Chapter 7 Multiple Choice Questions

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. Which of the following statements best describes a lead compound?

A compound that contains the element lead. correct incorrect

A compound from the research laboratory that is chosen to go forward for preclinical and clinical trials correct incorrect

A molecule that shows some activity or property of interest and serves as the starting point for the development of a drug. correct incorrect

The first compound of a structural class of compounds to reach the market. correct incorrect

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. Which of the following statements best describes chemical space?

A measure of the 3-dimensional shape and size of a chemical structure. correct incorrect

The area required for the construction of a pharmaceutical production plant correct incorrect

The accessibility of a functional group to a reagent during a reaction. correct incorrect

A term used to describe structural diversity and the possible number of structures that could be synthesised correct incorrect

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. Identify the kind of interactions that are typically involved in binding a drug to the binding site of a protein.

predominantly van der Waals interactions correct incorrect

predominantly ionic bonds correct incorrect

predominantly hydrogen bonds correct incorrect

a combination of all of the above correct incorrect

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. Identify which of the following amino acids has a side chain that may be important in binding a drug by ionic bonding.

aspartate correct incorrect

glycine correct incorrect

serine correct incorrect

valine correct incorrect

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. What disadvantage is there in using linear peptide scaffolds in chemical libraries aimed at finding lead compounds?

It is difficult to synthesise the compounds correct incorrect

There is a lack of suitable reagents correct incorrect

Active compounds are likely to have poor pharmacokinetic properties correct incorrect

Active compounds are likely to have poor pharmacodynamic properties. correct incorrect

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. What is a peptidomimetic?

A peptide lead compound that mimics the action of an endogenous neurotransmitter or hormone. correct incorrect

A structure that has been designed to mimic a peptide lead compound in binding to a target binding site, but has better pharmacokinetic properties. correct incorrect

A structure that has the ability to bind to peptides or proteins. correct incorrect

A peptide that consists of unnatural amino acids rather than natural amino acids. correct incorrect

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. Which statement is false when comparing a drug having a cyclic scaffold with one having a linear scaffold?

There is more chance of a drug with a rigid scaffold finding an active conformation for a particular binding site correct incorrect

A drug with a cyclic scaffold is likely to have stronger interactions with a target binding site. correct incorrect

A drug with a cyclic scaffold has fewer conformations correct incorrect

There is less chance of a drug with a cyclic scaffold binding to a target binding site. correct incorrect

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. Which of the following best identifies one of the aims of diversity orientated synthesis?

To develop chemical libraries involving simple heteroaromatic scaffolds correct incorrect

To develop chemical libraries involving 'globular' cyclic scaffolds correct incorrect

To develop chemical libraries using a diverse range of starting materials correct incorrect

To develop chemical libraries using multi-step syntheses. correct incorrect

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. Fragment-based lead discovery involves studying how a series of small molecules interact with a target binding site. What term is given to these molecules?

Isotopes correct incorrect

Isomers correct incorrect

Aptamers correct incorrect

Epitopes correct incorrect

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. Which of the following properties is not desirable in a click reaction?

Rapid rate of reaction correct incorrect

Water as a feasible solvent correct incorrect

Low thermodynamic driving force correct incorrect

Chemoselective for a narrow range of functional groups correct incorrect