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4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
Patrick: An Introduction to Medicinal Chemistry 6e Chapter 12
Results
You have answered 3 out of 15 questions correctly. Your percentage score is 20%. Question 1 What is meant by a lead compound in medicinal chemistry?
Your answer: a) A drug containing the element lead. Correct answer: c) A compound that acts as the starting point for drug design and development. Feedback: 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. 199
Page reference: Question 2
Which of the following needs to be established before the search for a lead compound takes place?
Your answer: a) the pharmacophore Correct answer: c) a bioassay Feedback: The lead compound has to have some sort of desirable biological activity, and so a bioassay to detect that activity is required. Structureactivity relationships and the identification of a pharmacophore are stages in the drug design process that come after the discovery of the lead compound. Patents are taken out at a later stage once potentially useful compounds have been designed and developed. 195-196
Page reference: Question 3
What is the term used for the automated in vitro testing of large numbers of compounds using genetically modified cells?
Your answer: a) robotic testing Correct answer: b) high throughput screening Feedback: https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
1/5
4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
As well as being automated and capable of handling large numbers of compounds, high throughput screening (HTS) can be carried out on small scale, allowing results to be obtained quickly and efficiently. 196-197
Page reference: Question 4
Which of the following statements is false with respect to nmr screening to detect drug-target interactions?
Your answer: a) The procedure relies on small molecules (drugs) having shorter relaxation times than large molecules (targets). Feedback: The procedure relies on small molecules (drugs) having longer relaxation times than large molecules (targets). When a small drug binds to a macromolecular target, it essentially becomes part of that target and the signals for that compound will have shorter relaxation times. If there is a time delay in measuring the nmr spectrum, the signals for molecules that bind to the protein will disappear from the spectrum.
Page reference: 197 Question 5
BIAcore is a detection system patented by Pharmacia Biosensor to detect a ligand binding to a target. What is the name of the phenomenon used in this detection procedure?
Your answer: a) nuclear magnetic resonance Correct answer: c) surface plasmon resonance Feedback: Nuclear magnetic resonance and electron spin resonance are both forms of spectroscopy. BIAcore makes use of surface plasmon resonance, which involves the interaction of a reflected wave of plane polarised light with free oscillating electrons called plasmons in a metal film. Scintillation proximate assay involves the immobilisation of a target molecule on beads coated with a scintillant. A ligand labelled with 125I binds to the target and the radioisotope interacts with the scintillant to emit light. 195-196
Page reference: Question 6
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?
Your answer: a) combinatorial chemistry Correct answer: c) screening plant extracts Feedback: There are no preconceived ideas when screening plant extracts for active lead compounds. Some natural products are quite bizarre in structure! Combinatorial chemistry involves the synthesis of a large number of compounds using a standard synthetic route, and so the types of structures that will be synthesised are predictable and belong to a similar family of compounds. Database mining involves the computerised search of known compounds for particular pharmacophores. Me-too drugs are analogues of an established drug. 199-202
Page reference:
https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
2/5
4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
Question 7 Which source has been particularly fruitful in finding novel antitumour agents such as bryostatins and dolostatins?
Your answer: c) combinatorial chemistry Correct answer: a) marine sources Feedback: Marine life such as coral, fish and cyanobacteria have proved useful sources of novel lead compounds having antitumour properties. 200-201
Page reference: Question 8
Which of the following drugs was not isolated from a natural source?
Your answer: b) morphine Correct answer: c) isoniazid Feedback: Isoniazid was synthesised in the laboratory. The other three compounds were derived from natural sources. Quinine was isolated from the bark of the cinchona tree. Morphine was isolated from the seed pods of poppies. Artemisinin was isolated from a Chinese plant. 199, 203
Page reference: Question 9
What is the term used for drugs that are similar in structure to a known drug and which are used for the same purpose?
Your answer: a) 'copycat' drugs Correct answer: b) 'me-too' drugs Feedback: The terms given in options a), c) and d) are not used in medicinal chemistry. 203
Page reference: Question 10
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?
Your answer: b) complexity of structure Feedback: Natural products are often complex in structure which makes their synthesis difficult. As a result, the synthesis of analogues can also be difficult. https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
3/5
4/1/2019
Page reference: 199
Oxford University Press | Online Resource Centre | Chapter 12
Question 11 Which of the following is not an endogenous lead compound?
