Flashcards in Optimising leads Deck (16):
Adding alkyl groups to a molecule will make it more hydrophobic. True or false?
What is steric shielding used for?
To alter chemical and metabolic stability
Steric shielding hinders attacks by nucleophiles or enzymes. True or false?
Changing an ester to an amide decreases stability. True or false?
False - increases
What is the purpose of introducing medically susceptible groups to a molecule?
To decrease drug's lifetime
Esters are used to mask polar and ionisable COOH. True or false?
Levodopa is decarboxylated in the cell to dopamine. True or false?
Why can't dopamine cross the BBB?
Because it is too polar
Levodopa is a prodrug for dopamine. True or false?
Enalapril is a prodrug for enalaprilit. True or false?
What effect does masking polar groups have?
Reduced rate of excretion
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
Valium (diazepam) is a prodrug for nordiazepam. True or false?
What are prodrugs used for?
For membrane permeability or to prolong activity of drug, mask toxicity and side effects, mask taste
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