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Russel's medicinal chemistry > Medicinal chemistry 2 - Sources of lead compounds > Flashcards

Medicinal chemistry 2 - Sources of lead compounds Flashcards

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1
Q

What are bioassays used for?

A
  • used to test drug candidates

- Used in choosing the right bioassay

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2
Q

Whata re the four considerations when choosing the right bioassay?

A
  1. Simple
  2. Quick
  3. Relevant
  4. In vitro or in vivo
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3
Q

Give examples of targets used in vitro studies?

A
  • Isolated cells
  • Tissue
  • Enzyme
  • Receptor
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4
Q

In vivo involves animal model testing. TRUE OR FALSE?

A

TRUE

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5
Q

What are the advantages of in vitro testing?

A
  1. Inexpensive
  2. Easier to perform
  3. Less controversial
  4. Automated (often)
  5. No barrier concerns
  6. No metabolic enzymes to contend with
  7. Cell environment can be easily controlled
  8. Can measure potency and efficacy
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6
Q

What is potency?

A
  • Amount of drug required to achieve a defined biological effect
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7
Q

What is efficacy?

A
  • Measure of how effectively an agonist activates a receptor
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8
Q

Drug can have high affinity for a receptor but a low efficacy. TRUE OR FALSE?

A

TRUE

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9
Q

What are the advantages of in vivo testing?

A
  • Important for monitoring pharmacological activity - pharmacodynamics
  • Important for monitoring pharmacokinetics (ADME)
  • Allows identification of activity at undesired target
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10
Q

What is the desired scenario for in vivo testing?

A

-Good activity at the desired target and minimum activity at others

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11
Q

What are the disadvantages of in vivo testing?

A
  • Slow progress
  • Animal suffering
  • Pharmacokinetics - results may be misleading
  • Different results in different animal species
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12
Q

Provide an example of different results in different animal species?

A
  • Penicillin methyl ester is hydrolysed in mice and rats but not in rabbits, dogs and humans
  • Thalidomide - Teratogenic in rabbits and humans not in mice
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13
Q

In vitro determines whether drug interacts with target and in vivo tests pharmacokinetics properties. TRUE OR FALSE?

A

TRUE

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14
Q

In vivo identifies problems which cannot be picked up in vitro. TRUE OR FALSE?

A

TRUE

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15
Q

In test validaty - automation and easy detection are highly desirable. TRUE OR FALSE?

A

TRUE

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16
Q

What does HTS stand for?

A

High throughput screening

17
Q

What is robotics?

A

they are auntomated testing of many compounds (compound library) on a large number of targets

18
Q

What happens once drug type, drug target and the testing system have been determined?

A
  • We need to establish a lead compound
19
Q

What is a lead compound?

A
  • A compound showing the desired pharmaceutical activity (a starting point)
20
Q

Name a few sources in which lead compounds can originate from?

A
  • Natural product screening
  • Medical folklore
  • Screening compound libraries
  • Existing drugs “ me too drugs”
  • Natures ligands/ modulators
  • NMR data
21
Q

Most biologically active natural products are secondary metabolites. TRUE OR FALSE?

A

TRUE

22
Q

Natural product screening tend to be complex structures and therefore novel. TRUE OR FALSE?

A

TRUE

23
Q

what pools can we take from for Natural product screening?

A
  • Plant kingdom
  • Microbial world
  • Marine world
  • Animals
  • Toxins
24
Q

Give an example of medical folklore drugs?

A
  • Morphine
  • Reserpine
  • Salicin
  • Quinine
25
Q

Whata re compound libraries?

A
  • Coumpounds synthesised but not made it as far as the market place, therefore stored and used against new tragets as they appear on the off chance that they are beneficial
26
Q

Storage of compound libraries are usuallu catalogued based on functionality that is present and will also include compound intermediates on route to a more complex target molecule. TRUE OR FALSE?

A

TRUE

27
Q

Give an example of a compound library screening?

A
  • Antitubercular agent
28
Q

Isoniazid is the synthetic intermediate for TB but more active than the target compound. TRUE OR FALSE?

A

TRUE

29
Q

What are me too drugs?

A
  • Using drugs from competing companies as a starting point and modifying the structure to avoid patent restrictions, with approved therapeutic properties
30
Q

Give an example of a me too drug and give its therapeutic use?

A
  • Captopril

- It is an antihypertensive agent

Russel's medicinal chemistry (3 decks)

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