CHE 235: Medicinal Chemistry
Final Exam Questions

Why does a diabetic patient take insulin?

  1. to increase blood glucose levels
  2. to increase glucose uptake by muscle cells
  3. to repair islet beta cells
  4. to increase glucose uptake by brain cells
  5. more than one of the above
  6. none of the above

What is the mechanism of amyloid plaque formation in AD?

Beta-amyloid protein is cleaved from Amyloid Precursor Protein. Conformational change makes protein fragment insoluble and it is exported outside the cell. Protein sheets stack and aggregate, forming threatening plaques.

Why is AChE inhibition a goal of drug designers for treatment of AD?

Because increased acetylcholine levels in the brain increase cognitive function, and also AChE can bind to beta-amyloid molecules causing the dangerous conformational shift that leads to amyloid plaque formation.

What are two benefits that Voets et al. identified in looking at Aldosterone synthase inhibitors that weren't present when looking at Aldosterone antagonists?

  1. Fewer side effects on the endocrine system
  2. More selectivity
  3. Inhibition is more effective than receptor interference

In conducting the molecular modeling study of Aldosterone synthast inhibitors, researchers found which bond formed in the binding site to be the most important?

The Fe-N bond from the heme group to the inhibitor.

What are some of the steps in HIV-1 infection mechanism that could be targets for anti-HIV drugs and how will it function?

What differences between oral and injectables lead to favorable PK/PD properties for orals?

Orals are structurally more rigid and less polar. Also oral drugs tend to have lower molecular weight which makes them more permeable and easily absorbed.

Discuss the variation of oral drugs physical properties with respect to launch date.

Although researchers found that the drug targets can vary dramatically over time, mean physical properties are remarkably consistent.

What are siderophores and what role do they play in bacterial cells?

Low molecular weight molecules that are released by the cell to aid in the acquisition of iron by the cell.

Why is it important to research how to inhibit the production of siderophores in Mycobacterium tuberculosis?

Allows for a new pathway to inhibit the growth of bacterial that are resistant to first line drugs currently on the market.

What structural characteristic was the most determinant factor in the anti-carcinogenic activity of phenolic acids?

  1. Saturated carbon side chain
  2. Length of carbon side chain
  3. Number of hydroxyl substituents on the ring
  4. Carboxylic acid

Which is the malaria parasite that causes the most deaths?

  1. Plasmodium vivax
  2. Plasmodium malariae
  3. Plasmodium ovale
  4. Plasmodium falciparum
  5. none of the above

What are caspases?

Caspases are cysteinyl-aspartate specific proteases

What is the main caspase involved in apoptosis?

Caspase 3

What is apoptosis?

programmed cell death

In the study of orexin activity, what is measured to determine the funciton of each ligand/analogue?

intracellular calcium levels

For both orexin A and orexin B, which area of the peptide was found to be most important for ligand/receptor binding and activity?

the alpha helix near the C-terminal end of the peptide

What does RSV stand for?

  1. Replicating Simian Virus
  2. Respiratory Syncytial Virus
  3. Respiratory Simian virus
  4. RNA Syncytical Virus

What is a 1,4-benzodiazepene?

  1. a benzodiazepene that interacts with its target at the 1,4 positions
  2. a benzodiazepene with subsituents located in the 1,4 positions
  3. a benzodiazepene that with pharmacophores in the 1,4 positions
  4. a benzodiazepene with core nitrogens located in the 1,4 positions

Benodiazepenes exert their antiviral acitvity against RSV by:

  1. Inactivating the N-protein, preventing the viral replication
  2. Inactivating the F-protein, preventing viral fusion
  3. Inactivating viral RNA-polymerase
  4. Activing a cellular viral RNAse