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
Year CATS Level Semester CATS Value
Session 2023-24 Level 6 FHEQ First Semester 7.5

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

CHEM248 An Introduction to Medicinal Chemistry; CHEM231 Organic Chemistry II 


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 including computer-aided molecular design. 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 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)

(LO2) The mechanism of action, design and synthesis of b-lactam antibiotics and beta lactamase inhibitors.

(LO3) Approaches to antiviral drug design.

(LO4) The mechanism of action and antifungal drug design.

(LO5) 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 (13) will be delivered on campus with recordings available on Canvas.
Each lecture will have discussion points and questions which will be covered in subsequent lectures.
There is a single, formative MCQ supporting the lectures.

Tutorials will be held in-person on campus (equivalent to 2 x 2 hours). There will be one on-line molecular modelling workshop with associated problems
Two feedback sessions (also on campus) will provide students with answers to the tutorials and provide discussion points.

Lectures: 13 hr
Tutorials: 4 hr
Computational Workshop: 2 hr



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; Mechanism of action and drug design.
Lecture 6 - HIV Protease Inhibitors 2; SAR and Synthetic Approaches
Lecture 7 - Medicinal Chemistry of Antibacterials 1
Lecture 8 - Medicinal Chemistry of Antibacterials 2
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 Dr ug Design 2
Lecture 13 - Revision lecture

Recommended Texts

Reading lists are managed at Click here to access the reading lists for this module.

Teaching Schedule

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



Timetable (if known)              
Private Study 56


EXAM Duration Timing
% of
Penalty for late
written exam Resit: A single resit including reassessment of the coursework.  150    80       
CONTINUOUS Duration Timing
% of
Penalty for late
tutorials, modelling exercise Exemptions: electronic submission 3.2b, mix Resit: No separate resit, reassessment is included in exam resit    20