Medicinal Chemistry - - Unit 11 - Week 8 https://onlinecourses-archive.nptel.ac.in/noc19_...

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Unit 11 - Week 8
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Certification exam Assignment 8
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Course As per our records you have not submitted this Due on 2019-03-27, 23:59 IST.
outline
assignment.

How to access 1) The structure of a calcium channel blocker called Glipine is shown 1 point
the portal below. The functional groups highlighted in the box are potential van der
waals binding groups
About IISER
Pune

Pre-Requisite
True
Assignment
False
Week 1
No, the answer is incorrect.
Week 2 Score: 0
Accepted Answers:
Week 3 True
2) Extension tactics are often used to find the extra hydrophilic regions 1 point
Week 4
in the binding site by adding various alkyl or aryl-alkyl groups
Week 5
True
Week 6 False

Week 7 No, the answer is incorrect.

Score: 0
Week 8 Accepted Answers:
False
Optimizing
Drug-Target 3) The term “Me too drugs” are used for drugs that are similar in 1 point
Interactions
structure to a known drug and which are used for the different purpose
Part-I

Optimizing True
Drug-Target
Interactions False
Part-II
No, the answer is incorrect.
Optimizing Score: 0
Drug-Target
Accepted Answers:
Interactions © 2014 NPTEL - Privacy & Terms - Honor Code - FAQs -
Part-III False
A project of In association with
Optimizing 4) Primary and secondary amines act as both hydrogen bond donor and 1 point
Drug-Target acceptor whereas tertiary amines are only hydrogen bond acceptor
Interactions
Part-IV Funded by
True

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Medicinal Chemistry - - Unit 11 - Week 8 https://onlinecourses-archive.nptel.ac.in/noc19_...

Tutorial 12 FalsePowered by
Quiz :
No, the answer is incorrect.
Assignment 8
Score: 0
Week 8 Accepted Answers:
Feedback Form
True
Week 9 5) Replacement of the imidazole ring (in Structure I) with 1,2,4 triazole 1 point
ring (in UK 46245) is shown below. This resulted in decreased selectivity
Week 10
against the fungal form of the enzyme
Week 11

Week 12
True
Download False
videos
No, the answer is incorrect.
TRANSCRIPTS Score: 0
Accepted Answers:
Interaction False
Session
6) The isosteres of oxygen are S, NH and CH 2 1 point

True
False
No, the answer is incorrect.
Score: 0
Accepted Answers:
True
7) An anti-hypertensive agent Cilazaprilat was developed by varying 1 point
the ring size from six-membered ring to seven-membered ring helps with
improved binding

True
False
No, the answer is incorrect.
Score: 0
Accepted Answers:
True
8) Incorporation of fluorine as an isostere of hydrogen in antitumor drug 1 point
5-fluorouracil activates thymidylate synthase enzyme

True
False
No, the answer is incorrect.
Score: 0
Accepted Answers:
False
9) The inhibition of 17β-hydroxysteroid dehydrogenase type 1 enzyme 1 point
is useful in the treatment of estradiol-dependent tumors as the levels of
estradiol present in the body would be lowered

True
False

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Medicinal Chemistry - - Unit 11 - Week 8 https://onlinecourses-archive.nptel.ac.in/noc19_...

No, the answer is incorrect.

Score: 0
Accepted Answers:
True
10)The antipsychotic agent Sultopride is a non-selective D 2 and D3 1 point
receptor antagonist. DU 122290 was designed by employing a simplification
strategy to increase the activity and selectivity towards the D 3 receptor over
the D2 receptor

True
False
No, the answer is incorrect.
Score: 0
Accepted Answers:
False
11)The structure of Pronethalol is illustrated below. Which of the 1 point
following statements is true?

It is a selective due to larger van der waals binding area for the
aromatic region in the β- receptor than the α-receptor
Naphthalene ring system is sterically too big for α-receptor
It is a selective β blocker
All of the above
No, the answer is incorrect.
Score: 0
Accepted Answers:
All of the above
12)An example of structural modification which would increase the 1 point
lipophilicity of the molecule is

Adding a hydroxyl group (R-OH) to the molecule

Converting a hydroxyl group (R-OH) to an ether (R-O-R)
Converting a hydroxyl group (R-OH) to a carboxylic acid (R-COOH)
Adding and amino group (R-NH2) to a molecule

No, the answer is incorrect.

Score: 0
Accepted Answers:
Converting a hydroxyl group (R-OH) to an ether (R-O-R)
13)The structure A has a highly flexible side chain. Which of the 1 point
following statements is true?

A flexible molecule is more likely to be in active conformation when it

approaches its target binding site which results in increased activity
A flexible molecule is more likely to adopt conformations that will bind
to different targets, resulting in side effects

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Medicinal Chemistry - - Unit 11 - Week 8 https://onlinecourses-archive.nptel.ac.in/noc19_...

A flexible molecule is more likely to show target selectivity

A flexible molecule may be able to bind to its target binding site in
different binding modes, resulting in an increase in activity
No, the answer is incorrect.
Score: 0
Accepted Answers:
A flexible molecule is more likely to adopt conformations that will bind to
different targets, resulting in side effects
14)The lead compound (structure A) was identified as dual serine 1 point
threonine kinase and tyrosine kinase inhibitor by random screening of large
compound libraries. A selective tyrosine kinase inhibitor (structure B) was
designed by introducing a methyl group in the ortho position, forcing the
molecule to adopt a conformation which suited only binding to tyrosine
kinases. Which of the following strategies was used in the design of structure
B?

Simplification
Extension
Conformational blocker
Rigidification
No, the answer is incorrect.
Score: 0
Accepted Answers:
Conformational blocker
15)Which of the intermolecular bonding interactions below are possible 1 point
for an alkene?

Vander waals interactions only

Hydrogen bonding only
Ionic bonding only
Both ionic bonding and hydrogen bonding
No, the answer is incorrect.
Score: 0
Accepted Answers:
Vander waals interactions only
16)Structure A is an antihypertensive agent which acts by inhibiting the 1 point
enzyme angiotensin converting enzyme (ACE). Structure B was designed to
bind to the binding site more strongly and to have greater activity

Which of the following strategies was used in the design of structure

B?

Simplification
Use of an isostere
Rigidification
Extension
No, the answer is incorrect.

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Medicinal Chemistry - - Unit 11 - Week 8 https://onlinecourses-archive.nptel.ac.in/noc19_...

Score: 0
Accepted Answers:
Extension

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