Module Details

The information contained in this module specification was correct at the time of publication but may be subject to change, either during the session because of unforeseen circumstances, or following review of the module at the end of the session. Queries about the module should be directed to the member of staff with responsibility for the module.
Title Medicinal Chemistry of Anti-Infectives
Code CHEM335
Coordinator Professor PM O'Neill
Chemistry
P.M.Oneill01@liverpool.ac.uk
Year CATS Level Semester CATS Value
Session 2021-22 Level 6 FHEQ First Semester 7.5

Pre-requisites before taking this module (or general academic requirements):

CHEM231 CHEM231 - Organic Chemistry II; CHEM248 An Introduction to Medicinal Chemistry 

Aims

The aim of this module is to introduce students to the fundamental principles that underpin modern medicinal chemistry of anti-infective drugs; these will include qualitative and advanced quantitative SAR techniques, computer aided molecular design, further techniques in solid phase chemistry / combinatorial chemistry.  The course will build on the principles taught in the introductory medicinal chemistry module CHEM248.


Learning Outcomes

(LO1) By the end of the module students will have achieved a solid understanding of modern approaches to anti-infective drug design. In particular they should be able to show a clear understanding of:
* The mechanism of action, design and synthesis of b-lactam antibiotics.
* Antiviral drug design.
* Antifungal drug design.
* The importance of protease enzymes as drug targets as illustrated by examples including the falcipain 2 inhibitors (cysteine proteases) and HIV protease inhibitors (aspartate proteases). Reference will be made to drug discovery programmes focused on the SARS CoV2 main protease (cysteine protase)
* advanced techniques in computational drug design.

(S1) Students will develop their chemistry-related cognitive abilities and skills i.e. abilities and skills relating to intellectual tasks, including problem solving as required by the Chemistry subject benchmark statement. In particular they will gain the ability to adapt and apply methodology to the solution of unfamiliar problems

(S2) Communication skills through online team meetings

(S3) Organisational skills

(S4) IT skills through computational workshops and online exercises


Teaching and Learning Strategies

Lectures will be taught asynchronously via virtual learning environment (13 x 1h lectures with each lecture split into two halves), workshops (equivalent to 2x 2h) and associated assignments. Molecular modelling assignments will be supported virtually (e.g. via MS Teams and email). Each lecture will have discussion points and questions which will be covered in sequential lectures.

In summary:
13 lectures
2 tutorials (2 hours in length)
1 MCQ online
1 computational workshop and associated problems
3 feedback sessions (3 hours to provide students with answers and provide discussion points).


Syllabus

 

Lecture 1 - Introduction; Recap of the process of drug discovery including revision of QSAR, combinatorial chemistry and HTS. Major therapeutic areas targeted in module will be discussed.
Lecture 2 - Cysteine Protease Enzymes as Drug Targets; Design and Synthesis of Small Peptide Inhibitors.
Lecture 3 - Synthesis Aspects ; Peptides and Peptidomimetics
Lecture 4 - Peptide and Peptidomimetic Inhibitors of Falcipains 2 and 3. Computer based design of novel inhibitor templates.
Lecture 5 - HIV Protease Inhibitors 1; Mechanmism of action and drug design.
Lecture 6 - Medicinal Chemistry of Beta-Lactam Antibiotics 1
Lecture 7 - Medicinal Chemistry of Beta-Lactam Antibiotics 2
Lecture 8 - HIV Protease Inhibitors 2; SAR and Synthetic Approaches
Lecture 9 - Nucleoside analogues as antiviral agents
Lecture 10 - Medicinal Chemistry of antifungal agents
Lecture 11 - Advanced Techniques in Computational Drug Design 1
Lecture 12 - Advanced Techniques in Computational Drug Design 2
Lecture 13 - Revision lecture


Recommended Texts

Reading lists are managed at readinglists.liverpool.ac.uk. Click here to access the reading lists for this module.

Teaching Schedule

  Lectures Seminars Tutorials Lab Practicals Fieldwork Placement Other TOTAL
Study Hours 13

  6

      19
Timetable (if known)              
Private Study 56
TOTAL HOURS 75

Assessment

EXAM Duration Timing
(Semester)
% of
final
mark
Resit/resubmission
opportunity
Penalty for late
submission
Notes
remote examination. 2 hours on task  2 hours    60       
CONTINUOUS Duration Timing
(Semester)
% of
final
mark
Resit/resubmission
opportunity
Penalty for late
submission
Notes
two problem based tutorials, one MCQ, and one tutorial/computer modelling exercise Standard UoL penalties apply for late submission. There is no re-submission opportunity. These assignments are not  2 problem/computer m    40