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Org Chem PACOP > 101-150 > Flashcards

101-150 Flashcards

1
Q

Which substituent of chloramphenicol is responsible for its toxic effect?
a. The nitro group
b. The 2 alcohol groups
c. The dichloroacetamide group
d. The aromatic ring
e. A and B only

A

A and B only

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2
Q

Which of the following statements is correct regarding Erythromycin?
I. Erythromycin binds to the 50s subunit of bacterial ribosomes
II. When administered together with chloramphenicol, their bacteriostatic effect will increase.
III. The ketone and 2 alcohol groups in its structure are responsible for its acid sensitivity.
IV. Increasing the size of the macrocycle to a 16 membered ring can increase the acid stability of the molecule.

A

I, II, III, IV

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3
Q

Amantadine is one of the earliest antiviral drugs used clinically against flu. Which of the following statements is correct regarding amantadine?
I. Amantadine is an adamantine related to rimantadine.
II. It inhibits the penetration and uncoating of the influenza virus.
III. It can inhibit replication of the influenza virus by blocking a viral ion channel called matrix (M2) protein
IV. At high concentrations, it can alter pH of endosomes and prevent the acidic environment required by the hemagglutinins to fuse the viral membrane with that of the endosome.

A

I, II, III, IV

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4
Q

Which among the given structures can be intercalating agent which can slide between the base pairs of the DNA double helix and thereby can inhibit the enzymes involved in the replication and transcription processes?
a. Structure I
b. Structure II
c. Structure III
d. Structure IV
e. II and III

A

Structure I

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5
Q

Which among the given structures is an antimetabolite that can inhibit the enzymes involved in the synthesis of DNA or its nucleotide building blocks?
a. Structure I
b. Structure II
c. Structure III
d. Structure IV
e. II and III

A

Structure IV

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6
Q

Which of the given structures can form strong covalent bonds with the nucleophilic groups on
DNA which can eventually result to cross-linking of strands?
a. Structure I
b. Structure II
c. Structure III
d. Structure IV
e. II and III

A

II and III

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7
Q

Which of the given structures can be classified as an alkylating agent?
a. Structure I
b. Structure II
c. Structure III
d. Structure IV
e. II and III

A

II and III

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8
Q

A semi-synthetic analogue of camptothecin given intravenously and is a prodrug used in combination with fluorouracil and folinic acid for the treatment of advanced colorectal cancer.
a. Oblimersen
b. Calicheamicin
c. Carboplatin
d. Irinotecan
e. Cyclophosphamide

A

Irinotecan

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9
Q

An antisense drug designed to inhibit the mRNA molecules that code for proteins which suppress apoptosis.
a. Oblimersen
b. Calicheamicin
c. Carboplatin
d. Irinotecan
e. Cyclophosphamide

A

Oblimersen

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10
Q

A natural product that reacts with nucleophiles to produce diradical species. Its reaction with DNA ultimately leads to cutting of the DNA chains.
a. Oblimersen
b. Calicheamicin
c. Carboplatin
d. Irinotecan
e. Cyclophosphamide

A

Calicheamicin

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11
Q

It is the most commonly used alkylating agent in cancer chemotherapy, the metabolism of which produces arcolein which is toxic to the bladder and kidneys.
a. Oblimersen
b. Calicheamicin
c. Carboplatin
d. Irinotecan
e. Cyclophosphamide

A

Cyclophosphamide

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12
Q

An alkylating agent that can cause intrastrand cross-linking preferred over cisplatin for the
intravenous treatment of advanced ovarian tumors because of its less severe side effects.
a. Oblimersen
b. Calicheamicin
c. Carboplatin
d. Irinotecan
e. Cyclophosphamide

A

Carboplatin

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13
Q

Which of the following drugs is not an alkylating agent used in cancer chemotherapy?
a. Carmustine
b. Busulfan
c. Procarbazine
d. Mitomycin C
e. None of the choices

A

None of the choices

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14
Q

A thiopurine prodrug which is converted to its corresponding monophosphate that inhibits purine synthesis.
a. Methotrexate
b. 5-fluorouracil
c. 6-mercaptopurine
d. Pentostatin
e. Cytarabine

