The cell membrane and isosteres, biosteres and polar drugs Flashcards
(18 cards)
In the cell membrane there are phospholipids what are 2 key properties of them
hydrophobic tails and hydrophilic heads
What 4 things are in a cell membrane
phospholipids
cholesterol
inner membrane
outer membrane
Where are hydrophobic amino acids situated in the cell membrane
inside membrane
Where are polar proteins situated
on the surface
What do basic amino acids interact with
-ve phosphate groups of lipid head groups
What does SAR do
links chemical structure to biological activity
What’s the goal of SAR
identify which parts of the molecule are important for activity
help optimise binding and pharmacological properties
Isosteres
same valency , chemical and physical similarities
Bioisosteres
group that can replace another retaining biological activity
What is positive about a bioisostere
drug design reduce toxicity without altering desired effect
What are the 3 changes resulting from bioisosteric replacement
structural (size shape and bonding)
Receptor interactions (lipid or water solubility)
Pharmocokinetics (lipophilicity , pKa and h-bonding )
What are the 3 things in SARS that biological activity influences
H-bonding hydrophobic reactions
electron distribution
Environmental conditions
What are the 2 bioisosteres classification
classical and non-classical
define classical
conserve much of the same structural properties
define non-classical
dependent on specific binding needs of the ligand
What is lipinski rule of 5
Molecular weight less than 500da
more or equal to 5 -hbond donors
more or equal to 10 acceptors
log p is less than 5
2 steps of pinocytosis
drug engulfed by cell membrane and vesicle carries drug across cell
vesicle fuses with membrane to release the drug
What causes the soothing affect in lozenges
the blocking of voltage gated sodium ion channels which usually send pain signals to the brain
