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Question 1

What is meant by a lead compound in medicinal chemistry?

a) A drug containing the element lead.

b) A leading drug in a particular area of medicine.

c) A compound that acts as the starting point for drug design and development.

d) A drug which is normally the first to be prescribed for a particular ailment.

Question 2

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

a) The pharmacophore.

b) Structure-activity relationships.

c) A bioassay.

d) Patents.

Question 3

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

a) robotic testing

b) high throughput screening

c) multiscreening

d) nanotechnology

Question 4

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

a) The procedure relies on small molecules (drugs) having shorter relaxation times than large molecules (targets).

b) The procedure can be used on mixtures of compounds.

c) The method can detect weak binding.

d) The method can identify small molecules binding to different regions of the same binding site.

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?

a) nuclear magnetic resonance

b) electron spin resonance

c) surface plasmon resonance

d) scintillation proximate assay

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?

a) Combinatorial chemistry.

b) Database mining.

c) Screening plant extracts.

d) Me too drugs.

Question 7

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

a) marine sources

b) venoms and toxins

c) combinatorial chemistry

d) animals

Question 8

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

a) quinine

b) morphine

c) isoniazid

d) artemisinin

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?

a) 'copycat' drugs

b) 'me-too' drugs

c) 'derivative' drugs

d) 'analogue' drugs

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?

a) novelty of structure

b) complexity of structure

c) level of activity

d) availability

Question 11

Which of the following is not an endogenous lead compound?

a) neurotransmitter

b) alkaloid

c) hormone

d) modulator

Question 12

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

a) epimers

b) isomers

c) isotopes

d) epitopes

Question 13

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

a) Herbal medicines may contain a range of active principles acting together to produce a beneficial effect.

b) Herbal medicines have no side effects compared to conventional medicines.

c) It is more difficult to receive an overdose of an active drug if it is present in a herbal medicine rather than as a pure medicine.

d) Certain compounds in herbal medicines may enhance the activity of the active principle.

Question 14

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

a) The evanescent wave.

b) Monochromatic plane-polarised light.

c) The receptor.

d) The flow of buffer solution.

Question 15

Which of the following is not an endogenous compound?

a) dopamine

b) endorphins

c) noradrenaline

d) desipramine

Oxford University Press, Online Resource Centre, Chapter 12.

Chapter 12

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