Your answer: a) neurotransmitter Correct answer: b) alkaloid Feedback: Alkaloids are plant natural products containing nitrogen. The other options are endogenous compounds in the body. 199, 204-206
Page reference: Question 12
What is the term used for small molecules that bind to different regions of a binding site?
Your answer: a) epimers Correct answer: d) epitopes Feedback: The correct answer is epitopes. Epimers are diastereomers differing in their configuration at one asymmetric centre. Isomers are different structures having the same molecular formula. Isotopes are elements which have the same number of protons and electrons, but a different number of neutrons. 209-210
Page reference: Question 13
Which of the following statements is not true of herbal medicines?
Your answer: a) Herbal medicines may contain a range of active principles acting together to produce a beneficial effect. Correct answer: b) Herbal medicines have no side effects compared to conventional medicines. Feedback: There is no reason why herbal medicines should be free of side effects. They contain active components which will vary in their selectivity for their targets. Some will produce more side effects than others. 212-213
Page reference: Question 14
https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
4/5
4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
The following diagram illustrates the detection system known as surface plasmon resonance. What is represented by D?
Your answer: a) the evanescent wave Feedback: D is the evanescent wave which interacts with free oscillating electrons called plasmons in the metal film, when the angle of incidence (α) is correct. Symbol A represents a receptor which is covalently linked to the dextran matrix, and which will bind ligands present in the buffer flow. B is monochromatic plane-polarised light. C is the flow of buffer solution. 197-198
Page reference: Question 15
Which of the following is not an endogenous compound?
Your answer: a) dopamine Correct answer: d) desipramine Feedback: Endogenous compounds are any compounds occurring naturally in the body. Desipramine is a synthetic drug and is not an endogenous compound. 204-206
Page reference:
Copyright © Oxford University Press, 2016. All Rights Reserved.
https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
5/5
Oxford University Press | Online Resource Centre | Chapter 12
Patrick: An Introduction to Medicinal Chemistry 6e Chapter 12
Results
You have answered 3 out of 15 questions correctly. Your percentage score is 20%. Question 1 What is meant by a lead compound in medicinal chemistry?
Your answer: a) A drug containing the element lead. Correct answer: c) A compound that acts as the starting point for drug design and development. Feedback: 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. 199
Page reference: Question 2
Which of the following needs to be established before the search for a lead compound takes place?
Your answer: a) the pharmacophore Correct answer: c) a bioassay Feedback: The lead compound has to have some sort of desirable biological activity, and so a bioassay to detect that activity is required. Structureactivity relationships and the identification of a pharmacophore are stages in the drug design process that come after the discovery of the lead compound. Patents are taken out at a later stage once potentially useful compounds have been designed and developed. 195-196
Page reference: Question 3
What is the term used for the automated in vitro testing of large numbers of compounds using genetically modified cells?
Your answer: a) robotic testing Correct answer: b) high throughput screening Feedback: https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
1/5
4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
As well as being automated and capable of handling large numbers of compounds, high throughput screening (HTS) can be carried out on small scale, allowing results to be obtained quickly and efficiently. 196-197
Page reference: Question 4
Which of the following statements is false with respect to nmr screening to detect drug-target interactions?
Your answer: a) The procedure relies on small molecules (drugs) having shorter relaxation times than large molecules (targets). Feedback: The procedure relies on small molecules (drugs) having longer relaxation times than large molecules (targets). When a small drug binds to a macromolecular target, it essentially becomes part of that target and the signals for that compound will have shorter relaxation times. If there is a time delay in measuring the nmr spectrum, the signals for molecules that bind to the protein will disappear from the spectrum.
Page reference: 197 Question 5
BIAcore is a detection system patented by Pharmacia Biosensor to detect a ligand binding to a target. What is the name of the phenomenon used in this detection procedure?
