Page 140 - Medicinal Chemistry Self Assessment

Section 4 Whole Molecule Drug Evaluation

Answers

2.8 Aliskiren

Aliskiren is an orally active agent used in the treatment of hypertension. This non-peptide drug acts as an inhibitor
of renin, the enzyme that converts angiotensinogen (its endogenous substrate) to angiotensin I. Biologically inactive,
angiotensin I is rapidly converted to angiotensin II by angiotensin converting enzyme. Angiotensin II is a potent
agonist when bound to its receptor and produces significant vasoconstriction, as well as an increase in blood pressure.
In the presence of aliskiren, angiotensinogen is not converted to angiotensin I so less angiotensin II is produced to
activate the angiotensin II receptor. Consequently less vasoconstriction occurs, and a drop in blood pressure results.
Medicinal Chemistry Self-Assessment Book: Batch Two
Chapters 1.8 and 2.8

1. Conduct a structural evaluation of aliskiren, focusing on the boxed functional groups and use the informa-
Chapter 1.8/2.8 (remove bold from drug name x2)
tion in the grid to inform your answers to the questions that follow.

E
D F
A
B

Aliskiren
C

Aliskiren

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