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?Image Upload
    • Ability to form water soluble salts
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  2. Image UploadIs this sulfonamide acidic or basic?
    • Acidic
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  3. Image Upload
    What difference in activity would you expect between these two molecules?
    10x increase in potency of the Reduced form
  4. Image Upload
    What differences in therapeutic activity, DOA and electrolyte patterns are evident between these two structures?
    None, should be similar, only potency is altered
  5. Image Upload
    What type of group would be best for activity at this position?
    • Electron withdrawing, Halogen
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
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    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. Image Upload
    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. Image Upload
    OCH3, CH3 and NH2, will increase or decrease activity at this location, why?
    • Decrease, because they are electron donors
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  9. Image Upload
    What substituent character would be ideal for potency at this location?
    Lipophilicity

    (Sulfamylbenzothiadiazine 1,1 dioxide)
  10. Image Upload
    What substituent character would be ideal for increasing DOA at this location?
    • Lipophilicity
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  11. Image Upload
    What can this substituent be?
    H or CH3

    (Sulfamylbenzothiadiazine 1,1 dioxide)
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    What would this substituent need to be for the molecule to have acidic character?
    H (Secondary Sulfonamide)

    (Sulfamylbenzothiadiazine 1,1 dioxide)
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    If this substituent were CH3 would the sulfonamide have acidic, neutral or basic character?
    • Neutral
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  14. Image Upload
    What group at R3 would increase DOA and activity?
    CH3

    (Sulfamylbenzothiadiazine 1,1 dioxide)
  15. Image Upload
    What effect would an ethyl group at R3 have on this molecule's activity?
    Reduced activity

    (Sulfamylbenzothiadiazine 1,1 dioxide)
  16. Image Upload
    What is this molecule called?
    Quinazolinone
  17. Image Upload
    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)
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    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)
    • Image Upload
  19. Image Upload
    What is this structure?
    Toluene
  20. Image Upload
    What is this group called?
    • Lactone ring
    • (Spirolactone)
  21. Image Upload
    What is this structure called?
    Eplerenone
  22. Image Upload
    What are these structures?
    A: Eplerenone   B: Spirolactone
  23. Image Upload
    Which of these drugs has fewer side effects?
    A(A: Eplerenone   B: Spirolactone)
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    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. Image Upload
    Should this drug be used alone or in combination therapy?
    Should this drug be used alone or in combination therapy?
  26. Image Upload
    Which drug has a lower binding affinity for androgenic and progestogenic receptors?
    A

    (A: Eplerenone   B: Spirolactone)
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    Which drug has lower incidence of endocrine-related side effects such as gynecomastia?
    • A
    • (A: Eplerenone   B: Spirolactone)
  28. Image Upload
    What type of diuretic is this?
    • Pteridine ring derivative
    • (Amiloride)
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    What is this drug?
    Amiloride
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    What is this drug?
    Triamterene
  31. Image Upload
    What type of diuretic is this?
    • Pteridine ring derivative
    • (Triamterene)
  32. Image Upload
    What group at C6 would enhance activity?
    • Lipophilic group
    • Such as:  benzene ring or a chlorine

    (Pteridine)
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    How is this drug excreted?
    • ionized and excreted mainly in the urine
    • (Amiloride)
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    How is this drug excreted?
    • Undergoes metabolism to inactive metabolites and then is excreted (it doesn't say how)
    • (Triamterene)
Author:
kyleannkelsey
ID:
249884
Card Set:
Chem Basis Diuretics Structures 2
Updated:
2013-12-06 21:39:43
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Chem Basis Diuretics Structures 2
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