Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
Which development in drug discovery best explains why naturally
occurring compounds from medicinal plants can serve as starting points
for modern drug development?
A. Natural products are always safe at therapeutic doses.
B. Natural products can provide structurally diverse molecules with
biological activity that can be optimized into drug candidates.
C. Natural products usually require no chemical modification before
clinical use.
,D. Natural products are preferred because their mechanisms are always
fully understood.
Correct Answer:
B. Natural products can provide structurally diverse molecules with
biological activity that can be optimized into drug candidates.
Rationale:
B is correct because natural products can provide chemically diverse
biologically active molecules that serve as leads for further
optimization. Their initial activity does not guarantee safety, efficacy, or
optimal pharmacokinetics.
A is incorrect because natural origin does not eliminate toxicity or
adverse effects.
C is incorrect because many natural-product leads require chemical
modification to improve potency, selectivity, stability, or disposition.
D is incorrect because the biological mechanisms of natural products
may initially be uncertain and require substantial investigation.
Question 2
A researcher isolates a plant-derived compound that produces a
reproducible biological effect in an experimental system but has poor
pharmacokinetic properties. What is the most appropriate
interpretation?
A. The compound should be abandoned because pharmacokinetics are
irrelevant to drug discovery.
B. The compound may represent a lead that can undergo structural
optimization.
C. The compound is automatically a drug because it has biological
, activity.
D. The compound should immediately proceed to clinical trials.
Correct Answer:
B. The compound may represent a lead that can undergo structural
optimization.
Rationale:
B is correct because a biologically active compound can serve as a lead
even when its initial properties are suboptimal. Medicinal chemistry
may improve potency, selectivity, metabolic stability, solubility, or other
drug-like properties.
A is incorrect because pharmacokinetics are essential to determining
whether adequate drug exposure can be achieved.
C is incorrect because biological activity alone is insufficient for
designation as a useful therapeutic drug.
D is incorrect because promising compounds require substantial
preclinical evaluation before clinical testing.
Question 3
What is the primary purpose of medicinal chemistry during lead
optimization?
A. To replace all biological testing with chemical analysis
B. To identify every disease associated with the target
C. To systematically modify a lead structure to improve desirable drug
properties
D. To determine whether a disease is caused by a genetic mutation