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What is this drug?
Furosemide (Lasix)
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What is this drug used to treat?
- Heart failure, pulmonary edema and poisoning
- (Furosemide)
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Is this a potent Diuretic?
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(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)
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What is the pharmacophore of this drug and what type of drug is it?
Sulfamylbenzoic acid, Loop diuretic (Furosemide)
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What is this drug?
Hydrochlorothisazide
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What is the pharmacophore of this drug and what type of drug is it?
Sulfamylbenzothiadiazine 1,1 dioxide, Thiazide Diuretic(Hydrochlorothisazide)
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The Hydrogen at the N2 position is good or bad for activity?
Good(Hydrochlorothisazide)
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What component of this drug increase potency?
- Double bond at the C3– N4 position
- and
- Electron withdrawing group at the C7
(Hydrochlorothisazide)
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Is this drug active as its parent compound?
- Yes
- (Hydrochlorothisazide)
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What is this drug?
Metolazone (Zaroxoyln)
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What is the pharmacophore of this drug and what type of drug is it?
quinazolinone type diuretic(Metolazone)
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What effect does the Toluene ring structure at the N3 have on the molecule?
Enhances activity and potency(Metolazone)
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The Methyl group at C2 has what character?
Lipophilic(Metolazone)
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The Lipophilic methyl group at C2 has what effect on the molecule?
Enhances activity(Metolazone)
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What effect does the reduction of the N1-C2 double bond have?
Increases the potency(Metolazone)
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The C7 chlorine has what effect on the molecule, explain?
Enhances activity because it is electron withdrawing(Metolazone)
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What is this drug?
Methyclothiazide
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What aspects of this drug increase its potency?
C2 methyl group, C3 lipophilic group (CH2Cl) and C6 electron withdrawing group (Cl)
(Methyclothiazide)
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What groups enhance the potency of this drug?
 lipophilic groups at C2 and C4(Furosemide)
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