1.

What is the aim of Structure Activity Relationship

(SAR)?
a. Identify which functional groups are important
for binding and/or activity
b. Defines the relative position of the binding groups
c. Important to drug design
d. Find a lead compound

b) A drug which is normally the first to be prescribed for a

zparticular ailment.
c) A drug containing the element lead.
d) A leading drug in a particular area of medicine
Answer:A

Answer: A
8.
2.

What are the functions of pharmacophore EXCEPT?

a. Defines the important groups involved in binding
b. Need to know Active Conformation
c. Important to drug design
d. Alter, remove or mask a functional group

a)high throughput screening

b) robotic testing
c) multiscreening
d) nanotechnology

Answer: D
3.

Which are the possible effects of Carboxylic Acids?

Possible binding interactions as free acid
Charged oxygen atoms are strong HBAs
Reduction removes carbonyl oxygen as potential
HBA and prevents ionization
iv.
Sometimes present but often toxic

i.
ii.
iii.

a.
b.
c.
d.

i ,iii
ii , iv
i , ii , iii
iv only

Answer: C
4.

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.
Answer: C

5.

Which of the following needs to be established before

the search for a lead compound takes place?
a) thepharmacophore
b) Structure-activity relationships
c) a bioassay
d) patents
Answer: C

6.

What is the term used for the automated in vitro testing of

large numbers of compounds using genetically modified
cells?
a) robotic testing
b) multiscreening
c) high throughput screening
d) nanotechnology
Answer: C

7.

What is meant by a lead compound in medicinal

chemistry?
a) A compound that acts as the starting point for drug
design and development.

What is the term used for the automated in vitro testing of

large numbers of compounds using genetically modified
cells?

Answer:A
9.

Which of the following statements is false with respect to

nmr screening to detect drug-target interactions?
a)The procedure can be used on mixtures of compounds.
b)The method can detect weak binding.
c)The procedure relies on small molecules (drugs) having
shorter relaxation times than large molecules (targets).
d)The method can identify small molecules binding to
different regions of the same binding site.
Answer : C

10. What is a lead compound defined as?

A lead compound in drug discovery is a
_________compound that has pharmacological or
biological activity.
A. Chemical
B. Physical
C. Biological
D. Physical and Chemical
E. All of the above
Answer : A
11. What is Drug design sometimes referred to as
_____________.
A.Rational Drug Design
B.Irrational Drug Design
C.Chemical Drug Design
D.Biological Drug Design
E.All of the above
12. Drug Design with the help of computers may be used at
any of the following stages of drug discovery including?
A. Hit identification using virtual screening(structure-or
ligand-based design)
B. Hit to lead optimization of affinity and
selectivity(structure based design,QSAR,etc..)
C. Lead optimization of other pharmaceutical properties
while maintaining affinity.
D. All of the above
E. None of the above
13. Which one is the method of simplification? (c)

a.
b.
c.
d.

In vitro
In vivo
Remove excess rings
Alter

14. Artemisinin drug is use for? (a)

a. Antimalarial
b. Anti-hypertension
c. Anti-diabetes
d. Antidiuretic
15. Source of lead compound, except? (d)
a. Natural world
b. Synthetic world
c. Virtual world
d. Semi synthetic world
16. There are several sources and methods of discovering new
compounds. Which of the following is most likely to lead to
the discovery of a complex structure quite unlike any other
previously discovered?
A)
Combinatorial chemistry
B)
Database mining
C)
Screening plant extracts
D)
Me too drugs
17. What is the term used for drugs that are similar in structure
to a known drug and which are used for the same purpose?
A) Me-too drugs
B) Derivative drugs
C) Copycat drugs
D) Analogue drugs
18. Which source has been particularly fruitful in finding novel
antitumour agents such as bryostatins and dolostatins?
A) Venoms and toxins
B) Animals
C) Marine Sources
D) Combinatorial chemistry
19. Below are The reason Why lead compound are often
simplified, except :
a. Lead compound from natural sources are difficult to
synthesise
b. Quicker and cheaper
c. Less toxic and more selective
d. To hide the taste of compounds
20. What is the Disadvantage of oversimplification :
a. Simpler molecules have more conformation
b. Can be easily synthesize
c. Easy to be copied by competitor
d. Less interaction with binding site
21. Which below is the description of Efficacy:
a. Strength which compound bind to receptor
b. Concentration required to 50% effect
c. Measure of maximum biochemical effect resulting
from compound binding on receptor
d. Time required to 50% effect
22. Which of the following statements best describes structureactivity relationships (SAR)?
a. The study of which functional groups are important to
the chemical reactivity of the drug
b. The study of the physicochemical properties that are
important to the absorption of a drug into the blood
supply.

c.
d.

The study of the structural features of a drug that

are important to its biological activity.
The study of the structural features of a drug that are
important to its chemical stability.

