benzothiadiazine
What heterocycle is this?
a
An alkyl placed at position ____ will increase lipophilicity and duration of action.
a) position 2
b) position 3
c) position 3-4
d) position 6
e) position 7
b
A lipophilic group placed at position ______ will increase potency.
a) position 2
b) position 3
c) position 3-4
d) position 6
e) position 7
c
Saturation at position _____ will increase activity 10x.
a) position 2
b) position 3
c) position 3-4
d) position 6
e) position 7
d
The electron-withdrawing group must be at position ______.
a) position 2
b) position 3
c) position 3-4
d) position 6
e) position 7
e
Position ____ increases activity but leads to hypersensitivity.
a) position 2
b) position 3
c) position 3-4
d) position 6
e) position 7
chlorobenzensulfonamide
What is the highlighted structure?
3-4; saturated bond= increased activity
This is HCTZ. What is the position of the red circle? What does this change do to the structure?
phthalimide ring
What structure is this?
phenoxy; acts as electron-withdrawing group
What is this group?
What does this addition do?
benzensulfonamide
What is the name of this group?
butyl amine; increases lipophilicity; assists hepatic metabolism
What is the name of this group?
What does it do?
pyridine
What is the name of this group?
aniline
What is the name of this group?
sulfonylurea
What is the name of this group?
chlorothiazide, HCTZ, chlorthalidone, indapamide, furosemide, bumetanide, torsemide
Which drugs have a sulfonamide in their structures? (7)
irreversible inhibitor that covalently binds Na/K/Cl cotransporter, unsaturated lactone nucleophile that reacts with sulfhydryl groups of cysteine receptor; phenoxyacetic acid;
This is Ethacrynic acid.
What is unique about its MOA?
What is the name of this group?
antagonist for aldosterone; spironolactone, aldosterone
What does this structure do? What drugs is it found in?
triamterene
Which drug contains 3 aromatic rings that are highly aminated?
the open ring and cl- group
Why is Amiloride 100x more potent than Triamteren?
catechol ring
What is the highlighted structure?
dichlorobenzene; imidazole
What is the blue structure?
What is the red structure?
piperazine
What is the red structure?
s
Which has more activity? S or R enantiomer?
a
Induces release of NO from the drug.
a) nitroprusside
b) hydralazine
b
Induces release of NO from the endothelium.
a) nitroprusside
b) hydralazine
d
Which activates the dopamine receptors?
a) minoxidil
b) hydralazine
c) nitroprusside
d) fenoldopam
r-isomer
Which is more active?
R-isomer of Fendolopam
S-isomer of Fendolopam
sulfhydryl; enhances potency in ACE inhibition
What is this red structure?
What does its addition do?
losartan
What was the first-marketed ARB?
carbon atom, position delta
Where is the amine positioned?