Shared Flashcard Set

Details

Med Chem
na
20
Chemistry
Professional
03/28/2013
Click here to study/print these flashcards.

Create your own flash cards! Sign up here.

Additional Chemistry Flashcards

 

 

Cards

Term
[image]
 Definition
  1. thiazide diuretic
  2. Na/Cl transporter
  3. sulfonamide=targeting
  4. 3-4 saturation = ↑ diuretic effect
Term
[image]
 Definition
  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
Term
[image]
 Definition
  1. Loop diuretic
  2. Na/K/2Cl symporter
  3. arylsulfonamide= targeting
  4. 2-amino benzoic acid
  5. hypokalemia
Term
[image]
 Definition
  1. Carbonic anhydrase inhibitor
  2. Thiadiazole 
  3. Sulfamoyl(sulfonamide)= targeting
  4. Sulfonamide =  acidic
  5. Used in glaucoma
Term
[image]
 Definition
  1. Carbonic anhydrase inhibitor
  2. Sulfonamide = targeting
  3. Ionizable amine = water soluble
  4. Used for glaucoma
Term
[image]
 Definition
  1. Thiazide-like diuretic
  2. Sulfamoyl =  targeting
  3. C-6 chloro enhances effect
  4. No sulfonamide group, replaced with amide = less soluble = longer duration
Term
[image]
 Definition
  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. ↓ Na, Cl, H2O
Term
[image]
 Definition
  1. Osmotic diuretics(urea&mannitol)
  2. Osmotically draws water from tissues into tubule
  3. Polar molecules
Term
[image]
 Definition
  1. Na/K exchange channel inhibitor (triamterene)
  2. Pteridine ring
  3. Na not absorbed, K not excreted
  4. Used along with thiazides
Term
[image]
 Definition
  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
Term
[image]
 Definition
  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.
Term
[image]
 Definition
  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.
Term
[image]
 Definition
  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
Term
[image]
 Definition
  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 ↓ activity
  5. Added methyl on ester increase potency.
  6. Closed lactone ring = prodrug
Term
[image]
 Definition
  1. HMG-CoA reductase inhibitor(pravastatin)
  2. ↓ biosynthesis of endogenous cholesterol
  3. Decalin ring with double bonds.
  4. Ester side chain
  5. Has β hydroxyl group on decalin = ↑hydrophilicity, distribution and hepatic specificity
  6. Open lactone = active, not prodrug
Term
[image]
 Definition
  1. Fibric acid derivative(fenofibrate)
  2. Stimulates lipoprotein lipase
  3. PPRα-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
Term
[image]
 Definition
  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
Term
[image]
 Definition
  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
Term
[image]
 Definition
  1. Calcium Channel blocker(diltiazem) benzothiazepine
  2. Blocks cardiac Ltype calcium channels
Term
[image]
 Definition
  1. Calcium channel blocker (verapamil) arylalkylamine
  2. Blocks cardiac L-type calcium channels
Supporting users have an ad free experience!