This module is at an advanced level and requires learners to apply their prior knowledge of the principles of drug action and drug duration to more advanced topics in medicinal chemistry. The mechanism of action of a number of organic and inorganic drugs / therapies will be described in detail in terms of biological interactions, and relevant aspects of pharmacology. The use of QSARs in medicinal chemistry, the regulatory environment will be discussed. The roles and functions of metals in biological systems may also be discussed in detail.
The practical element will build on skills in previous modules, while supporting and reinforcing the concepts discussed in the lectures.
Quantitative Structure Activity Relationships
Historical context. Role in drug discovery and design. Hydrophobicity factors - P (partition factor) and p (substituent hydrophobicity constant) and examples. Electronic factors - Hammett substitution constant and aliphatic electronic substituent constants. Steric factors - Taft, Molar Refractivity, Verloop. Hansch Equation. Craig Plot. Topliss scheme. 3D QSAR and molecular modelling. Introduction to the role of QSARS in compiling the safety file/dossier for a chemical which is notifiable to the European Chemical Agency.
Chemotherapeutic agents
e.g. Antiparasitic agents, Anticancer agents, Antibacterial agents, Antiviral agents
Transition metal properties and how they are modified in biology
Specific roles of Iron, zinc, and cobalt in biological systems. Haemoglobin, myoglobin, zinc enzymes, vitamin B12. Applications of metal containing pharmaceuticals in medicines: Anticancer applications and applications of metal complexes in the treatment of fungal and bacterial infections.
A selection from the following may be included instead of some of the other topics above
Photomedical treatments, Industrial medicinal chemistry, Pharmacodynamic agents (e.g. Drugs that act on the cardiovascular system, Drugs to treat diabetes), Drug delivery.
Laboratory component
Laboratory work is sourced from the School of Chemical and BioPharmaceutical Sciences Laboratory Manuals.
Students will learn through lectures, problem solving and laboratory practicals.
Self directed learning is encouraged.
Online resources to encourage pre-laboratory and pre-lecture preparation will be hosted in Brightspace
| Module Content & Assessment | |
|---|---|
| Assessment Breakdown | % |
| Formal Examination | 75 |
| Other Assessment(s) | 25 |