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Question 1

Combinatorial chemistry can be useful at various stages of the drug design / development process. Which of the following is not such a stage?

a) Finding a lead compound.

b) Optimising a lead compound.

c) Structure determination of the lead compound.

d) Structure-activity relationships of the lead compound.

Question 2

What is meant by a linker or an anchor?

a) The bond which links a molecule to a solid support.

b) A reactive functional group on the solid support which allows a molecule to be attached to the solid support.

c) A molecular unit which is attached to the solid support and which contains a reactive functional group that allows attachment of a starting material.

d) The functional group on the starting material which is used to attach the molecule to the solid support.

Question 3

Which of the following statements regarding linkers is false?

a) The link between the molecule and the solid support must be stable to the reaction conditions used in the synthesis.

b) The link between the molecule and the solid support must be easily cleaved under specific conditions.

c) The choice of linker used depends on the functional groups available on the first molecule to be attached.

d) The linker must be on the outer surface of the resin bead if a molecule is to become attached to it.

Question 4

The following structure is a protecting group used in peptide synthesis.

What conditions are used to release the protecting group during a solid phase peptide synthesis?

a) Hydrofluoric acid

b) Piperidine

c) Hydrogen and a palladium charcoal catalyst

d) Trifluoroacetic acid

Question 5

The following structure is a protecting group used in peptide synthesis.

What is the name of the protecting group?

a) Tertiary-butyl

b) Benzyloxycarbonyl

c) Benzyl

d) 9-fluorenylmethoxycarbonyl

Question 6

The following structure is a protecting group used in peptide synthesis.

What conditions are used to release the protecting group during a solid phase peptide synthesis?

a) Hydrofluoric acid

b) Piperidine

c) Hydrogen and a palladium charcoal catalyst

d) Trifluoroacetic acid

Question 7

The following structure is a protecting group used in peptide synthesis.

What is the name of the protecting group?

a) Tertiary-butyloxycarbonyl

b) Benzyloxycarbonyl

c) Benzyl

d) 9-fluorenylmethoxycarbonyl

Question 8

The following structure is a protecting group used in peptide synthesis.

What conditions are used to release the protecting group during a solid phase peptide synthesis?

a) Hydrofluoric acid

b) Piperidine

c) Acetic acid

d) Trifluoroacetic acid

Question 9

Which of the following statements is true?

a) Parallel combinatorial synthesis involves the synthesis of a large number of compounds using the same reaction sequence, where there is a mixture of compounds in each reaction vessel.

b) Parallel combinatorial synthesis involves the synthesis of a large number of compounds using the same reaction sequence, where there is a different, single compound formed in each reaction vessel.

c) Mixed combinatorial synthesis involves the synthesis of a large number of compounds using a variety of different synthetic routes to produce a mixture of compounds in each reaction vessel.

d) A parallel combinatorial synthesis carried out in a specified number of vessels will produce more compounds than a mixed combinatorial synthesis.

Question 10

The following structure is a protecting group used in peptide synthesis.

What functional group does it protect?

a) Carboxylic acid

b) Amine

c) Alcohol

d) Phenol

Question 11

The following structure is a protecting group used in peptide synthesis.

What is the name of the technique which involves the use of this protecting group in combinatorial synthesis?

a) Mix and split

b) Photolithography

c) Parallel synthesis

d) Photosynthesis

Question 12

Dynamic combinatorial chemistry is an alternative method of producing compounds other than the classic mix and split method. Which of the following statements is true about dynamic combinatorial chemistry?

a) The target should be absent from the reaction flask.

b) There is no scope for amplification.

c) It is necessary to 'freeze' the equilibrium reaction to identify active compounds.

d) The reactions involved should be irreversible.

Question 13

What is meant by a scaffold?

a) The lead compound.

b) The carbon skeleton of a compound.

c) The core structure of a molecule that is common to a series of compounds.

d) The pharmacophore.

Question 14

What is meant by a privileged scaffold?

a) A scaffold that is present in a wide range of drugs with different activities.

b) A scaffold that is easily synthesised.

c) A scaffold that is patented.

d) A scaffold that is free of side effects.

Question 15

Which of the following statements is true with respect to scaffolds?

a) The scaffold should be large to allow a wide variation of substituents.

b) The scaffold should not be capable of forming any binding interactions with the target.

c) Substituents should be localised at particular regions of the scaffold.

d) Similar functional groups on the scaffold should be capable of being varied independently of each other.

Oxford University Press, Online Resource Centre, Chapter 16.

Chapter 16

Instructions

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Question 10

Question 11

Question 12

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Question 15