Answer : C
23. Which of the following major aims in drug design is not
related to the pharmacodynamics of a drug?
a. The reduction of side effects
b. The maximisation of activity
c. The maximisation of oral bioavailability
d. The reduction of toxicity
Answer : C
24. SAR shows that the important binding groups in morphine
are the phenol, aromatic ring and amine. A diagram can be
drawn which shows these functional groups and their
relative orientations. What is the term for this?
a. Pharmacophore
b. Pharmacodynamics
c. Pharmacokinetics
d. Chromophore
Answer : A
25. Hydrogen is often replaced in drugs with a fluorine
atom for a variety of reasons. What term is used to
describe the fluorine atom whien it is used to replace
hydrogen.
a. Isotope
b. Isostere
c. Isomer
d. Isobar

26. The simplification strategy is commonly

used in drug design. What must be
retained in a molecule during the
simplification process?
a. the molecular weight
b. the stereochemistry
c. The pharmocophore (active structure)
d. The hydrophobic character

27. Which of the following terms refers to the

study of which strucural features of a drug
are important to its biological activity.
a. Pharmacodynamics
b. Pharmacokinetics
c. Strucutre-activity relationship
d. Pharmacological activity

28. The following is stages in drug designing and development

except
A) Identify target disease
B) Establish testing procedures
C) Find a lead compound
D) Industrial trials
29. What does Structural 2D Pharmacophore defines
A) Defines the minimum skeleton connecting
important binding groups

B) Defines the relative position of the binding groups

C) Defines the important groups involved in binding
D) Define the importance in drug designing
30. The following is the disadvantage of simplification except
A) Decreased in activity and selectivity
B) Simpler selectives have more conformations
C) More likely to bind with more than one binding site
D) Bind to only one binding site
31. Which of this following is not a drug targets ?
A. Lipids
B. Proteins
C. Fibres
D. Carbohydrates
2 . Drug targets including target selectivity within the body
except
A. Selectivity between different enzymes and receptors
B. Selectivity between receptor types and subtypes
C. Selectivity between isozymes
D. Selectivity between nucleic acids
3 . Which one is true about target selectivity in drug targets
between species ?
A. Antimalaria agents
B. Identify targets which are not invading pathogen
C. Identify targets which are shared but significantly
different in structure
D. Analgesic agents
32. In vivo test, it could be explain in such according to :
(Ans : B)
a) More suitable for routine testing
b) Carried out in live animal or human
c) To identify competitive or n0n-competitive
inhibition
d) Results are easier to rationalise
33. Which is below a lead compound that is from natural
world? (Ans : C)
a) Chloramphenicol maleate
b) Oxytocin
c) Tubocurarine
d) Alprazolam
34. What is the source of lead compound from virtual
world? (Ans : A)
a) Computer-aided drug design
b) Computer-graphic drug design
c) Multimedia-computerised drug design
d) Chemical drug-computerised design
35. Which of the following does not define
pharmacophores ?
A. Defines the important groups involve in binding
B. Defines the relative position of the binding groups
C. To identify target disease
D. Important to drug design and drug discovery
Answer : C
36. Why does a 3D pharmacophores needs to be related to
the active conformation ?
A. To compare activity of rigid analogues
B. To identify possible conformations and their
activities
C. To confirm the activity target binding site

D. To define relative positions of the binding

interactions
Answer:B
37. What is the second stage name in the development of
Oxamniquine ?
A. Simplification
B. Finding a lead compound
C. Drug metabolism studies
D. Preparing a binding interaction
Answer:A
38. How to testing drugs in every drugs design?
i. Testing in vivo or in vitro.
ii. Test are required in ordered to find lead compounds and
for drugs optimasation.
iii.Combination tests is often used in research
programmes.
iv. Identify competitive or non competitive inhibition.
a.
b.
c.
d.
e.

iv
i, ii
ii, iii, iv
i, ii, iii
All of the above

39. What is meant by binding site?

a. The area of a macromolecular target that is
occupied by a drug when it binds.
b. The portion of the drug to which a drug target
binds.
c. The functional groups used by a drug in binding to
a drug target.
d. The bonds involved in binding a drug to its
target.
40. Which of the following binding interactions is likely to
be the most important initialinteraction when a drug
enters a binding site?
a. van der Waals interactions
b. hydrogen bond
c. ionic
d. induced dipole-dipole interaction
41. Which of the following is the last stage in drug design
and development?
A. Identify drug target
B. Identify target disease
C. Clinical trials
D. Toxicological and safety test
42. What are the drug targets in Nucleic Acid ?
A. RNA
B. Receptor
C. Carrier Proteins
D. Enzymes
43. How does target selectivity occur in drug targets ?
A. Internal factors
B. Normal Flora
C. External Factors
D. Within the body
44. (..) is functional group for analgesic activity, except
a. Alcohols
b. Ketones
c. Aldehydes
d. Alkynes

