Lec 1 LOs

Question 1

how do you modulate biological activity of the drug?

Answer 1

1. binding to the receptor
2. moving to the location where the receptor is present

Question 2

what is a drug?

Answer 2

a drug is any substance that brings a change in biologic function through its chemical actions

Question 3

how are structure and activity correlated?

Answer 3

structure determines activity
- the properties of the drugs depend on the chemical constituents of the molecule
- when you modify the structure, you change the property
- when you examine the structure, you can predict the properties

Question 4

what is a pharmacophore?

Answer 4

drugs that bind to the same target that share a similar structural motif

Question 5

what is the structural motif used for?

Answer 5

it is responsible for binding to the receptor

Question 6

what do the other parts of the drugs do?

Answer 6

they are still affecting drug properties such as agonism, solubility, membrane crossing, etc.

Question 7

what are the chemical properties of the drugs that can be deduced from the structure?

Answer 7

1. size
2. ionization
3. solubility
4. hydrophobicity
5. stereochemistry

Question 8

what are the chemical properties of the drugs that affect their biological activity?

Answer 8

1. membrane permeability
2. excretion
3. metabolism
4. target binding