A

6-mercaptopurine

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15
Q

An antimetabolite that is very similar in structure to the natural folates differing only in additional
amino and methyl groups. It inhibits the enzyme dihydrofolate reductase which is responsible in
maintaining levels of the enzyme cofactor tetrahydrofolate.
a. Methotrexate
b. 5-fluorouracil
c. 6-mercaptopurine
d. Pentostatin
e. Cytarabine

A

Methotrexate

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16
Q

This drug acts as a prodrug for a suicide inhibitor. It is converted in the body to the fluorinated analogue of 2’deoxyuridylic acid monophosphate which then combines with the enzyme thymidylate
synthase and the cofactor.
a. Methotrexate
b. 5-fluorouracil
c. 6-mercaptopurine
d. Pentostatin
e. Cytarabine

A

5-fluorouracil

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17
Q

An anti-leukemia drug isolated from Streptomyces antibioticus and is a powerful inhibitor of Adenosine deaminase.
a. Methotrexate
b. 5-fluorouracil
c. 6-mercaptopurine
d. Pentostatin
e. Cytarabine

A

Pentostatin

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18
Q

A prodrug analogue of 2’deoxycytidine which inhibits DNA polymerases.
a. Methotrexate
b. 5-fluorouracil
c. 6-mercaptopurine
d. Pentostatin
e. Cytarabine

A

Cytarabine

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19
Q

Which of the following pairs is correctly matched?
I. Glucocorticoids: Megestrol acetate
II. Progestins: prednisone
III. Estrogens: Diethylstilbestrol
IV. Androgens: Fluoxymesterone

A

III, IV

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20
Q

A decapeptide analogue of the luteinizing hormone – releasing hormone designed to be more resistant to peptidase degradation.
a. Goserelin
b. Raloxifene
c. Cyproterone acetate
d. Anastrazole
e. 4-hydroxyandrostenedione

A

Goserelin

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21
Q

A reversible competitive inhibitor of the enzyme aromatase , the design of which is based on structure of amino gluthetimide.
a. Goserelin
b. Raloxifene
c. Cyproterone acetate
d. Anastrazole
e. 4-hydroxyandrostenedione

A

Anastrazole

22
Q

This mode of therapy involves an antibody which has catalytic activity designed to activate a prodrug.
a. Antibody-directed enzyme prodrug therapy (ADEPT)
b. Antibody-directed abzyme prodrug therapy (ADAPT)
c. Gene-directed enzyme prodrug therapy (GDEPT)
d. Photodynamic therapy
e. All of the above

A

Antibody-directed abzyme prodrug therapy (ADAPT)

23
Q

This mode of therapy involves the delivery of a gene that codes for an enzyme capable of activating an anticancer prodrug into a cancer cell.
a. Antibody-directed enzyme prodrug therapy (ADEPT)
b. Antibody-directed abzyme prodrug therapy (ADAPT)
c. Gene-directed enzyme prodrug therapy (GDEPT)
d. Photodynamic therapy
e. All of the above

A

Gene -directed enzyme prodrug therapy (GDEPT)

24
Q

This involves irradiation of tumors containing porphyrin photosensitizers resulting to the
production of reactive oxygen species which are fatal to the cell.
a. Antibody-directed enzyme prodrug therapy (ADEPT)
b. Antibody-directed abzyme prodrug therapy (ADAPT)
c. Gene-directed enzyme prodrug therapy (GDEPT)
d. Photodynamic therapy
e. All of the above

A

Photodynamic therapy

25
Q

This therapy involves an antibody-enzyme conjugate that is targeted to specific cancer cells.
Once the antibody has become attached to the outer surface of cancer cells, a prodrug is administered which is activated by the enzyme at the tumor site.
a. Antibody-directed enzyme prodrug therapy (ADEPT)
b. Antibody-directed abzyme prodrug therapy (ADAPT)
c. Gene-directed enzyme prodrug therapy (GDEPT)
d. Photodynamic therapy
e. All of the above

A

Antibody-directed enzyme prodrug therapy (ADEPT)

26
Q

Which of the following statements is true regarding acetylcholine?
I. It is very useful in treating such conditions that require it because it can be readily synthesized in the laboratory.
II. It is easily hydrolyzed in the stomach by acid catalysis and cannot be given orally.
III. It is administered intravenously as it is stable in blood because of the absence of enzymes such as esterases.
IV. There is no selectivity of action upon administration of acetylcholine.

