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Flashcards in Optimising leads Deck (16):
1

Adding alkyl groups to a molecule will make it more hydrophobic. True or false?

True

2

What is steric shielding used for?

To alter chemical and metabolic stability

3

Steric shielding hinders attacks by nucleophiles or enzymes. True or false?

True

4

Changing an ester to an amide decreases stability. True or false?

False - increases

5

What is the purpose of introducing medically susceptible groups to a molecule?

To decrease drug's lifetime

6

Esters are used to mask polar and ionisable COOH. True or false?

True

7

Levodopa is decarboxylated in the cell to dopamine. True or false?

True

8

Why can't dopamine cross the BBB?

Because it is too polar

9

Levodopa is a prodrug for dopamine. True or false?

True

10

Enalapril is a prodrug for enalaprilit. True or false?

True

11

What effect does masking polar groups have?

Reduced rate of excretion

12

Azathioprine is a prodrug for 6-mercaptopurine. True or false?

True - polar group on azathioprine is masked to increase lifetime of drug and prevent it from being excreted as quickly

13

Valium (diazepam) is a prodrug for nordiazepam. True or false?

True

14

What are prodrugs used for?

For membrane permeability or to prolong activity of drug, mask toxicity and side effects, mask taste

15

Aspirin is used as a prodrug for salicylic acid. Why?

Because the phenol on salicylic acid causes stomach ulcers so it is masked by an ester

16

Palmitate ester is a prodrug for chloramphenicol. True or false?

True - used to reduce hydrophobicity