Med Chem Respiratory

Question 1

Structure of acetylcholine

Answer 1

• quaternary nitrogen

- ester group (the non double bonded O is very important feature for activity)

Question 2

How is muscarine similar to acetylcholine?

Answer 2

• quaternary nitrogen
• two Cs between N and O

side note: distance from N to O is 3.8 angstroms

Question 3

Mechanism of action of Theophylline

Answer 3

Competitive nonselective phosphodiesterase inhibitor
- inhibits TNFalpha and leukotriene
- decrease inflammation
BUT
has narrow therapeutic index and interacts with many drugs

Question 4

Roflumilast: what enzyme does it block and what are the major side effects?

Answer 4

Blocks PDE-4 -> antiinflammatory
Causes lots of crap
- diarrhoea, nausea, headache, insomnia, etc.

Question 5

Structure of noradrenaline and adrenaline

Answer 5

• catecholamines

Question 6

What is the purpose of/define a bioisoestere

Answer 6

A biologically similar substituent. One bioisoestere is replaced with another to enhance desired properties of a compound without making significant changes in chemical structure.