Page 35 - Medicinal Chemistry Self Assessment
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24 Medicinal Chemistry Self Assessment
3. Metabolites do not necessarily have the same mechanism of action as the parent drug. In the case of
chlorimipramine (a tricyclic antidepressant that inhibits serotonin uptake), a phase I transformation
produces a metabolite that is also a tricyclic antidepressant, but whose mechanism of action is via
3. Metabolites do not of action as the parent drug. In the case of I transformations are possible?
inhibition of norepinephrine reuptake. Which phase I transformation has occurred? What additional
3. Metabolites do not of action as the parent drug. In the case of I transformations are possible?
phase I transformations are possible?
Chlorimipramine
Chlorimipramine
4. Evaluate each of the following metabolic transformations and determine which phase I metabolic
4. Evaluate each of the phase I metabolic transformation has occurred.
transformation has occurred.
4. Evaluate each of the phase I metabolic transformation has occurred.
H
N C H 3 NH
H 2
CH C H 3 CH 3 NH 2
N3
CF 3 CH 3 CF 3 CH 3
CF 3Dexfenfluramine CF 3
Dexfenfluramine
Fluvoxamine
Fluvoxamine
Baclofen
Baclofen
Answers can be found in Section 2.7 [this will be linked to section 2.7 title]
Note: The questions in this chapter are related to Chapter 8 in Harrold MW and Zavod RM, Basic Concepts in
Medicinal Chemistry, American Society of Health-System Pharmacists, ©2013.