Chem Basis Diuretics Structures 3

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kyleannkelsey
ID:
249907
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Chem Basis Diuretics Structures 3
Updated:
2013-12-01 13:22:48
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Chem Basis Diuretics Structures
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Chem Basis Diuretics Structures 3
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  1. What is this drug?
    Furosemide (Lasix)

  2. What is this drug used to treat?
    • Heart failure, pulmonary edema and poisoning
    • (Furosemide)

  3. Is this a potent Diuretic?
    • Yes
    • (Furosemide)

  4. (True/False) Adding a substituent to C3 would enhance activity.
    • False, it would abolish activity, you can only have a subtituent at C2 or C3 on sulfamylbenzoic acid derivatives
    • (Furosemide)

  5. What is the pharmacophore of this drug and what type of drug is it?
    Sulfamylbenzoic acid, Loop diuretic (Furosemide)

  6. What is this drug?
    Hydrochlorothisazide

  7. What is the pharmacophore of this drug and what type of drug is it?
    Sulfamylbenzothiadiazine 1,1 dioxide, Thiazide Diuretic(Hydrochlorothisazide)

  8. The Hydrogen at the N2 position is good or bad for activity?
    Good(Hydrochlorothisazide)

  9. What component of this drug increase potency?
    • Double bond at the C3– N4 position
    • and
    • Electron withdrawing group at the C7

    (Hydrochlorothisazide)

  10. Is this drug active as its parent compound?
    • Yes
    • (Hydrochlorothisazide)

  11. What is this drug?
    Metolazone (Zaroxoyln)

  12. What is the pharmacophore of this drug and what type of drug is it?
    quinazolinone type diuretic(Metolazone)

  13. What effect does the Toluene ring structure at the N3 have on the molecule?
    Enhances activity and potency(Metolazone)

  14. The Methyl group at C2 has what character?
    Lipophilic(Metolazone)

  15. The Lipophilic methyl group at C2 has what effect on the molecule?
    Enhances activity(Metolazone)

  16. What effect does the reduction of the N1-C2 double bond have?
    Increases the potency(Metolazone)

  17. The C7 chlorine has what effect on the molecule, explain?
    Enhances activity because it is electron withdrawing(Metolazone)

  18. What is this drug?
    Methyclothiazide

  19. What aspects of this drug increase its potency?
    C2 methyl group, C3 lipophilic group (CH2Cl) and C6 electron withdrawing group (Cl)

    (Methyclothiazide)
  20. What groups enhance the potency of this drug?
    lipophilic groups at C2 and C4(Furosemide)

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