A

II, IV

27
Q

Which part of the acetylcholine structure can be altered without decreasing its activity on cholinergic receptors?
a. The quaternary nitrogen
b. The ester functional group
c. The ethylene bridge between the ester and nitrogen
d. All of the above
e. None of the choices

A

None

28
Q

Which part of the acetylcholine structure is essential for activity?
a. The quaternary nitrogen
b. The ester functional group
c. The ethylene bridge between the ester and nitrogen
d. All of the above
e. None of the choices

A

All

29
Q

Which of the following statements is incorrect regarding the structure-activity relationship of
acetylcholine?
a. Replacing the nitrogen atom with a neutral carbon atom increases the activity
b. The overall size of the molecule cannot be altered greatly.
c. There must be two methyl groups on the nitrogen.
d. A and B
e. B and C

A

Replacing the nitrogen atom with a neutral carbon atom increases the activity

30
Q

Which of the following statements is true regarding acetylcholine analogues?
a. Addition of steric shield in the ethylene bridge renders resistance to chemical and enzymatic
hydrolysis
b. Changing the ester to a carbamate increases resistance to hydrolysis
c. Changing the ester to a carbamate makes it selective to muscarinic receptor
d. A and B
e. B and C

A

A and B

31
Q

Which of the given structures is more stable to acid hydrolysis than acetylcholine?
a. I
b. II
c. III
d. I & II
e. All of the above

A

All of the above

32
Q

Which of the given structures is more selective to muscarinic receptor than nicotinic receptor?
a. I
b. II
c. III
d. I & II
e. All of the above

A

I & II

33
Q

Given below is the general structure of muscarinic antagonists which was mostly based on the structure of atropine. Which of the following statements is true regarding the structural features of muscarinic antagonists?
a. The alkyl group on nitrogen can be larger than methyl
b. The nitrogen can be tertiary or quaternary
c. Very large acyl groups (R1 and R2) are allowed
d. A and B only
e. All of the above

A

All of the above

34
Q

Physostigmine is a carbamate inhibitor of the enzyme acetylcholinesterase which was first isolated from Physostigma venenosum. Which of its functional group/s is/are essential for its activity?
a. Carbamate group
b. Benzene ring
c. Pyrrolidine ring
d. A and C only
e. All of the above

A

All

35
Q

Which part of the catecholamine is not important in the binding site interactions?
a. The 2 phenolic groups
b. Secondary alcohol
c. Ionized amine
d. The aromatic ring
e. A and B only

A

aromatic ring

36
Q

Which part of the catecholamine structure is involved in Van der Waals interactions?
a. The 2 phenolic groups
b. Secondary alcohol
c. Ionized amine
d. The aromatic ring
e. A and B only

A

The 2 phenolic groups

37
Q

Which part of the catecholamine structure is involved in ionic binding to the receptor site?
a. The 2 phenolic groups
b. Secondary alcohol
c. Ionized amine
d. The aromatic ring
e. A and B only

A

Ionized amine

38
Q

Which part of the catecholamine structure is involved in H-bonding to the receptor binding site?
a. The 2 phenolic groups
b. Secondary alcohol
c. Ionized amine
d. The aromatic ring
e. A and B only

A

A and B

39
Q

Which of the following modifications to the catecholamine structure can increase alpha-2
receptor activity?
a. Increasing the size of N-alkyl substituent
b. Addition of an alpha methyl group
c. Removal of the phenolic groups
d. A and B only
e. B and C only

A

Addition of an alpha methyl group

40
Q

Which of the following modifications to the catecholamine structure can increase the selectivity for beta receptors?
a. Increasing the size of N-alkyl substituent
b. Addition of an alpha-methyl group
c. Removal of the phenolic groups
d. A and B only
e. B and C only

