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 investigates compounds used for centuries in
traditional medicine and discovers that a plant extract produces a
reproducible physiological effect. Which feature of this approach makes
it valuable for early drug discovery?
A. It guarantees that the active compound will have acceptable
pharmacokinetics
,B. It provides naturally occurring chemical structures with biological
activity
C. It eliminates the need for purification and characterization
D. It demonstrates clinical efficacy before laboratory testing
Correct Answer:
B. It provides naturally occurring chemical structures with biological
activity
Rationale:
B is correct because medicinal plants can provide chemically diverse
molecules that already interact with biological systems, making them
useful starting points for identifying active compounds. The historical
progression from medicinal plants to isolated active constituents is an
important part of drug discovery.
A is incorrect because biological activity does not guarantee favorable
absorption, distribution, metabolism, or toxicity characteristics.
C is incorrect because plant extracts generally contain multiple
constituents and require isolation and characterization of active
components.
D is incorrect because activity observed from traditional use does not
establish efficacy or safety in controlled human studies.
Question 2
A natural product produces a strong biological effect, but its chemical
structure is too complex for convenient large-scale synthesis. What is
the most appropriate next step in drug discovery?
, A. Immediately begin Phase I clinical trials
B. Abandon the compound because natural products cannot become
drugs
C. Isolate and characterize the active constituent and investigate
structurally related analogs
D. Assume the entire plant extract is the active pharmaceutical
ingredient
Correct Answer:
C. Isolate and characterize the active constituent and investigate
structurally related analogs
Rationale:
C is correct because natural products can serve as starting points for
identifying active molecular entities that can subsequently be
characterized and optimized. Structural modification of an active
compound can improve properties relevant to development.
A is incorrect because extensive preclinical characterization is required
before human testing.
B is incorrect because many important therapeutic compounds
originated from natural-product discovery.
D is incorrect because an extract may contain numerous compounds
with different pharmacological effects and cannot automatically be
treated as a defined drug substance.
Question 3
During a high-throughput screening campaign, a compound produces
measurable inhibition of a target but has only moderate potency and
uncertain selectivity. How should this compound initially be classified?