MEDICINAL CHEMISTRY II - 2017/8

Module code: CHE3049

Module provider

Chemistry

Module Leader

WHELLIGAN DK Dr (Chemistry)

Number of Credits

15

ECT Credits

7.5

Framework

FHEQ Level 6

JACs code

F150

Module cap (Maximum number of students)

N/A

Module Availability

Semester 2

Overall student workload

Independent Study Hours: 120

Lecture Hours: 11

Assessment pattern

Assessment type Unit of assessment Weighting
Coursework COURSEWORK 30%
Examination EXAM 1.5 HOURS 70%

Alternative Assessment

None available

Prerequisites / Co-requisites

Module overview

The module provides a well-rounded knowledge of medicinal chemistry. Through its employment of example drug discovery projects from the research areas of viruses, antibiotics, diabetes, adrenergic receptors, cancer, nanotherapeutics and inorganic medicinal chemistry, it provides students with an understanding of design and discovery strategies which should allow them to critically evaluate new medicinal chemistry projects as well as suggest new research directions and ideas for improvements.

Module aims

To give students an advanced understanding of how drugs work and are designed, discovered and developed.

To provide students with a conceptual understanding of drug discovery, for several disease classes, through medicinal chemistry examples

Learning outcomes

Attributes Developed
Analyse classes of medicinally important natural products (antibiotics, terpenes) in terms of their biosynthesis and mode of action
Conceptually rationalise the role of metal complexes in diagnostics and therapy and be able to solve problems related to their use
Understand the targeting of biological pathways with drugs to treat several major diseases
Review and critically evaluate material describing the mode of action, discovery and development of known drugs
Apply medicinal chemistry methods for the determination of structure-activity relationships and improvement of drug pharmacodynamics and pharmacokinetics

Attributes Developed

C - Cognitive/analytical

K - Subject knowledge

T - Transferable skills

P - Professional/Practical skills

Module content





Indicative content includes:




Target validation: genetic engineering, RNAi.

X-ray crystallography (crystallisation, soaking, X-ray), structure based design. 

Advanced binding interactions: DG, binding role of functional groups and amino acids, the hydrophobic effect.




Adrenergic receptors: GPCRs, agonists, antagonists, partial agonists, GPCRs, affinity, efficacy, potency.  Associated drugs, their mechanisms of action and discovery.




Viruses and antiviral drugs.  Vaccines and antiviral drugs.  DNA chain terminators.  Enzymes: kinases, peptidases, reversible inhibitors.




Antibiotics, their discovery.  Natural and semisynthetic β–lactams (penicillins and cephalosporins), their mechanism of action.  Other antibiotics, the problem of drug resistance (MRSA etc).




Diabetes, mechanisms of action of insulin and drugs.  Discovery of new therapeutics.  Receptors: kinase-linked receptors, ligand gated ion-channel receptors, intracellular receptors, signal transduction.




Cancer and chemotherapy.  Nucleic acids as drug targets: DNA intercalation, alkylation.  The design of modern targeted therapeutics.




Photodynamic therapy.  Porphyrin and phthalocyanine complexes, their mode of action.

Metal ions and chelating agents in therapy.  Ligand design, choice of metal ion and targeting strategies.

Radioisotopes for biological imaging and therapy.  Ligand design and targeting strategies.




Nanotherapeutics




Process chemistry, scale-up.




The pharmaceutical industry.  Generic drugs. Ethical aspects. Clinical trials. Patents





 

 

Methods of Teaching / Learning

The learning and teaching strategy is designed to:



Build on students’ knowledge of the drug discovery process, methods and characteristics of drugs by providing them with a fuller understanding of considerations during their design through the use of case studies in several specific areas.


Provide students with an ability to understand new drug discovery programmes, critically evaluate them and suggest future work or improvements.



 

The learning and teaching methods include:



Formal lectures which contain occasional group problem-solving tasks. (30 h)


Coursework: a written critical review of published medicinal chemistry programmes for a given biomolecular target, not discussed in lectures, followed by suggested future directions. (25 h)


Independent learning (reading (some directed) and revision).(92.5 h)


Revision tutorial (1 h)


Written exam (closed book, 1.5 h)


Assessment Strategy

The assessment strategy is designed to provide students with the opportunity to demonstrate,

 

through coursework, the ability to:


research, understand and critically evaluate drug discovery programmes reported in the literature, against a target not met in lectures, by applying knowledge gained in the module  [LOs 2, 3, 4]


 

through written examination, all learning outcomes [LOs 1-5]

 

Thus, the summative assessment for this module consists of:


coursework incorporating a review of medicinal chemistry programmes on a given target [LOs 3, 5] (25 h, deadline week 9, 30%)
examination [LOs 1-5] (1.5 h, 70%)


 

Formative assessment and feedback

Small problem-solving tasks are included in some lectures.  During the task, the lecturer moves amongst the groups commenting and guiding the students’ starting points and answering strategies.  Common difficulties are highlighted to the whole class and the final solution is given on the board/visualiser.

Feedback to the written review consists of annotations on the returned document and a breakdwon of marks into specific headings along with written general feedback giving justifications for the marks and suggestions for improvement.

Reading list

Reading list for MEDICINAL CHEMISTRY II : http://aspire.surrey.ac.uk/modules/che3049

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.