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Patrick: An Introduction to Medicinal Chemistry 4e

Chapter 20

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Question 1

What are the two main targets currently used in anti-HIV therapy?

Question 2

Which of the following enzymes is responsible for processing HIV proteins during the production of new viruses?

Question 3

Which of the following statements is true regarding the following structure (nevirapine)?
Figure 1

Question 4

Which of the following statements is true for non-nucleoside reverse transcriptase inhibitors?

Question 5

The protease enzyme in HIV has two important, identical amino acids involved in the catalytic mechanism which leads to peptide bond hydrolysis. What are the two amino acids?

Question 6

The HIV protease enzyme is symmetrical, whereas mammalian proteases are not. What significance might this have?

Question 7

The following structure (saquinavir) is a protease inhibitor.
Figure 2
The region marked in blue is a hydroxyethylamine moiety. What does this moiety represent?

Question 8

The following structure (saquinavir) is a protease inhibitor.
Figure 2
The decahydroisoquinoline ring system in the protease inhibitor shown above was used to replace an amino acid residue that is present in the lead compound used in the development of saquinavir. Which amino acid was replaced?

Question 9

The following structure (saquinavir) is a protease inhibitor.
Figure 2
Into which binding subsite of the protease enzyme's active site does the quinoline ring system fit?

Question 10

The following structure (ritonavir) is a protease inhibitor.
Figure 3
What feature of the protease enzyme was the inspiration for the design of this particular structure?

Question 11

Which of the following protease inhibitors was developed by a hybridisation strategy?

Question 12

The following protease inhibitor (palinavir) illustrates an extension strategy involving the group shown in blue.
Figure 4
Which subsites are occupied by the extended residue?

Question 13

An enzyme carried by the flu virus catalyses the following reaction. Which enzyme is it?
Figure 5

Question 14

Which of the following statements is false regarding the characteristics of a good protein target for antiviral drugs?

Question 15

Which of the following antiviral drugs does not result in the eventual appearance of aciclovir triphosphate in virally infected cells?
Figure 6