Page 145 - Medicinal Chemistry Self Assessment

C
D

E

134 Medicinal Chemistry Self Assessment

5. Renin catalyzes the cleavage of a specific Leu-Val peptide bond within the structure of angiotensin-
5. Renin catalyzes the cleavage of a specific Leu-Val peptide bond within the structure of side
ogen. The structure of aliskiren contains functional groups that mimic the side chains for these two
amino acids. The hydrolyzable peptide bond (found between Leu-Val) has been replaced by a non-
chains of these two amino acids and box the non-hydrolyzable hydroxyethylene group.
hydrolyzable hydroxyethylene group in aliskiren. Circle the functional groups that mimic the amino
acid side chains of these two amino acids and box the non-hydrolyzable hydroxyethylene group.

Answer:
Answer

H 3 C H 3 C CH 3
H O H H 3 C CH 3
H 2 N N NH
(remove bold from drug name) Chapter 2.8 2
O O O

H 3 CO H 3 C CH 3

6. Aliskiren can be co-administered with other anti-hypertensive agents to provide better likely is it
6. Aliskiren can be co-administered with other anti-hypertensive agents to provide better hypertension
Aliskiren

that a plasma protein binding interaction will occur if these drugs are co-administered?
management. Amlodipine is a second-generation dihydropyridine calcium channel blocker used in

the treatment of hypertension. Aliskiren and amlodipine are both plasma protein bound (47–51%

and 93–97%, respectively). How likely is it that a plasma protein binding interaction will occur if

these drugs are co-administered? (remove bold from drug name) Chapter 1.8/2.8

Amlodipine

Amlodipine