PH2S47 - Heterocyclic Chemistry and an Introduction to Drug Design 01 Sep 2020 - 31 Aug 2023 | Version 6
Associated Module Information
| Module Code: | PH2S47 | ||
|---|---|---|---|
| Module Title: | Heterocyclic Chemistry and an Introduction to Drug Design | ||
| Faculty: | Faculty of Computing, Engineering and Science | ||
| Faculty Group: | Chemical and Environmental Sciences | ||
| Faculty Sub Group: | Chemical and Environmental Sciences | ||
| Module Leader: | Rehana Karim | ||
| Module Team: | Andrew Graham, Natasha Galea, Gareth Owen, Suzanna Kean | ||
| First Intended Intake: | MAR 2015 | Final Year of Intake: | 2013 |
| Date Closed: | |||
| Credit Value: | 20 | Credit Level: | 5 |
| Language: | English | ||
| Percentage of Module Taught in Welsh: | 0 | ||
| Equivalent Module: | |||
| HECOS codes: | 100423 - pharmaceutical chemistry | ||
| HECOS Code Weighting: | 100 | ||
Document Version Information
| Version | 6 |
|---|---|
| Valid From | 01 Sep 2020 |
| Valid To | 31 Aug 2023 |
Module Aims
1. To provide a comprehensive introduction to heterocycles together with an appreciation of their reactivity and pharmaceutical importance.
2. Apply the principles of chemistry for an understanding of drug action, design and synthesis.
3. Understand and apply various analytical techniques to chemical and pharmaceutical analysis.
Content Summary
a) Introduction to Heterocyclic Chemistry
Introduction - General nature of heterocyclic compounds and their importance as pharmaceuticals, agrochemicals, dyestuffs and pigments. Heterocyclic structures in natural compounds. Reminder of benzene - structure and reactivity.
Reactivity of pi -Excessive Heteroaromatics - Electronic structure and effect on reactivity. Electrophilic (and nucleophilic) substitution reactions of pyrroles, indoles, furans, thiophenes, and azoles. Reactivity of selected functionalised derivatives.
Reactivity of pi -Deficient Heteroaromatics - Electronic structure and effect on reactivity. Electrophilic and nucleophilic substitution. Reactions of pyridines, and their benzo- fused analogues. Reactions at the heteroatoms. Reactivity of N-oxides and some functionalised derivatives.
b) Introduction to Drug Design
An introduction to fundamental aspects of medicinal and pharmaceutical chemistry. Development of pharmaceutical chemistry and future directions. Basic structural requirements for pharmaceutical activity (Lipinski rule of 5) including physicochemical, stereoisomeric and electronic properties of drug molecules and intermolecular forces. Drug targets including drug receptors, enzymes and non-specific interactions. Fundamentals of pharmacokinetics and pharmacodynamics including partitioning of drugs and drug transport and routes of administration. Basic drug design, development and lead compound identification. Fundamentals of structure-activity relationships and quantitative structure-activity relationships including case studies on the design and development of salbutamol, propranolol and cimetidine. Inflammatory and analgesic drugs; antifungal and antibiotic drugs.
Learning and Teaching Methods
| Activity Type | Hours |
|---|---|
| Lecture | 18 |
| Tutorial | 18 |
| Practical classes and workshops | 12 |
| Directed Study | 76 |
| Independent Study | 76 |
| Total Hours Selected | 200 |
Learning Outcomes
| # | Learning Outcome |
|---|---|
| LO1 | Critically evaluate strategies for the synthesis of a wide range of heterocyclic compounds |
| LO2 | Demonstrate knowledge of the techniques used and an ability to work safely and effectively with a range of organic reagents. |
| LO3 | Apply diagnostic and creative skills to review fundamental aspects of medicinal and pharmaceutical chemistry and demonstrate knowledge of basic drug design, development and lead compound identification. |
Module Requisites
N/A
Assessment Criteria
| Assessment Category | Assessment Type | Description | Duration | Word Count | Weight (%) | Best of? | Pass Mark |
|---|---|---|---|---|---|---|---|
| Synchronous Onsite Assessment (Exam) | Onsite Closed Book Examination 1 | Final end of year exam | 150 | N/A | 65 | No | 40 |
| Practical Assessment (CW) | Practical Coursework 1 | Written reports describing laboratory experiments - Students are expected to spend 1 hour on their assessment for every 1 hour spent in the laboratory. | 0 | N/A | 35 | No | 40 |
Assessment Matrix
| Assessment Type | Learning Outcomes | ||
|---|---|---|---|
| LO1 | LO2 | LO3 | |
| Onsite Closed Book Examination 1 | ✔ | ✘ | ✔ |
| Practical Coursework 1 | ✔ | ✘ | ✔ |