Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A researcher investigates a medicinal plant used traditionally for
relieving pain and isolates a purified compound that consistently
produces the biological effect seen with the plant extract. What is the
most important reason for isolating the compound rather than
continuing to use the whole extract?
,A. The purified compound eliminates the need for pharmacological
testing
B. The purified compound allows its biological activity and chemical
properties to be evaluated more precisely
C. The purified compound is automatically safer than the original
extract
D. The purified compound will always have greater efficacy than the
extract
Correct Answer: B
Rationale:
B is correct because isolation of an active compound permits more
precise evaluation of its pharmacological activity, chemical structure,
mechanism, and potential therapeutic properties.
A is incorrect because purification does not eliminate the need for
pharmacological and toxicological testing.
C is incorrect because purification does not guarantee greater safety;
toxicity must still be evaluated.
D is incorrect because purification does not necessarily increase
efficacy; the whole extract may contain multiple active constituents or
components that affect activity.
Question 2
Which characteristic most directly distinguishes a drug lead from a
newly identified chemical hit during drug discovery?
A. A lead has already been approved for clinical use
B. A lead has demonstrated properties that justify further optimization
, C. A lead must be derived from a medicinal plant
D. A lead must have maximum potency regardless of other properties
Correct Answer: B
Rationale:
B is correct because a lead is a promising molecule whose biological
activity and chemical properties make it suitable for further
optimization toward a useful candidate.
A is incorrect because regulatory approval occurs much later in
development.
C is incorrect because leads can originate from natural products,
synthetic chemistry, screening programs, or computational approaches.
D is incorrect because potency alone is insufficient; selectivity,
pharmacokinetic properties, safety, and other characteristics are also
important.
Question 3
A medicinal chemistry team modifies the chemical structure of an
active compound while systematically comparing changes in molecular
structure with changes in biological activity. Which concept are the
researchers primarily investigating?
A. Structure-activity relationship
B. Therapeutic index
C. Bioavailability
D. Drug clearance
Correct Answer: A