BMC1021 - Introduction to Medicinal Chemistry

Leader: Dr Ian Crosby

Offered

Clayton Second semester 2007 (Day)

Synopsis

This subject introduces the participant to drugs and why we need new ones? Topics to be covered will include a historical perspective of drug discovery; an introduction to drug action, sources of drugs, drug discovery by design, protein-drug interactions, drug solubility membranes,pharmacokinetics, drug stability, drugs and metal chelation, metalloproteins, chelation therapy.

Objectives

1. Appreciate the relative scale of organisms, organs, cells, bacteria, viruses, proteins, drugs, atoms.
2. Give simple definitions of drug, activity, potency, efficacy, side-effect, ligand, macromolecule, agonist, antagonist, substrate, inhibitor, ED50, LD50, therapeutic index, lead compound, analogue compound, dosage form, active consituent, excipient, route of administration, prodrug, pharmacophore
3. Briefly discuss, in simple terms, enzyme action and methods of enzyme inhibition
4. Briefly discuss, in simple terms, the three main families of membrane bound receptors and the effect of ligand binding.
5. Briefly discuss other ways drugs can act (on carrier proteins, on structural proteins, on nucleic acid binding, on lipid function, on carbohydrate binding)
6. Briefly discuss molecular shape, structural rigidity, structural flexibility, configuration, molecular size
7. Outline the capabilities of molecular modelling and its limitations
8. Describe factors affecting drug receptor interactions down to the functional group level
9. Understand the importance of solvation/desolvation in drug binding
10. Understanding of solutions in terms of solubilisation of drugs
11. Identify where and how lipids contribute to solubility of drugs
12. Identify functional groups that can direct or improve solubility
13. Understand how surfactants or micelles aid water solubility
14. Define the partition coefficient as applied to a biological system
15. Identify components of a biological membrane
16. Understand the roles of different membrane proteins
17. Understand the effect of the blood-brain barrier in drug transport
18. Define how drugs act at membranes and cell walls
19. Define the factors that quantify the response of a drug
20. Understand the difference between chemical and metabolic stability
21. Be able to apply kinetic models to determine drug elimination
22. Factors that require consideration in drug design for targeting tissues
23. Define the term ligand, and understand how ligands combine with metal ions to form complexes.
24. Understand how drug action is affected by metal chelation
25. Factors that contribute to complex stability
26. Understand the principles of HASB
27. Define some of the roles of metalloproteins in biological processes
28. Outline the application of chelating agents in diseases
29. Have an appreciation of pharmaceutical industry in an Australian context

Assessment

End of semester exam: 60%; Two MCQ tutorial tests: 10%; Tutorial assignment:10%; Practical class: 20%