Lecture 3

Question 1

Define pro-drug

Answer 1

Compounds that are inactive until activated by metabolism

Question 2

Name examples of pro-drugs

Answer 2

Heroin, oseltamivir, bambuterol, clopidogrel

Question 3

Define soft-drug

Answer 3

Active species that are deactivated by metabolism

Question 4

Why use soft-drug design?

Answer 4

To reduce the duration of action
Reduce side effects/toxicity by limiting how broadly distributed the drug is
By having predictable metabolism to inactive species too reduce the risk of metabolism with varying biological activities

Question 5

Define isostere

Answer 5

Functional groups with similar electronic and steric properties resulting in similar biological activity