PAC2171 - Basis of drug action I

Leader(s): Dr Bim Graham

Offered

Parkville First semester 2009 (Day)

Synopsis

This unit aims to equip students with a foundation of knowledge about the molecular structure of drugs, together with an understanding of the fundamental relationship that exists between the molecular structure of drugs and their pharmacokinetic and pharmacodynamic properties. It also seeks to provide students with an appreciation of the drug design process and the methods used to synthesise and establish the structure of drug molecules. The subject provides a firm foundation for the subsequent Basis of Drug Action II unit, as well as the "Integrated Therapeutics" 3rd year subjects, which focus on describing the major classes of drugs and how they function.

Objectives

At the end of this unit students will be able to:

1. Identify functional groups in drug molecules and describe the bonding interactions they may undergo with a target macromolecule;
2. Define the stereochemistry of chiral compounds and discuss why the shapes of drug molecules are important for biological activity;
3. Relate the bioavailability and physicochemical properties of a drug molecule to its chemical structure;
4. Recognise and describe structural modification strategies used to optimise the pharmacokinetic and pharmacodynamic properties of a drug;
5. Apply the concepts of QSAR;
6. Describe the general synthetic strategies used to synthesise drug leads and their analogues;
7. Analyse and interpret data to describe chemical structures;
8. Be proficient in basic chemical laboratory techniques and communicating results in written form.

Assessment

practical attendance and performance: 5%; on-line multiple choice quizzes: 15%; final exam (2.5 hours): 80%

Contact hours

36 1 hour lectures/whole class tutorials, seven 3 hour practical classes

Prerequisites

PAC1121 Organic chemistry (or VCP1021 Medicinal chemistry IA)
PAC1142 Chemistry of biomolecules (or VCP1022 Medicinal chemistry IB)

Additional information on this unit is available from the faculty at:

http://www.monash.edu.au/muso/support/