Chapter 12 - Drug discovery: finding a lead Correctly Answered Questions
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Chapter 12 - Drug discovery: finding a lead
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Chapter 12 - Drug Discovery: Finding A Lead
Chapter 12 - Drug discovery: finding a lead
C (The more selective a drug is for its target, the less it will interact with other targets to produce undesirable side effects. Good oral absorption and fast metabolism are pharmacokinetic issues and do not affect the selectivity of the drug for one ...
Chapter 12 - Drug discovery: finding a
lead
C (The more selective a drug is for its target, the less it will interact with other targets to produce
undesirable side effects. Good oral absorption and fast metabolism are pharmacokinetic issues
and do not affect the selectivity of the drug for one target over another. The affinity of a drug
may have high affinity for the desired target, but it may also have high affinity for other less
desirable targets.) - Answer-**Which of the following properties of a drug is most likely to result
in a minimum of side effects?
a) Good oral absorption.
b) Fast metabolism.
c) Target selectivity.
d) Target affinity.
C (Micro-organisms such as fungi have proved a rich source of antibacterial agents. Fungi have
to compete against bacteria for nutrients, and the ability of fungi to produce antibacterial agents
give these fungi an advantage in this contest.) - Answer-**Which of the following sources has
been particularly fruitful in the discovery of antibacterial agents?
a) Plant extracts.
b) Venoms and toxins.
c) Micro-organisms.
d) Animals.
B (Teprotide is a peptide which was isolated from the venom of the Brazilian viper and was one
of the lead compounds for the development of the antihypertensive agent captopril.) - Answer-
From which source did one of the lead compounds (teprotide) for the antihypertensive agent
captopril come?
a) Marine sources.
b) Venoms and toxins.
c) Combinatorial chemistry.
d) Animals.
B (Natural products are often complex in structure which makes their synthesis difficult. As a
result, the synthesis of analogues can also be difficult.) - Answer-**Natural products are often
used as lead compounds in the design and synthesis of novel drugs. Which of the following
general characteristics of a natural product is most likely to be a disadvantage in synthesizing
analogues?
a) Novelty of structure.
b) Complexity of structure.
c) Level of activity.
d) Availability.
, B (Morphine is isolated from the poppy plant. Aspirin and diamorphine are semi synthetic drugs
prepared from compounds isolated from a natural source. Isoniazid is synthesized in the
laboratory.) - Answer-Which of the following drugs is isolated from a natural source?
a) Aspirin.
b) Morphine.
c) Isoniazid.
d) Diamorphine (Heroin).
D (It can often be tedious and expensive to extract an active compound from its natural source.
Natural products are also often complex in structure which makes their synthesis difficult.
Novelty is usually an advantage. Side effects and poor activity are obviously disadvantages, but
if it is possible to prepare analogues by modifying the lead compound or synthesizing
analogues, it is often possible to increase activity and lower side effects.) - Answer-**Natural
products are often used as lead compounds in the design and synthesis of novel drugs. Which
of the following general characteristics of a natural product is most likely to be a disadvantage?
a) Novelty of structure.
b) Side effects.
c) Level of activity.
d) Its availability.
D (Endogenous compounds are any compounds occurring naturally in the body. These are also
biochemicals, but this is not the term that is used in medicinal chemistry. A hormone and a
neurotransmitter are examples of endogenous compounds, but not all endogenous compounds
are hormones or neurotransmitters.) - Answer-**Which of the following terms is used to indicate
that a lead compound is one of the body's own chemicals?
a) A neurotransmitter.
b) A biochemical.
c) A hormone.
d) An endogenous compound.
B (Endogenous compounds are any compounds occurring naturally in the body. Fluoxetine is a
synthetic drug and is not an endogenous compound.) - Answer-Which of the following is not an
endogenous compound?
a) Adrenaline.
b) Fluoxetine.
c) Serotonin.
d) Testosterone.
C (A lead compound is a compound that acts as the starting point for drug design and
development. It may have disadvantages such as low activity or the presence of side effects,
but it acts as a starting point for the development of a better agent.) - Answer-**What is meant
by a lead compound in medicinal chemistry?
a) A drug containing the element lead.
b) A leading drug in a particular area of medicine.
c) A compound that acts as the starting point for drug design and development.
d) A drug which is normally the first to be prescribed for a particular ailment.
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