A

Increasing the size of N-alkyl substituent

41
Q

Which of the following modifications to the catecholamine structure can result to a significant
drop in activity for the beta receptor?
a. Increasing the size of N-alkyl substituent
b. Addition of an alpha methyl group
c. Removal of the phenolic groups
d. A and B only
e. B and C only

A

Removal of the phenolic groups

42
Q

Which of the following statements is true about the SAR of aryloxypropranolamines?
a. A secondary amine is essential for activity.
b. The alcohol group on the side chain is essential for activity.
c. Substitution in the methylene bridge increases the activity.
d. A and B only
e. B and C only

A

A and B

43
Q

Which of the following is incorrect about the SAR of aryloxypropranolamines?
a. Variation of the aromatic ring is possible.
b. Heteroaromatic rings can be introduced to the system.
c. Substitution on the side chain methylene group increases metabolic stability.
d. Adding an N-arylethyl group is detrimental.
e. A, B, and C only

A

Adding an N-arylethyl group is detrimental.

44
Q

What is the clinical indication of aryloxypropranolamines?
a. Asthma
b. Hypertension
c. For cardiogenic shock
d. Obesity
e. All of the above

A

Hypertension

45
Q

Which of the following statements is/are true regarding the structural features required for the hypnotic activity of barbiturates? (refer to the structure of barbituric acid)

I. Replacement of sulphur for the carbonyl oxygen at carbon 2 results in quick onset and short duration of action.

II. Within the same series of barbituric acid derivatives, the branched chain isomer has greater activity and shorter duration. The greater the branching, the more potent the drug.

III. Within the same series of barbituric acid derivatives, the unsaturated allyl, alkenyl and cycloalkenyl analogues have greater potency than the saturated analogues with the same number of
carbon atoms.

IV. Methylation of one of the imide hydrogens (the transition from 5,5-disubstituted barbituric acid to 1,5,5-trisubstituted barbituric acid) increases onset and decreases duration of action.

A

I, II, III, and IV are correct

46
Q

Which of the following statements describe the ideal antiepileptic drug?

I. It should completely suppress seizures in doses that also cause sedation.

II. It should be well tolerated, highly effective against various types of seizures and devoid of
undesirable side effects on vital organs and functions

III. Its onset of action should be rapid after parenteral injection for control of status epilepticus.

IV. It should have a long duration of effect after oral administration for prevention of recurrent
seizures.

A

II, III, and IV are correct

47
Q

Which of the following correctly describes the barbiturate 5-ethyl-5-phenylbarbituric acid?
a. It is also known as Phenobarbital
b. The sedative-hypnotic effect of this drug limits its use in older children and adults
c. It exhibits anticonvulsant effects in doses that do not cause sedation.
d. A and B only
e. A and C only

A

A and B

48
Q

Which of the following statements correctly describe 2-ethyl-2-methylsuccinide?
a. It is widely accepted treatment of petit mal condition.
b. It can cause ataxia and gingival hyperplasia.
c. It is also known as Dilantin.
d. A and B only
e. B and C only

A

It is widely accepted treatment of petit mal condition.

49
Q

Which of the following statements correctly describe 5,5-diphenyl-2,4-imidazolidinedione?
a. It is widely accepted treatment of petit mal condition.
b. It can cause ataxia and gingival hyperplasia.
c. It is also known as Dilantin.
d. A and B only
e. B and C only

A

B and C

50
Q

Which of the following statements correctly describe the structure-activity relationship of tricyclic psychotropic drugs?
I. Optimal psychotropic activity is observed in ring systems that have a six-membered or
seven-membered central ring.
II. Dihenylalamine and Diphenylmethane derivatives that lack a central ring are devoid of
psychotropic activity.
III. Derivatives that contain a five-membered central ring lack psychotropic activity.
IV. Rigidly planar tricyclic diphenylmethane derivatives such as anthracene are inactive

A

I only

Org Chem PACOP (6 decks)

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