LECTURE 1

Question 1

Define pharmacophore

Answer 1

The similar structural motif that is shared by drugs that bind to the same target, which is responsible for binding to the receptor

Question 2

Define the structure-activity relationship

Answer 2

“The properties of a drug depend on the chemical constituents of the molecule”
– The structure of the drug influences the activity of the drug

Question 3

What are the implications of the structure-activity relationship?

Answer 3

By modifying the structure, one can change the drug properties
By examining the structure, one can predict the drug properties

Question 4

List the chemical properties of drugs that can be deduced from the structure

Answer 4

• How tightly a drug interacts with the target
  Target binding
• How soluble a drug is in water
• How well a drug crosses the biological membranes
  Membrane permeability
• How fast a drug is degraded in the body
  Metabolism
  Excretion

Question 5

List the key chemical properties of drugs that affect their biological activities

Answer 5

• Size
• Ionization
• Solubility
• Hydrophobicity
• Stereochemistry