Lec 1 Flashcards
Give the 2 main routes of drug development
COMPOUND > PHYSIOLOGICAL EFFECT > MOLECULAR TARGET MOLECULAR TARGET > COMPOUND > PHYSIOLOGICAL EFFECT
For this compound below give options of its molecular targets
- pi electron ring stacking interactions w/ Phe, Tyr, Trp
Draw the structure of Aspirin and state its mode of action in the body (including its targets etc)
- affects the cyclooxygenase component of Prostaglandin H2 Synthase
- acetylates a crucial Ser residue in the CO AS
- both the acetylated Ser and salicyclic acid product block the hydrophobic tunnel from arachidoic acid (substrate) so there is no prostaglandin synthesis
What is the result of reduced prostaglandin levels?
signalling pathways affected include
- blood clotting
- inflammation
- fever
Draw the mechanism the reaction of Aspiring with the Ser residue in the AS of CO
What are stereoisomers?
compounds that only differ in the 3D arrangement of their atoms
Describe the 2 forms of stereoisomers
What is cis/trans isomerism, you may want to draw a diagram to aid you answer
- cis = higher mass groups are on SAME side as double bond
- trans = vice versa
What are the 3 ways to distinguish chirality and explain each one slightly?
- L/D isomers - D = COORN clockwise
- +/- = direction in which they relflect plane polarised light
- R/S = assigned priority (via atomic numbers) and rotations (when looking from lowest priority group to the chiral C) either clockwise (R) or anticlockwise (S)
Assign R/S chirality to this compound
S
Assign R/S chirality to this compound
