ADVANCED MEDICINAL CHEMISTRY - 2020/1

Module code: CHEM037

Module Overview

The module brings students to a position of knowledge, understanding and skills which would facilitate a new role in drug discovery research. It covers the most important aspects of modern medicinal chemistry in detail and also teaches developments in radioisotope medicinal chemistry, antibiotics and nanotherapeutics.

Module provider

Chemistry

Module Leader

WHELLIGAN Daniel (Chemistry)

Number of Credits: 15

ECTS Credits: 7.5

Framework: FHEQ Level 7

JACs code:

Module cap (Maximum number of students): N/A

Module Availability

Semester 2

Prerequisites / Co-requisites

none

Module content

Indicative content includes:

 


  • Target validation using genetic engineering molecular biology tools.

  • An introduction to X-ray crystallography and structure based design. 

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

  • Structure-Activity Relationships (SARs), medicinal chemistry strategy and synthesis.

  • Enzymes: methods of catalysis, inhibitor design and discovery. 

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

  • Receptors: agonists, antagonists, partial agonists, GPCRs, kinase-linked receptors, ligand gated ion-channels, signal transduction, affinity, efficacy, potency. 

  • Pharmacokinetics and strategies for improvements:  solubility, permeability, blood-brain barrier, pKa, log P, metabolism, toxic metabolites, excretion.

  • Nucleic acids as drug targets: DNA intercalation, alkylation, chain terminators, nucleic acid therapeutics. 

  • 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.

  • Radioisotope production, radioloabelling and radioimmunoassay

  • Nanotherapeutics

  • Process chemistry, scale-up.

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


Assessment pattern

Assessment type Unit of assessment Weighting
Coursework Coursework 20
Examination Examination 2 hr 80

Alternative Assessment

None.

Assessment Strategy

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


  • through coursework, the ability to research and understand a specified target protein, evaluate an imaginary hit molecule (with reference to published target ligands) in terms of possible binding interactions, and propose analogues with improved efficacy along with literature-based routes to their synthesis

  • through written examination, all learning outcomes



 

Thus, the summative assessment for this module consists of:


  • coursework incorporating a written research proposal and oral presentation to the class including the answering of questions

  • examination (2 h)



 

Formative assessment

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

The research proposal oral presentation takes place one week before the deadline for the written proposal to allow the students to act on (and therefore better internalise) immediate feedback.  For the presentation, some feedback is given immediately in the form of questions and suggestions for improvement of the proposed research.  Formal written feedback is given later including marks, why they were awarded and what could be done to improve.  Feedback to the written research proposal consists of annotations on the returned document and general comments on the mark sheet indicating why the given marks have been assigned and what could be done to improve.

Module aims

  • • give students an advanced understanding of how drugs work and are designed/discovered and developed.
  • • provide students with the ability to critically evaluate published medicinal chemistry programmes and make suggestions for drug design.

Learning outcomes

Attributes Developed
001 Review, critically evaluate and present background material from current topics in medicinal chemistry CKPT
002 Apply medicinal chemistry knowledge to suggest analogues of molecules, and their synthesis, to test structure-activity relationships, improve potency or alter pharmacokinetics KCP
003 Have a critical awareness of the natural function of major drug targets and the action of drugs upon them at the molecular level KC
004 Understand, critically evaluate and suggest late-stage and modern drug development strategies including process chemistry and the design of nanotherapeutics KC
005 Critically appreciate the role of metal complexes in diagnostics and therapy and solve problems related to choice of isotope and ligands KC

Attributes Developed

C - Cognitive/analytical

K - Subject knowledge

T - Transferable skills

P - Professional/Practical skills

Overall student workload

Independent Study Hours: 114

Lecture Hours: 32

Tutorial Hours: 1

Practical/Performance Hours: 3

Methods of Teaching / Learning

The learning and teaching strategy is designed to:


  • build on students’ knowledge of the basic drug discovery process and characteristics of drugs by providing them with a fuller understanding of considerations during drug design.

  • provide students with medicinal chemistry ‘tools’ which can be applied to the design of new medicinal chemistry programmes and permit critical evaluation of published programmes.



 

The learning and teaching methods include:


  • formal lectures bolstered by many examples and case studies of small molecule drugs, inorganic agents, antibiotics and nanotherapeutics as well as occasional group problem-solving tasks.

  • coursework: a written and orally presented research proposal for a medicinal chemistry programme based on a given target and imaginary hit.

  • all students attend all oral presentations to gain insights into these additional aspects of medicinal chemistry as well as practise their critical evaluation through asking questions.

  • independent learning (reading and revision). 

  • revision tutorial

  • written exam


Indicated Lecture Hours (which may also include seminars, tutorials, workshops and other contact time) are approximate and may include in-class tests where one or more of these are an assessment on the module. In-class tests are scheduled/organised separately to taught content and will be published on to student personal timetables, where they apply to taken modules, as soon as they are finalised by central administration. This will usually be after the initial publication of the teaching timetable for the relevant semester.

Reading list

Reading list for ADVANCED MEDICINAL CHEMISTRY :

Other information

None.

Programmes this module appears in

Programme Semester Classification Qualifying conditions
Medicinal Chemistry MChem 2 Compulsory A weighted aggregate mark of 50% is required to pass the module

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 2020/1 academic year.