The aim of this module is to introduce students to the fundamental principles that underpin modern medicinal chemistry, including an introduction to targets for drug action, methods of administration, qualitative and quantitative SAR, natural products medicinal chemistry, kinase drug discovery and solid phase chemistry /combinatorial chemistry. The course will also introduce approaches to the design of high quality hits using fragment based drug design introducing the concepts of Ligand Efficiency, and Lipophilic Ligand Efficiency.

(LO1) By the end of this module students are expected to have acquired an understanding of

The principle bonding interactions in drug receptor interactions.

(LO2) The basic concepts of structure activity relationships (SAR) and quantitative structure activity relationships (QSAR)

(LO3) The basic concepts of structure activity relationships (SAR) as applied to Beta Blocker Drug Design

(LO4) The basic concept of modulating drug metabolism by the use of fluorine substitution

(LO5) The basic concepts of Ligand Efficiency and Lipophilic Ligand Efficiency and Fragment Based Drug Design

(LO6) Peptide synthesis, protecting groups and combinatorial chemistry/ parallel synthesis approaches

(LO7) Optimal properties of small molecule leads, Lipinski’s Rules and Pro-drug design

(LO8) The importance of natural product drug discovery and understanding of kinase inhibitor mechanism

(S1) Students will develop their chemistry-related cognitive abilities and skills, i.e. abilities and skills relating to intellectual tasks, as required by the Chemistry subject benchmark statement, including:

Problem solving and the ability to adapt and apply methodology to the solution of unfamiliar problems.

(S2) Communication skills through online Teams Meetings and face to face tutorials

(S3) Organisational skills

Lectures. These will be delivered in-person. Selected lectures will have discussion points and questions which will be covered in following lectures.
Formative MCQ will be posted online in Canvas.
The lectures are supported by two in-person workshops (equivalent to 2 x 2 hr).

Coursework. Two assignments with marked work returned to students, supported by two feedback sessions on MS Teams (2 x 1 hr).

*Lectures: 14 hr
*Workshops: 4 hr
*Feedback sessions: 2 hr

Lecture 1 Structures of Proteins: Bonds/ Energies Involved in Drug Receptor Interactions Introduction to Medicinal Chemistry:
Lecture 2 Drug discovery and development
Lecture 3 The Pharmaceutical, Pharmacokinetic and Pharmacodynamic Phases
Lecture 4 Structure Activity Relationships (SAR I)
Lecture 5 (SARII): Fluorine Substitution in Medicinal Chemistry
Lecture 6 Quantitative Structure Activity Relationships (QSAR)
Lecture 7 Drug Design – Ligand Efficiency and Lipophilic Ligand Efficiency
Lecture 8 Drug Design - Fragment Based Drug Discovery
Lecture 9 Peptide Synthesis: Protecting Group Strategy in Synthesis
Lecture 10 Combinatorial Chemistry I
Lecture 11 Combinatorial Chemistry II
Lecture 12 Drug Design – Lipinski's Rules
Lecture 13 Natural Products in Medicinal Chemistry
Lecture 14 Kinase Drug Discovery