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4/1/2019 Oxford University Press | Online Resource Centre | Chapter 12

Patrick: An Introduction to Medicinal Chemistry 6e


Chapter 12

Results
You have answered 3 out of 15 questions correctly.
Your percentage score is 20%.
Question 1
What is meant by a lead compound in medicinal chemistry?

Your answer:
a) A drug containing the element lead.
Correct answer:
c) A compound that acts as the starting point for drug design and development.
Feedback:
A lead compound is a compound that acts as the starting point for drug design and development. It may have disadvantages such as low
activity or the presence of side effects, but it acts as a starting point for the development of a better agent.
Page reference: 199

Question 2
Which of the following needs to be established before the search for a lead compound takes place?

Your answer:
a) the pharmacophore
Correct answer:
c) a bioassay
Feedback:
The lead compound has to have some sort of desirable biological activity, and so a bioassay to detect that activity is required. Structure-
activity relationships and the identification of a pharmacophore are stages in the drug design process that come after the discovery of the
lead compound. Patents are taken out at a later stage once potentially useful compounds have been designed and developed.
Page reference: 195-196

Question 3
What is the term used for the automated in vitro testing of large numbers of compounds using genetically modified cells?

Your answer:
a) robotic testing
Correct answer:
b) high throughput screening
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As well as being automated and capable of handling large numbers of compounds, high throughput screening (HTS) can be carried out on
small scale, allowing results to be obtained quickly and efficiently.
Page reference: 196-197

Question 4
Which of the following statements is false with respect to nmr screening to detect drug-target interactions?

Your answer:
a) The procedure relies on small molecules (drugs) having shorter relaxation times than large molecules (targets).
Feedback:
The procedure relies on small molecules (drugs) having longer relaxation times than large molecules (targets). When a small drug binds to
a macromolecular target, it essentially becomes part of that target and the signals for that compound will have shorter relaxation times. If
there is a time delay in measuring the nmr spectrum, the signals for molecules that bind to the protein will disappear from the spectrum.
Page reference: 197

Question 5
BIAcore is a detection system patented by Pharmacia Biosensor to detect a ligand binding to a target. What is the name of the phenomenon
used in this detection procedure?

Your answer:
a) nuclear magnetic resonance
Correct answer:
c) surface plasmon resonance
Feedback:
Nuclear magnetic resonance and electron spin resonance are both forms of spectroscopy. BIAcore makes use of surface plasmon
resonance, which involves the interaction of a reflected wave of plane polarised light with free oscillating electrons called plasmons in a
metal film. Scintillation proximate assay involves the immobilisation of a target molecule on beads coated with a scintillant. A ligand labelled
with 125I binds to the target and the radioisotope interacts with the scintillant to emit light.
Page reference: 195-196

Question 6
There are several sources and methods of discovering new compounds. Which of the following is most likely to lead to the discovery of a
complex structure quite unlike any other previously discovered?

Your answer:
a) combinatorial chemistry
Correct answer:
c) screening plant extracts
Feedback:
There are no preconceived ideas when screening plant extracts for active lead compounds. Some natural products are quite bizarre in
structure!
Combinatorial chemistry involves the synthesis of a large number of compounds using a standard synthetic route, and so the types of
structures that will be synthesised are predictable and belong to a similar family of compounds. Database mining involves the computerised
search of known compounds for particular pharmacophores. Me-too drugs are analogues of an established drug.
Page reference: 199-202

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Question 7
Which source has been particularly fruitful in finding novel antitumour agents such as bryostatins and dolostatins?

Your answer:
c) combinatorial chemistry
Correct answer:
a) marine sources
Feedback:
Marine life such as coral, fish and cyanobacteria have proved useful sources of novel lead compounds having antitumour properties.
Page reference: 200-201

Question 8
Which of the following drugs was not isolated from a natural source?

Your answer:
b) morphine
Correct answer:
c) isoniazid
Feedback:
Isoniazid was synthesised in the laboratory. The other three compounds were derived from natural sources. Quinine was isolated from the
bark of the cinchona tree. Morphine was isolated from the seed pods of poppies. Artemisinin was isolated from a Chinese plant.
Page reference: 199, 203

Question 9
What is the term used for drugs that are similar in structure to a known drug and which are used for the same purpose?

Your answer:
a) 'copycat' drugs
Correct answer:
b) 'me-too' drugs
Feedback:
The terms given in options a), c) and d) are not used in medicinal chemistry.
Page reference: 203

Question 10
Natural products are often used as lead compounds in the design and synthesis of novel drugs. Which of the following general characteristics of
a natural product is most likely to be a disadvantage in synthesising analogues?

Your answer:
b) complexity of structure
Feedback:
Natural products are often complex in structure which makes their synthesis difficult. As a result, the synthesis of analogues can also be
difficult.

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Page reference: 199

Question 11
Which of the following is not an endogenous lead compound?

Your answer:
a) neurotransmitter
Correct answer:
b) alkaloid
Feedback:
Alkaloids are plant natural products containing nitrogen. The other options are endogenous compounds in the body.
Page reference: 199, 204-206

Question 12
What is the term used for small molecules that bind to different regions of a binding site?

Your answer:
a) epimers
Correct answer:
d) epitopes
Feedback:
The correct answer is epitopes. Epimers are diastereomers differing in their configuration at one asymmetric centre. Isomers are different
structures having the same molecular formula. Isotopes are elements which have the same number of protons and electrons, but a different
number of neutrons.
Page reference: 209-210

Question 13
Which of the following statements is not true of herbal medicines?

Your answer:
a) Herbal medicines may contain a range of active principles acting together to produce a beneficial effect.
Correct answer:
b) Herbal medicines have no side effects compared to conventional medicines.
Feedback:
There is no reason why herbal medicines should be free of side effects. They contain active components which will vary in their selectivity
for their targets. Some will produce more side effects than others.
Page reference: 212-213

Question 14

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The following diagram illustrates the detection system known as surface plasmon resonance. What is represented by D?

Your answer:
a) the evanescent wave
Feedback:
D is the evanescent wave which interacts with free oscillating electrons called plasmons in the metal film, when the angle of incidence (α) is
correct. Symbol A represents a receptor which is covalently linked to the dextran matrix, and which will bind ligands present in the buffer
flow. B is monochromatic plane-polarised light. C is the flow of buffer solution.
Page reference: 197-198

Question 15
Which of the following is not an endogenous compound?

Your answer:
a) dopamine
Correct answer:
d) desipramine
Feedback:
Endogenous compounds are any compounds occurring naturally in the body. Desipramine is a synthetic drug and is not an endogenous
compound.
Page reference:
204-206

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