5

Question 1

what is SAR

Answer 1

• discerning what part of the molecule is responsible for activity both in vivo and vitro

Question 2

what is in vitro activity

Answer 2

give clues to whether a drug is active against a target like a enzyme or receptor

Question 3

what is in vivo activity

Answer 3

gives additional info concerning the transport of the drug to the site of action and its metabolism

Question 4

3 steps of SAR

Answer 4

1. systematically change structure of pharmacophore
2. test activity of the compound each time
3. use optimised drug

Question 5

what is a pharmacophore

Answer 5

• is responsible for the molecules biological activity

Question 6

what can changing non-pharmacophore do

Answer 6

changing the non-pharmacophore can improve properties

Question 7

what is rational data

Answer 7

use data from similar molecule as a starting point

Question 8

what is homologation

Answer 8

the systematic increase or decrease of a chain or ring size by addition or subtraction of a standard unit

Question 9

what does a bell shaped curve mean for activity and why

Answer 9

increases activity as increase lipophilicity means increases penetration through cell membrane
decreased activity as solubility is reduced so distribution of drug through aq phase is ineffective

Question 10

apparent continuous increase meaning and how to fix

Answer 10

• need to continue as not complete
• need to extend the hydrocarbon chain on molecule
• continue until you maximum activity and see a plateau

Question 11

abnormal curves meaning

Answer 11

• flexibility of longer gain still allows the compound to fold in a conformation suitable for binding
• however it will not increase to the activity to the original peak

Question 12

serrated variation meaning

Answer 12

• depends if the number of carbons is odd or even
• normally with enzymes as enzymes can more easily bind/metabolize odd or even chains thus favour one of other

Question 13

physical and 2 biological reason for serrated variation

Answer 13

the energy for the chain to fold into the correct conformation of binding can vary with odd or even chain number

• metabolic degradation of a compound or urinary excretion

Question 14

what is a conjunctive and disconjunctive apporach

Answer 14

• conjunctive approach - making a ring
• disjunctive approach - break ring in a diff positions to give chain