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drug design > drug design 2 > Flashcards

drug design 2 Flashcards

1
Q

what is lead optimisation

A

aims to mamimize the interaction of a drug with its rarget binding site in order to improve activity, electivity and to minimize side affects

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2
Q

what does structure based drug design

A

uses X-ray crystallogrpahy and computer based molecularmodelling to study its binding

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3
Q

how can drug optimaistion be achieved

A
  • variation of sbsituents
    -exentision of structure by isosceles and biosteres
  • simplification of the structure
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4
Q

what si the pharmacetical phase

A

disintergration and dissolution, determiens amount of drug avalible for absorption

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5
Q

what is the pharamkinetic phase

A

ADME, deternmines amount of drug avalaible for action

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6
Q

What is the pharamcodynamic phase

A

interactions with the tissue, dtermines indcution of therpuetic effect, what the drug does to the body

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7
Q

what are examples of enteral routes of administartion

A
  • oral
    -retal
    -vaginal
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8
Q

what is parental routes of admistration

A
  • intravenous, intramuscular, subcutaneous
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9
Q

if it is oral what do you want the drug to be

A

inactive so its activited, if its active liver would inactivate

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10
Q

why should you only take one therapy at a time sometimes

A

the p450 are all occupied

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11
Q

what are dosage form

A
  • lquid formualtuoin
  • semisolid formulations
  • solid formulations
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12
Q

what is the objective of pharmakinics

A

optimisation of avalibilty

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13
Q

what factors influecne how drug reaches its target

A
  • hydrophilic/ hydrophobic character (want slighlty more hydrophobic)
  • ionisatiobn
  • size
    chemical and metabolic properties
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14
Q

what are the partition steps drugs will go through

A
  • elave aqueous extracellualr fluid
  • passing through lipid membrane
  • entering aqueous enviroments before reaching receptor
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15
Q

which enzyme normally breaks down drugs

A

P450

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16
Q

what are the problems relating to metabolsim

A
  • metabolites have different properties to og drug
  • loss of activity
  • more toxic
  • activity of enzyme varies
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17
Q

what is a pharmacophore

A

minium structural requirements to have biological activity

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18
Q

what is the role of structure-activity relationship in drug design

A

changing things like functional groups

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19
Q

what is a drug receprtor

A

Specialised target macromolecule presnet on the cell surface or intracellularly that binds and mediates is pharmacological action

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20
Q

what are the drug targets

A
  • enzymes
  • receptors
  • carrier proteins
    -structural prtoeins
  • nucleic acid
  • lipids
  • carbohydrates
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21
Q

what are agnosists

A

mimic the chemical messsenger

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22
Q

what are antagonist

A
  • bind to receptor
  • dont activate
    block binding
23
Q

what is potentiation

A

a bigger affect than you would have normally got

24
Q

what is the most common membrane bound receptor

A

G- coupled receptors

25
Q

what are the types f interaction betwen drugs and receptors

A
  • ionic
  • h binds
  • van der Waal
    thsi depends on the fucntion groups and the charges
26
Q

what allows receptor interactions

A
  • drugs must have correct binding groups
  • groups must be corrcetly positioned
  • drug needs t be correct size for binding site
27
Q

what factors influence binding and action

A
  • molecular structure
  • isomerism
  • fcuntional groups
  • rigidity
28
Q

what is the pharamacophore

A
  • which part of molecular are importat to biological activity
  • which functional groups are important to bonding to receptors
29
Q

what is pharmakinetic optimisation

A

optimising acess to the target

30
Q

what is the pharamdynamic optimisation

A

optimising target interactions

31
Q

modifciations that affect solubilty

A
  • add ioniazble centre
  • increases polaroaty
    -decreases lipocicity
32
Q

modification to permeabilty

A
  • reduces polarity
  • increase lipophilicty
  • prodrug approaches
33
Q

what would make a drug cross the blood brian barrier

A

pro drug approach
increases lipophoicity

34
Q

what is a pro drug approach

A

putting the drug as one thing and the it acting as something else

35
Q

how many rings has morphone got

A

5

36
Q

how do you make codine out pf moprphine and whats the difference

A

reduction in pain relief to 20%
chnage a free hydroxyl group to CH3

37
Q

how do you have to administer codeine

A

cannot do if injected stright into CNA, instead need to be oral as needs liver

38
Q

what happens whern you remove 6OH and replace with acetyl group

A

get more activity and can pass through to brain at higehr conc as less poalr

38
Q

what happens whern you remove 6OH and replace with acetyl group

A

get more activity and can pass through to brain at higehr conc as less poalr

39
Q

how is diamoprhone (Heriorin) made

A

take phenol OH and alchohol group and put acteyl groups on and improves blood brain barrier

40
Q

what is viutal to the pain releif of morphine

A

nitrogen (ionic bonding)
aramatic ring (van der waals)
phenolic OH (H bond)
the postioning of the drug

41
Q

what are the most common drug targets

A
  • enzyme
  • receptors
42
Q

what does it mean if a drug is charged

A

cant travel across membranes

43
Q

do you want your drug to be slightly hydrophilic or hydrophobic

A

slighty more hydrophobic

44
Q

what do the typess of intercations between the drugs and the receptors depend on

A

fucntional groups

45
Q

what interctaions might a drug have

A
  • ionic
    -ion dipole
    -h bonds
46
Q

what is isomerism

A

same structure but different arrangemennt

47
Q

what is an exmaple of ligand based drug design

A

morphine

48
Q

how do you look at structure active relationships

A

take the lead and change its structure

49
Q

how is codine made from morphone and what is its actitivity

A

the phenolic OH is replaced with methyl ether and activity is 20% of morphine

50
Q

how do you increase the potency of morphone and what can it do

A

swap the 6-OH with 6-acetyl and increases analgesic affects as less polar could potneially move across blood brain barrier

51
Q

how do you make heriorin from morphine

A

swap phenolic oh to acetl group as well as 6 OH tho acetyl group get herorin this can cross blood brian barrier and very hydrophobic

52
Q

what is crucial to analegiscal activity in morphine

A

the nitrogen and ring, the phenol OH and 6-oh

drug design (12 decks)

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