Medicinal Chemistry Flashcards

1
Q

What are drugs?

A

Drugs are substances that alter biochemical processes in the body

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2
Q

When can a drug be classified as a medicine?

A

When it has beneficial effects

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3
Q

What do medicines contain?

A

Medicines usually contain the active ingredient (drug) and other ingredients such as fillers to add bulk or sweetness to improve the taste

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4
Q

What must a molecule have to be drug-like?

A
  • no more than 5 hydrogen bond donors
  • no more than 10 hydrogen bond acceptors
  • a molecular weight under 500 amu
  • An octanol/water partition coefficient log p no more than 5
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5
Q

What do most medicines contain?

A

A single active ingredient, usually an organic compound

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6
Q

What is paracetamol?

A

Paracetamol works as a painkiller by affecting chemicals in the body called prostaglandins

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7
Q

What are prostaglandins?

A

Substances released in response to illness or injury

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8
Q

What does paracetamol do?

A

Blocks the production of prostaglandins, making the body less aware of the pain or injury

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9
Q

What are some side effects of paracetamol?

A
  • a rash or swelling
  • hypotension
  • liver and kidney damage
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10
Q

What is the goal of medicinal chemists?

A

To find compounds that have potent effects on given diseases with minimum side effects

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11
Q

Why must a drug be selective?

A

A drug must be selective , it must be transported to the correct cells in the body and must react in the selected cell

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12
Q

What is a prototype compound called?

A

the lead compound

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13
Q

What happens to analogues of the lead compound ?

A

They are synthesised to try and improve the therapeutic properties or reduce the side effects

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14
Q

What is the name given to changing the functional groups and structure?

A

Molecular modification

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15
Q

Where does cocaine come from?

A

Leaves of erythroxlon coca

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16
Q

What is morphine said to be?

A

The best analgesic (pain relieving drug)

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17
Q

What is codiene made from?

A

Morphine

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18
Q

How is heroin formed?

A

By diluting morphine with ethanoic anhydride

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19
Q

What is often present in illegally produced heroin?

A

ethanoic acid

20
Q

How did a chemist discover etrophine?

A

By understanding how morphine binds to the opiate receptor

21
Q

How do we know drugs are safe?

A
  • drug testing
  • pre-clinical trials
  • clinical trial exception applications
  • phase 1 clinical trial
22
Q

Who is drug testing overseen by?

A

The medicines and healthcare products regilatory agency (MHRA)

23
Q

What are biochemical receptors?

A

Large protein molecules that can be activated by the binding of a molecule or drug

24
Q

What are receptors?

A

usually protein molecules on the surface of cells, or enzymes that catalyse chemical reactions within a cell

25
Q

What is the binding site?

A

A hollow or cleft which the messenger can fit and bind to

26
Q

What does the active molecule do to the active site?

A

Triggers a biological response

27
Q

What does the active site do to allow the substrate to better fit?

A

Enzymes active site changes slightly

28
Q

What happens when the active compound binds to the active site?

A

It inhibits or blocks the enzyme from catalysing the reaction of the substrates

29
Q

How does binding occur?

A

As a result of noncovalent interactions between the receptor and the drug molecules

30
Q

What can receptors and drug molecules form?

A

Van der Waal’s forces when they are brought close together

31
Q

What is a group that provides a hydrogen bond said to be?

A

A hydrogen bond donor

32
Q

What is a group that provides and oxygen or nitrogen lone pair said to be?

A

A hydrogen bond acceptor

33
Q

What are the two things a drug can do after an attachment to a receptor site?

A

It can either initiate a response or prevent a response from occuring

34
Q

What is an agonist?

A

A drug which produces a response similar to the body’s natural response

35
Q

How does an agonist work?

A

They interact by binding to the receptor site and competing with the natural compound

36
Q

What does an antagonist do?

A

An antagonist drug interacts with the receptor site and produces no response but prevents the action of the body’s natural active compound

37
Q

What is an agonist said to be?

A

an inhibitor

38
Q

What can be said about penicillins?

A

They bind to proteins in the cell walls of bacteria and inhibit bacteria cell wall synthesis

39
Q

What kind of molecule are penicillins?

A

Antagonists

40
Q

When is noradrenaline produced?

A

In response to stress

41
Q

How does phenylephrine work?

A

Directly on the receptors as an agonist

42
Q

How do amphetamines work?

A

Indirectly by causing nerve terminals in the body to produce noradrenaline

43
Q

How is the strucural fragment produced?

A

By overlaying the structures

44
Q

What releases enkephalins?

A

Nerve cells

45
Q

What do opiates/morphine do?

A

They bind to the receptor in a way that the enzymes can’t remove them as a result of relieving pain (pain is still there, just not registered)