Page 41 - Medicinal Chemistry Self Assessment

1.8 Aliskiren
1. Conduct a structural evaluation of aliskiren, focusing on the boxed functional groups, and use

E
D
F
A
B
Aliskiren
C

2. Aliskiren is marketed as are possible.
2.
2. the information in the grid to inform your answers to the questions that follow.
2.
2.
2.
Medicinal Chemistry Self Assessment
30 2.
2.
Aliskiren

5. Renin catalyzes the cleavage of a specific Leu-Val peptide bond within the structure of angiotensin-
2.
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 The hydrolyzable peptide bond (found between Leu-Val) has been replaced by a non-
5. Renin non-hydrolyzable hydroxyethylene group.
2.
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.
2.

2.

2.
(remove bold from drug name) Chapter 2.8

2.

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6. Aliskiren can be co-administered with other anti-hypertensive agents to provide better hypertension
management. Amlodipine is a second generation dihydropyridine calcium channel blocker used in
2.
Aliskiren

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

2.
and 93–97%, respectively). How likely is it that a plasma protein binding interaction will occur if

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

Amlodipine

Answers can be found in Section 2.8 [this will be linked to section 2.8 title]