Your answer: a) nuclear magnetic resonance Correct answer: c) surface plasmon resonance Feedback: Nuclear magnetic resonance and electron spin resonance are both forms of spectroscopy. BIAcore makes use of surface plasmon resonance, which involves the interaction of a reflected wave of plane polarised light with free oscillating electrons called plasmons in a metal film. Scintillation proximate assay involves the immobilisation of a target molecule on beads coated with a scintillant. A ligand labelled with 125I binds to the target and the radioisotope interacts with the scintillant to emit light. 195-196
Page reference: Question 6
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?
Your answer: a) combinatorial chemistry Correct answer: c) screening plant extracts Feedback: There are no preconceived ideas when screening plant extracts for active lead compounds. Some natural products are quite bizarre in structure! Combinatorial chemistry involves the synthesis of a large number of compounds using a standard synthetic route, and so the types of structures that will be synthesised are predictable and belong to a similar family of compounds. Database mining involves the computerised search of known compounds for particular pharmacophores. Me-too drugs are analogues of an established drug. 199-202
Page reference:
https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
2/5
4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
Question 7 Which source has been particularly fruitful in finding novel antitumour agents such as bryostatins and dolostatins?
Your answer: c) combinatorial chemistry Correct answer: a) marine sources Feedback: Marine life such as coral, fish and cyanobacteria have proved useful sources of novel lead compounds having antitumour properties. 200-201
Page reference: Question 8
Which of the following drugs was not isolated from a natural source?
Your answer: b) morphine Correct answer: c) isoniazid Feedback: Isoniazid was synthesised in the laboratory. The other three compounds were derived from natural sources. Quinine was isolated from the bark of the cinchona tree. Morphine was isolated from the seed pods of poppies. Artemisinin was isolated from a Chinese plant. 199, 203
Page reference: Question 9
What is the term used for drugs that are similar in structure to a known drug and which are used for the same purpose?
Your answer: a) 'copycat' drugs Correct answer: b) 'me-too' drugs Feedback: The terms given in options a), c) and d) are not used in medicinal chemistry. 203
Page reference: Question 10
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?
Your answer: b) complexity of structure Feedback: Natural products are often complex in structure which makes their synthesis difficult. As a result, the synthesis of analogues can also be difficult. https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
3/5
4/1/2019
Page reference: 199
Oxford University Press | Online Resource Centre | Chapter 12
Question 11 Which of the following is not an endogenous lead compound?
Your answer: a) neurotransmitter Correct answer: b) alkaloid Feedback: Alkaloids are plant natural products containing nitrogen. The other options are endogenous compounds in the body. 199, 204-206
Page reference: Question 12
What is the term used for small molecules that bind to different regions of a binding site?
Your answer: a) epimers Correct answer: d) epitopes Feedback: The correct answer is epitopes. Epimers are diastereomers differing in their configuration at one asymmetric centre. Isomers are different structures having the same molecular formula. Isotopes are elements which have the same number of protons and electrons, but a different number of neutrons. 209-210
Page reference: Question 13
Which of the following statements is not true of herbal medicines?
Your answer: a) Herbal medicines may contain a range of active principles acting together to produce a beneficial effect. Correct answer: b) Herbal medicines have no side effects compared to conventional medicines. Feedback: There is no reason why herbal medicines should be free of side effects. They contain active components which will vary in their selectivity for their targets. Some will produce more side effects than others. 212-213
Page reference: Question 14
https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
4/5
4/1/2019
Oxford University Press | Online Resource Centre | Chapter 12
The following diagram illustrates the detection system known as surface plasmon resonance. What is represented by D?
Your answer: a) the evanescent wave Feedback: D is the evanescent wave which interacts with free oscillating electrons called plasmons in the metal film, when the angle of incidence (α) is correct. Symbol A represents a receptor which is covalently linked to the dextran matrix, and which will bind ligands present in the buffer flow. B is monochromatic plane-polarised light. C is the flow of buffer solution. 197-198
Page reference: Question 15
Which of the following is not an endogenous compound?
Your answer: a) dopamine Correct answer: d) desipramine Feedback: Endogenous compounds are any compounds occurring naturally in the body. Desipramine is a synthetic drug and is not an endogenous compound. 204-206
Page reference:
Copyright © Oxford University Press, 2016. All Rights Reserved.
https://global.oup.com/uk/orc/chemistry/patrick6e/student/mcqs/ch12/
5/5
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