(a), 3, 4, 5] (1.5 h, closed book)
Formative assessment and feedback
Most lectures contain a small problem-solving task which is addressed in groups of 2-3. During the task, the lecturer moves amongst the groups commenting and guiding the students’ starting points and answering strategies. Common problems are highlighted to the whole class and the final solution is given on the board/visualiser.
Feedback to the coursework will consist of annotations to individual student’s work as well as a general feedback document covering common misconceptions and mistakes.
Reading list for MEDICINAL CHEMISTRY 1 : http://aspire.surrey.ac.uk/modules/che2029
Please note that the information detailed within this record is accurate at the time of publishing and may be subject to change. This record contains information for the most up to date version of the programme / module for the 2017/8 academic year.