Chem Basis Diuretics Structures 2

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kyleannkelsey
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Chem Basis Diuretics Structures 2
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2013-12-06 16:39:43
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Chem Basis Diuretics Structures
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Chem Basis Diuretics Structures 2
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  1. If this sulfonamide is Secondary (R3=H), what capability will it have that it would not if it were tertiary?
    • Ability to form water soluble salts
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  2. Is this sulfonamide acidic or basic?
    • Acidic
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  3. What difference in activity would you expect between these two molecules?
    10x increase in potency of the Reduced form

  4. What differences in therapeutic activity, DOA and electrolyte patterns are evident between these two structures?
    None, should be similar, only potency is altered

  5. What type of group would be best for activity at this position?
    • Electron withdrawing, Halogen
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  6. In order from most to least, organize the following substituents ability to increase potency at this position, explain why: CI, Br and CF3
    • What type of group would be best for activity at this position?
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  7. A string electron withdrawing group at this position imparts what benefits?
    • Increase potency and the acidity of C7 sulfamyl resulting in an increase distribution to the site of action (kidney)
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  8. OCH3, CH3 and NH2, will increase or decrease activity at this location, why?
    • Decrease, because they are electron donors
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  9. What substituent character would be ideal for potency at this location?
    Lipophilicity

    (Sulfamylbenzothiadiazine 1,1 dioxide)

  10. What substituent character would be ideal for increasing DOA at this location?
    • Lipophilicity
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  11. What can this substituent be?
    H or CH3

    (Sulfamylbenzothiadiazine 1,1 dioxide)

  12. What would this substituent need to be for the molecule to have acidic character?
    H (Secondary Sulfonamide)

    (Sulfamylbenzothiadiazine 1,1 dioxide)

  13. If this substituent were CH3 would the sulfonamide have acidic, neutral or basic character?
    • Neutral
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  14. What group at R3 would increase DOA and activity?
    CH3

    (Sulfamylbenzothiadiazine 1,1 dioxide)

  15. What effect would an ethyl group at R3 have on this molecule's activity?
    Reduced activity

    (Sulfamylbenzothiadiazine 1,1 dioxide)

  16. What is this molecule called?
    Quinazolinone

  17. How does this molecule compare to Thiazide diuretics?
    Same activity and side effects, derivatives with similar substituents at the R1, R2 and R3 will be equipotent

    (Quinazolinone)

  18. What substituent at R3 would allow for a potent diuretic effect which results in maintaining activity in patients with kidney disease (Clcr < 30ml/min.)?
    • Toluene
    • (Quinazolinone)

  19. What is this structure?
    Toluene

  20. What is this group called?
    • Lactone ring
    • (Spirolactone)

  21. What is this structure called?
    Eplerenone

  22. What are these structures?
    A: Eplerenone   B: Spirolactone

  23. Which of these drugs has fewer side effects?
    A(A: Eplerenone   B: Spirolactone)

  24. When should A be used over B?
    When a patient has good therapeutic response to B, but cannot tolerate the side effects(A: Eplerenone   B: Spirolactone)

  25. Should this drug be used alone or in combination therapy?
    Should this drug be used alone or in combination therapy?

  26. Which drug has a lower binding affinity for androgenic and progestogenic receptors?
    A

    (A: Eplerenone   B: Spirolactone)

  27. Which drug has lower incidence of endocrine-related side effects such as gynecomastia?
    • A
    • (A: Eplerenone   B: Spirolactone)

  28. What type of diuretic is this?
    • Pteridine ring derivative
    • (Amiloride)

  29. What is this drug?
    Amiloride

  30. What is this drug?
    Triamterene

  31. What type of diuretic is this?
    • Pteridine ring derivative
    • (Triamterene)

  32. What group at C6 would enhance activity?
    • Lipophilic group
    • Such as:  benzene ring or a chlorine

    (Pteridine)

  33. How is this drug excreted?
    • ionized and excreted mainly in the urine
    • (Amiloride)

  34. How is this drug excreted?
    • Undergoes metabolism to inactive metabolites and then is excreted (it doesn't say how)
    • (Triamterene)

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