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Flashcards in Med Chem Test 1 Deck (29)
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1

The structure Endothelin-1 contains two ____ bonds between two____ amino acids. 

A. Covalent, Threonine

B. Ionic, Cysteine 

C. Disulfide, Cysteine

D. Hydrogen, Cysteine

 

C

2

ET-1 concentrations are ____ in patients presenting with PAH, leading to increased _____

A. Increased, Vasoconstriction

B. Increased, Vasodilation

C. Decreased, Vasoconstriction

D. Decreased, Vasodilation

A

3

In the structure of Bosentan (Tracleer) the following functional group undergoes _____ through the enzyme _____

A. Oxidation, 2C9

B. Hydrolysis, 2C9

C. O-demethylation, 2C9

D. Methylation, 2C9

C

4

In the structure Bosentan (Tracleer) the circiled group undergoes ____ in order to produce the ___ metabolite

A. Hydroxylation, Inactive

B. Hydroxylation, Active

C, Reduction, Inactive

D. Reduction, Active

B

5

Which of the following statments is true regarding Bosentan?

A. Hydroxylation at the red portion will create a minor inactive metabolite

B. O-demethylation at the blue portion will create a minor inactive metabolite

C. Hydroxylation at the red portion will create a major active metabolite

D. The drug can have a metabolite that undergoes both hydroxylation and demethylation. 

E. The majority of Bosentan's activity is done by the parent unmetabolized molecule and 20% comes from the active metabolite. 

B, C, D, E

6

What are the functional groups circled here?

A. Red: Pyrimidine, Blue: Sulfonamide

B. Red: Sulfonamide, Blue: Pyrimidine

C. Red: Sulfonamide, Blue: Pyradine

D. Red: Sulfamide, Blue: Pyrimidine

B

7

What is the major possible side effect of Bosentan?

A. Liver Injury & Tetratogenicity

B. Kidney failure

C. Anaphylaxis 

D. CNS damage

A

8

Of the following drugs which of them is specific for ET-1 A type receptors?

A. Bosentan (Tracleer)

B. Macitentan (Opsumit)

C. Riosiguat (Adempas)

D. Ambrisentan (letaris)

D

9

Based on the structure of Ambrisenten, the blue group is a _____ and the red group is a _____

A. Carboxylic Acid, Pyradine

B. Ester, Pyrimidne

C. Carboxylic Acid, Pyrimidne

D. Ester, Pyradine

C

10

What statements about Ambrisentan are true? (Select All)

A. Contains a carboxylic acid and Pyrimidine functional group

B. Has a much higher affinity for ET-1 B receptors than ET-1 A receptors. 

C. Has a possible chance to cause Liver injury and tetratogenicity

D. Has the potential to become soluble at lower pHs due to having a low pKa of 4

E. has the potential to become more soluble at higher pHs due to having a low pKa of 4

A, C, E

11

What kind of reaction can this functional group in ambrisentan undergo?

A. Acyl-Glucuronidation

B. Esterification

C. Ester hydrolysis

D. Reduction

A

12

What kind of reaction can this group in Ambrisentan undergo?

A. Reduction

B. Hydroxylation

C. O-Demethylation

D. COMT

C

13

What kind of reaction can this group undergo in ambrisentan?

A. Reduction

B. Ester hydrolysis

C. Ether hydrolysis 

D. Esterification

C

14

The two methyl groups can undergo ____ and then undergo a second reaction known as ____

A. COMT, Glucuronidation

B. Hydroxylation, Glucuronidation

C. COMT, Sulfation

D. Hydroxylation, Sulfation 

B

15

The following structure of Macitentan (Opsumit) includes all of the following EXCEPT:

A. Sulfonamide

B. Halogen

C. Pyrimidine

D. Ether

E. Sulfamide

A

 

Do not get the sulfonamide group confused with the sulfamide group. Sulfonamide only has one nitrogen and sulfamide has 2.

16

Which of the following drugs is non-selective to ET-1 A and ET-1 B receptors? (Select All)

A. Ambrisentan (Letairis)

B. Macitentan (Opsumit)

C. Bosentan (Tracleer)

D. Tadalafil 

B,C

17

Macitenten undergoes ____ to form an ____ metabolite 

A. N-dealkylation, Inactive

B. N-dealkylation, Active

B

18

Nitric oxide ____ sGC in order to ____ levels of cGMP and promote muscle _____

A. Activates, Increase, Relaxation

B. Activates, Increase, Contraction

C. Deactivates, Decrease, Relaxation

D. Deactivates, Decrease, Contraction

A

19

When nitric oxide is placed in an _____ environment it will form the _____ which is capable of the shift in bonds known as  _____

A. Aqueous, Nitrous Ion, Resonance

B. Aqueous, Nitrate Ion, Metabolism

C. Aqueous, Nitrate Ion, Resonance

D. Hydrophibic, Nitrate Ion, Resonance

C

20

What enzyme is sildenafil blocking that is preventing cGMP from being converted into GMP?

A. PDE

B. GLUT

C. SULT

D. sGC

A

21

The boxed structure of Sildenafil is a ____ and is thus known as a ____.

A. Pyrimadine, Pyrimadine derivative

B. Indole, Indoline derivative

C. Pyrazole, Pyrazoline derivative

D. Purine, Purine derivative

D

22

All of the following statments are true about Sildenafil Citrate (Revatio) EXCEPT:

A. Sildenafil is a PDE5 inhibitor

B. Undergoes extensive presystemic metabilism (intestinal and first pass metabolism)

C. Keeps cAMP levels high within the muscle to promote muscle relaxation

D. Sildenafil is a purine derivative

C

 

Sildenafil keeps cGMP levels elevated not cAMP.

23

Which of the following statments is true regarding the metabolism of sildenafil?

A. Sildenafil undergoes N-dealkylation to produce an N-desmethyl metabolite

B. Sildenafil's N-desmethyl metabolite is 50% as potent as the parent compound. 

C. The vast majority of sildenafil's activity comes from the parent compound. 

D. All of the above

D

24

What two reactions can metabolite of tadalafil undergo? (Select All)

A. SULT

B. COMT

C. O-Gluc

D. Hydroxylation

B, C

25

Which of the following hydroxyls can undergo COMT metabolism? 

A. Red

B. Blue

A

26

What kind of CYP3A4 reaction is occuring here?

A. O-Demethylation

B. Ether Hydrolysis

C. Ester Hydrolysis

D. Oxidation

A

27

Which hydroxyl group can undergo O-Glucuronidation?

A. Red

B. Blue

C. Both

C

28

T/F Metabolites formed by Tadalafil are all inactive

 

T

29