Chem Basis ACEIs and ARBs 2

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  1. What is the Pharmacophore for Enalapril analogs?
  2. The carboxylic terminal of the proline of Enalapril Analogs is essential for what?
    Binding to the cationic site
  3. What part of the Enalapril analog pharamcophore is essential for binding to the zinc binding site?
    Second carboxylic group in the free form
  4. What is the ACEI Phosphorus containing analog Pharmacophore?
    Phosphinylacetyl proline
  5. What is the carboxylic terminal of proline is essential for in Phosphorus containing analog?
    binding to the cationic site
  6. What is the ionized –OH of the phosphinyl group of the Phosphorus containing analog essential for?
    Binding to the zinc binding site
  7. Most ARBs have what pharamcophore?
    1-N-benzyl 2-butyl Imidazole
  8. What type of substituents of ARBs enhance binding to the AT1 receptor?
    Acidic groups and the R group
  9. What are the three key features of the ACE active sites?
    Cationic site, Postive Zinc site and Carbonyl site
  10. What type of bond usually form at at the Carbonyl site of the ACE binding site?
  11. Therefore, ACE cleaves how many amino acids from its substrate to produce Ag-II?
  12. Why was succinic acid added to Proline to create ACEIs?
    To extend the molecule between the Zinc and cationic binding sites
  13. The addition of a methyl group at the C2 of succinic acid of the ACEI Pharmacophore has what effect on the molecule?
    Considerable increase in the inhibitory activity
  14. Increasing the length of the side chain by adding another methyl to succinic acid (forms glutamic acid) had what effect on the ACEI pharamcophore?
    Did not enhance the activity
  15. The optimal distance for the ACEI pharamcophore should not exceed ________ atoms.
  16. What are the major disadvantages of captopril analogs?
    Low potency, taste disturbances, allergic reactions and short DOA
  17. What R1 substituent of the Enalapril analog pharamcophore is optimal for activity and in what configuration?
    R1 = phenyl ethyl group in the S-configuration
  18. What does the optimal activity of a phenyl ethyl group at the R1 position of the Enalapril analog Pharmacophore indicate about the auxiliary binding site next to the zinc binding site?
    Hydrophobic/Van der Waal binding at this site
  19. Enalapril or Catapril analogs have higher affinity to ACE and are more potent?
    Enalapril analogs
  20. How often is Lisinopril dosed?
    Once a day
  21. What is the main difference between the Pharmacophore for enalapril/catapril analogs and Phosphorous containing analogs?
    The zinc binding site has been modified to a phosphorous containing group (O=P-OH, phosphinyl) and alanine has been replaced with Acetic acid
  22. The acidic group on ARBs miminc what part of Angiotensin II?
    Tyr4 phenol or the Asp1 carboxylate
  23. What can the acidic group be on an ARB?
    Carboxylic acid, a Phenyl tetrazole or a Phenyl carboxylate
  24. (True/False) Taste disturbances and allergic reactions are often associated with the Mercapto group of ACEIs.
  25. (True/False) The proline group of ACEIs is involved with the zinc binding site.
  26. (True/False) The methyl group addition at the C-2 position significantly decreased the unwanted side effects.
  27. (True/False) The auxillary binding site next to the zinc may increase some molecules affinity for binding site.
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Chem Basis ACEIs and ARBs 2
2013-12-02 03:18:53
Chem Basis ACEIs ARBs
Chem Basis ACEIs and ARBs 2
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