Chem Basis Diuretics Structures 1

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kyleannkelsey
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249856
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Chem Basis Diuretics Structures 1
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2013-11-30 22:10:07
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Chem Basis Diuretics Structures
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Chem Basis Diuretics Structures 1
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  1. What is this structure?
    Loop Diuretic Pharmacophores

  2. What is this structure?
    Pyridylsulfonylurea, One of the Loop diuretic pharamcophores

  3. What is this structure?
    Sulfamylbenzoic acid, One of the Loop diuretic pharamcophores

  4. Is this structure essential?
    Yes

  5. What is this structure?
    Sulfamylbenzothiadiazine 1,1 dioxide, Thiazide Diuretic Pharmacophore

  6. What is this structure?
    Pteridine Analog pharmacophore

  7. What is this structure called?
    • Sulfonamide
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  8. Is this structure essential for activity?
    • Yes
    • (Sulfamylbenzoic acid)

  9. What type of substituent should be at this location?
    • Lipophilic
    • (Sulfamylbenzoic acid)
  10. At these two positions, what type of substitution pattern would abolish activity?
    • Both positions carrying substituents. Only one can be substituted.
    • (Sulfamylbenzoic acid)
  11. Is this structure essential to the pharamcophore?

    • Yes
    • (Sulfamylbenzoic acid)

  12. Is this highly ionized at physiological pH?
    • Yes
    • (Sulfamylbenzoic acid)
  13. What effect does this structure have on the pharmacodynamics of this pharamcophore?
    • Helps keep the compound localized at site of action in the kidney
    • (Sulfamylbenzoic acid)

  14. What is this drug?
    Torsemide
  15. What position should this substituent be in?
    • Ortho to the sulfamyl group
    • (Sulfamylbenzoic acid)
  16. What is the pharmacophore and what type of diuretic is this drug?
    • Pyridylsulfonyl urea, Loop Diuretic
    • (Torsemide)

  17. What is this substituent called?
    • Amino toluene
    • (Torsemide)


  18. Is this substituent lipophilic or hydrophilic?
    • Lipophilic
    • (Torsemide)

  19. What position should this substituent be in?
    • Ortho to the sulfonylurea
    • (Torsemide)
  20. Reducing this double bond has what effect on the molecule?
    • Diminished activity
    • (Ethacrynic acid)
  21. What is this molecule?
    Ethacrynic acid

  22. What effect do these Hydrogens have on this structure?
    • Provides maximum reactivity
    • (Ethacrynic acid)

  23. What pharmacophore does this drug have and what type of diuretic is it?
    • Phenoxyacetic acid, Loop diuretic
    • (Ethacrynic acid)

  24. What is this group called and what position should it be in for optimal activity?
    • Oxyacetic acid, para to the a,b-unsaturated carbonyl
    • (Ethacrynic acid)

  25. How many sulfonamides are present in this molecule?
    • 2
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  26. What is this sulfonamide structure called?
    Endocyclic

    (Sulfamylbenzothiadiazine 1,1 dioxide)

  27. What is this sulfonamide structure called?
    • Exocyclic
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  28. This sulfonamide can be Primary, Secondary or Tertiary?
    • Secondary or Tertiary
    • (Sulfamylbenzothiadiazine 1,1 dioxide)
  29. This sulfonamide can be Primary, Secondary or Tertiary?
    • Must be Primary
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  30. If this sulfonamide were Secondary, what would R3 be?
    • H
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

  31. If this sulfonamide were Tertiary, what would R3 be?
    • alkyl group
    • (Sulfamylbenzothiadiazine 1,1 dioxide)

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