TEST BANK
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research team is investigating a plant used in traditional medicine for
centuries to relieve severe pain. Which development step best
represents the transition from a medicinal plant to a pharmacologically
defined drug candidate?
A. Standardizing the plant's color and odor
B. Isolating and characterizing the active chemical constituent
,responsible for the effect
C. Increasing the amount of plant material administered to patients
D. Replacing the plant with a chemically unrelated synthetic compound
Correct Answer:
B. Isolating and characterizing the active chemical constituent
responsible for the effect
Rationale:
Isolating and characterizing an active constituent allows investigators to
identify a specific chemical responsible for a biological effect and study
its pharmacology, structure, activity, and therapeutic potential. This is a
fundamental transition from an empirically used natural product to a
defined drug substance. A does not establish pharmacological activity. C
changes exposure without identifying the responsible molecule. D may
occur later during drug optimization but does not itself identify the
original active principle.
Question 2
A compound isolated from a medicinal plant produces a desirable
biological effect but is rapidly degraded in the body. Investigators
chemically modify its structure to improve stability while preserving its
therapeutic activity. Which drug-development strategy is being used?
A. Random screening
B. Structure-based optimization
C. Drug repurposing
D. Therapeutic drug monitoring
Correct Answer:
B. Structure-based optimization
, Rationale:
Chemical modification of an active compound to improve properties
such as stability while retaining or improving activity is a core
component of medicinal chemistry and lead optimization. The chemical
structure is altered to improve the candidate's overall drug-like
properties. A refers to searching compounds for biological activity
without necessarily starting from deliberate structural optimization. C
involves developing an existing drug for a new indication. D concerns
measurement of drug concentrations during clinical use, not discovery.
Question 3
A medicinal chemist compares several compounds that produce the
same desired cellular response but differ markedly in chemical
structure. What is the primary purpose of identifying these related
active compounds?
A. To eliminate the need for biological testing
B. To establish structure-activity relationships
C. To determine the patient's adherence to therapy
D. To calculate the therapeutic index of a marketed drug
Correct Answer:
B. To establish structure-activity relationships
Rationale:
Structure-activity relationship analysis examines how changes in
molecular structure influence biological activity. By comparing related
compounds, researchers can identify structural features associated with
potency, selectivity, efficacy, or toxicity and use that information to
optimize future compounds. A is incorrect because biological testing
remains essential. C concerns clinical medication use rather than
Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research team is investigating a plant used in traditional medicine for
centuries to relieve severe pain. Which development step best
represents the transition from a medicinal plant to a pharmacologically
defined drug candidate?
A. Standardizing the plant's color and odor
B. Isolating and characterizing the active chemical constituent
,responsible for the effect
C. Increasing the amount of plant material administered to patients
D. Replacing the plant with a chemically unrelated synthetic compound
Correct Answer:
B. Isolating and characterizing the active chemical constituent
responsible for the effect
Rationale:
Isolating and characterizing an active constituent allows investigators to
identify a specific chemical responsible for a biological effect and study
its pharmacology, structure, activity, and therapeutic potential. This is a
fundamental transition from an empirically used natural product to a
defined drug substance. A does not establish pharmacological activity. C
changes exposure without identifying the responsible molecule. D may
occur later during drug optimization but does not itself identify the
original active principle.
Question 2
A compound isolated from a medicinal plant produces a desirable
biological effect but is rapidly degraded in the body. Investigators
chemically modify its structure to improve stability while preserving its
therapeutic activity. Which drug-development strategy is being used?
A. Random screening
B. Structure-based optimization
C. Drug repurposing
D. Therapeutic drug monitoring
Correct Answer:
B. Structure-based optimization
, Rationale:
Chemical modification of an active compound to improve properties
such as stability while retaining or improving activity is a core
component of medicinal chemistry and lead optimization. The chemical
structure is altered to improve the candidate's overall drug-like
properties. A refers to searching compounds for biological activity
without necessarily starting from deliberate structural optimization. C
involves developing an existing drug for a new indication. D concerns
measurement of drug concentrations during clinical use, not discovery.
Question 3
A medicinal chemist compares several compounds that produce the
same desired cellular response but differ markedly in chemical
structure. What is the primary purpose of identifying these related
active compounds?
A. To eliminate the need for biological testing
B. To establish structure-activity relationships
C. To determine the patient's adherence to therapy
D. To calculate the therapeutic index of a marketed drug
Correct Answer:
B. To establish structure-activity relationships
Rationale:
Structure-activity relationship analysis examines how changes in
molecular structure influence biological activity. By comparing related
compounds, researchers can identify structural features associated with
potency, selectivity, efficacy, or toxicity and use that information to
optimize future compounds. A is incorrect because biological testing
remains essential. C concerns clinical medication use rather than
