Medicinal Chemistry

Question 1

What are drugs?

Answer 1

Drugs are substances that alter biochemical processes in the body

Question 2

When can a drug be classified as a medicine?

Answer 2

When it has beneficial effects

Question 3

What do medicines contain?

Answer 3

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

Question 4

What must a molecule have to be drug-like?

Answer 4

• 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

Question 5

What do most medicines contain?

Answer 5

A single active ingredient, usually an organic compound

Question 6

What is paracetamol?

Answer 6

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

Question 7

What are prostaglandins?

Answer 7

Substances released in response to illness or injury

Question 8

What does paracetamol do?

Answer 8

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

Question 9

What are some side effects of paracetamol?

Answer 9

• a rash or swelling
• hypotension
• liver and kidney damage

Question 10

What is the goal of medicinal chemists?

Answer 10

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

Question 11

Why must a drug be selective?

Answer 11

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

Question 12

What is a prototype compound called?

Answer 12

the lead compound

Question 13

What happens to analogues of the lead compound ?

Answer 13

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

Question 14

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

Answer 14

Molecular modification

Question 15

Where does cocaine come from?

Answer 15

Leaves of erythroxlon coca

Question 16

What is morphine said to be?

Answer 16

The best analgesic (pain relieving drug)

Question 17

What is codiene made from?

Answer 17

Morphine

Question 18

How is heroin formed?

Answer 18

By diluting morphine with ethanoic anhydride

Question 19

What is often present in illegally produced heroin?

Answer 19

ethanoic acid

Question 20

How did a chemist discover etrophine?

Answer 20

By understanding how morphine binds to the opiate receptor

Question 21

How do we know drugs are safe?

Answer 21

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

Question 22

Who is drug testing overseen by?

Answer 22

The medicines and healthcare products regilatory agency (MHRA)

Question 23

What are biochemical receptors?

Answer 23

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

Question 24

What are receptors?

Answer 24

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

Question 25

What is the binding site?

Answer 25

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

Question 26

What does the active molecule do to the active site?

Answer 26

Triggers a biological response

Question 27

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

Answer 27

Enzymes active site changes slightly

Question 28

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

Answer 28

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

Question 29

How does binding occur?

Answer 29

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

Question 30

What can receptors and drug molecules form?

Answer 30

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

Question 31

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

Answer 31

A hydrogen bond donor

Question 32

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

Answer 32

A hydrogen bond acceptor

Question 33

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

Answer 33

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

Question 34

What is an agonist?

Answer 34

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

Question 35

How does an agonist work?

Answer 35

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

Question 36

What does an antagonist do?

Answer 36

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

Question 37

What is an agonist said to be?

Answer 37

an inhibitor

Question 38

What can be said about penicillins?

Answer 38

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

Question 39

What kind of molecule are penicillins?

Answer 39

Antagonists

Question 40

When is noradrenaline produced?

Answer 40

In response to stress

Question 41

How does phenylephrine work?

Answer 41

Directly on the receptors as an agonist

Question 42

How do amphetamines work?

Answer 42

Indirectly by causing nerve terminals in the body to produce noradrenaline

Question 43

How is the strucural fragment produced?

Answer 43

By overlaying the structures

Question 44

What releases enkephalins?

Answer 44

Nerve cells

Question 45

What do opiates/morphine do?

Answer 45

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)