45. Which of the following is true about esters?

a. Ester cannot pass through fatty barrier
b. Dipole-dipole bonding by R-R
c. Ester are usually hydrolysed by esterase in the
blood
d. Ester is not acting as prodrug
46. Which of the following miscellaneous functional
groups in drugs is true?
a. Acid chlorides not reactive to be of use
b. Alkyl halides present in anticancer drugs to form
dipole-dipole binding with nucleophiles in target
c. Nitro groups sometimes present but often toxic
d. Alkynes present, usually important in binding
interactions
47. Lead compounds are found by characterizing
__________ products,employing combinational
chemistry,or by molecular modeling as in rational drug
design.
A. Synthetic
B. Semi-synthetic
C. Natural
D. None of the above
E. All of the above
48. In the most basic sense,drug design involves the design
of molecules that are complementary in _________ and
__________ to the biomolecular target with which they
interact and therefore will bind to it.
A.
B.
C.
D.
E.

Polarity.......solubility
Shape........charge
Shape......polarity
Solubility.....charge
Shape......design

49. What does QSAR stand for?

A.
B.
C.
D.
E.

Qualitative Structure-Activity Relationship

Quantitative Structure-Activity Relationship
Quantitative Shape-Affinity Relationship
Qualitative Shape-Activity Relationship
Quantitative Structure-Affinity Relationship

50. Sources of lead are the following EXCEPT?

A. The natural world
B. The synthetic world
C. The virtual world
D. The structure world
51. The Beaton of Penny crossISused for?
A. Epilepsy
B. Fever
C. Angina
D. Pneumonia
Answer is A
52. Examples of lead compounds from synthetic world are
following EXCEPT?
A. Protonsil
B. Sulfanilamide
C. Antabuse
D. Atracurium

53. Which of the following reagents would

react with the amine to give another
useful analogue for SAR studies?
a. LiAlH4
B. H2 in the presence of Pd/C
c. Alkyl iodine
d. Grignard reagent

54. Which of the following bidning

interactions are possible for a secondary
amide group?
A.

hydrogen bonding as a hydrogen

bond donor only

B. Hydrogen bonding as a hydrogen

bond acceptor only
C. Hydrogen bonding both as a
hydrogen bond donor and acceptor
D. Ionic bodning

55. Which of the following terms refers to

the study of which strucural features of
a drug are important to its biological
activity.
a. Pharmacodynamics
b. Pharmacokinetics
c. Strucutre-activity relationship
d. Pharmacological activity

56. What is the drug target for drug design and

development?
I.
Nucleic acid
II.
Plasmid
III.
Lipid
IV.
Proteins
A.
B.
C.
D.

I and II
II and IV
I, II and IV
I, III and IV

57. Which of the following is the method of drug design

and development?
I.
Identify target disease
II.
Identify drug target
III.
Identify pharmacophore
IV.
Scanning by using IR spectroscopy
a.
b.
c.
d.

I and II
I and III
I, II and III
All above

58. In vivo test is use to identify target disease, which of

the following correct except:
a. Carried out on humans or animals.
b. To observed the physiological effect.
c. To identify drug potency.
d. More suitable for routine testing.
59. What is the term used for small molecules that bind to
different regions of a binding site?
A. Epitopes
B. Epimers
C. Isomers
D. Isotopes
60. Which of the following is not an endogenous
compound?
a) Dopamine
b) Endorphins
c) Desipramine
d) Noradrenaline
61. Which of the following statements best describes
structure-activity relationships (SAR)?
a) The study of which functional groups are
important to the chemical reactivity of the
drug.
b) The study of the physicochemical properties
that are important to the absorption of a drug
into the blood supply.
c) The study of the structural features of a
drug that are important to its biological
activity.
d) he study of the structural features of a drug
that are important to its chemical stability
62. What does the symbol P represent in a QSAR equation?
A. partition coefficient
B. Ph
C. plasma concentration
D. prodrug
63. What is the symbol in a QSAR equation?
A. The substituent hydrophobicity constant
B. A measure of the steric properties for a substituent
C. The electronic effect of a substituent
D. The hydrophobicity of the molecule

64. What is meant by a lead compound in medicinal

chemistry?
A. A compound that acts as the starting point for
drug design and development.
B. A drug containing the element lead.
C. A leading drug in a particular area of medicine.
D. drug which is normally the first to be prescribed for
a particular ailment.
65. Which of the following drugs was not isolated from a
natural source?
A. Quinine
B. Morphine
C. Isoniazid
D. Artemisinin
66. 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 synthesising
analogues?
A. novelty of structure
B. level of activity
C. complexity of structure
D. availability
67. Which of the following is not an endogenous lead
compound?
a) Neurotransmitter
b) Hormone
c) Alkaloid
d) Modulator
68. Which of the intermolecular bonding interactions below
are possible for a secondary amide?
a) Both hydrogen bonding and ionic bonding
b) Ionic bonding only
c) Hydrogen bonding only
d) Van der Walls interaction only
69. What is the term used for drugs that are similar in a
structure to a known drug?
a) me-too drugs
b) copy-cat drugs
c) derivative drugs
d) analogue drugs