Med Chem

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  1. thiazide diuretic
  2. Na/Cl transporter
  3. sulfonamide=targeting
  4. 3-4 saturation = ^ diuretic effect

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  1. Thiazide diuretic
  2. Na/Cl transporter
  3. Sulfonamide =  targeting
  4. C-3 lipophilic group = long duration, enhances effect
  5. N-2 subsitution = ^ duration
  6. C3-4 saturation = ^ diuretic effect

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  1. Loop diuretic
  2. Na/K/2Cl symporter
  3. arylsulfonamide= targeting
  4. 2-amino benzoic acid
  5. hypokalemia

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  1. Carbonic anhydrase inhibitor
  2. Thiadiazole 
  3. Sulfamoyl(sulfonamide)= targeting
  4. Sulfonamide =  acidic
  5. Used in glaucoma

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  1. Carbonic anhydrase inhibitor
  2. Sulfonamide = targeting
  3. Ionizable amine = water soluble
  4. Used for glaucoma

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  1. Thiazide-like diuretic
  2. Sulfamoyl =  targeting
  3. C-6 chloro enhances effect
  4. No sulfonamide group, replaced with amide = less soluble = longer duration

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  1. Aldosterone Receptor antagonist
  2. Steroid ring required for antagonism
  3. Closed lactone for activity
  4. Very low H bonding
  5. 3-keto-4-ene A ring needed for antagonism
  6. ^ K, H+
  7. v Na, Cl, H2O

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  1. Osmotic diuretics(urea&mannitol)
  2. Osmotically draws water from tissues into tubule
  3. Polar molecules

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  1. Na/K exchange channel inhibitor (triamterene)
  2. Pteridine ring
  3. Na not absorbed, K not excreted
  4. Used along with thiazides

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  1. Lisinopril ACE-I
  2. C terminal carboxyl required for binding
  3. large ring=increase potency
  4. Zinc binding region with COOH
  5. No ester = active

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  1. ACE inhibitor (enalapril)
  2. C terminal carboxyl required for binding
  3. Large heterocycle ring = increase potency
  4. Zinc binding region has carboxyl after hydrolysis.
  5. With ester is a prodrug.
  6. Binds to ACE, prevents conversion of AT1>AT2, prevents bradykinin degradation.

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  1. ARB (losartan)
  2. Imidazole
  3. N-1 variable region with biphenyl substituent
  4. Acidic group on ortho(tetrazole) required
  5. C-2 has unbranched linear hydrocarbon
  6. C-4 electron withdrawing group (Cl)
  7. C-5 H-bonding or ionic interaction group (OH,COOH)
  8. Blocks binding of AT2 to its receptor
  9. Prevents vasoconstriction, aldosterone release, catecholamine release, renal Na reabsorption.

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  1. Renin inhibitor(aliskiren)
  2. Prevents angiotensinogen> AT1
  3. Binds to Renin
  4. Hydroxyethylene has OH instead of CO(middle)
  5. Stops peptide hydrolysis by aspartyl protease

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  1. HMG-CoA reductase inhibitor (lisinopril)
  2. Decrease endogenous biosynthesis of cholesterol
  3. Decalin ring-hydrophobic anchor(needs double bonds)
  4. Ester(can be ether) slight v activity
  5. Added methyl on ester increase potency.
  6. Closed lactone ring = prodrug

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  1. HMG-CoA reductase inhibitor(pravastatin)
  2. v biosynthesis of endogenous cholesterol
  3. Decalin ring with double bonds.
  4. Ester side chain
  5. Has ? hydroxyl group on decalin = ^hydrophilicity, distribution and hepatic specificity
  6. Open lactone = active, not prodrug

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  1. Fibric acid derivative(fenofibrate)
  2. Stimulates lipoprotein lipase
  3. PPR?-antagonist= ^ expression of HDL receptors
  4. Decreases triglycerides
  5. Aromatic ring = essential, Cl increases t1/2
  6. Ether,carbonyl or ester in middle,not required.
  7. Spacer in middle could be phenyl
  8. Isobutryic component-essential

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  1. Ezetimibe
  2. Prevents absorption of cholesterol at the brush border(exogenous)
  3. Reduces hepatic cholesterol store(endogenous) and increased clearance of plasma choleterol(endogenous).
  4. Beta lactam
  5. Fluorines decrease metabolism
  6. Beta OH targets drug to intestine

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  1. Calcium channel blocker(amlodipine) dihydropyradine
  2. L type vascular smooth muscle
  3. Dihydropyradine ring required
  4. Phenyl group on C-4 with ortho or meta substituent, keeps the rings perpendicular
  5. Esters in positions 3,5 are required, if acids = inactive.
  6. C2,6 are bulk

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  1. Calcium Channel blocker(diltiazem) benzothiazepine
  2. Blocks cardiac Ltype calcium channels

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  1. Calcium channel blocker (verapamil) arylalkylamine
  2. Blocks cardiac L-type calcium channels

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