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(S)-(−)-5-Methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-3H-benzoimidazole
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 345.4 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 155 oC |
4 | Solubility | Very soluble in water |
5 | Octanol/water partition coefficient | 0.6 |
5 | Presence of ring | Imidazole, pyridine |
6 | Number of chiral centers | Not present |
General structure activity of Heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]Pyridine derivatives acting as acid pump antagonists can be summarized as:
Large scale asymmetric synthesis of esomeprazole can be done by following method:
i. The suspension of pyrmeprazole in toluene is added to water solution of (S, S)-diethyl tartrate and titanium tetraisopropoide.
ii. N, N-diisopropylehylamine and cumene hydroperoxide are added.
iii. Sodium salt is obtained using sodium hydroxide and acetonitrile.[2]
Esomeprazole is used for treatment of:
Side effects of Esomeprazole are:
Q.1 Match the following with correct SAR of the Heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]Pyridine derivative acid-pump antagonists:
i. Increasing the hydrophobic value | A. Increases the activity |
ii. Increasing the GTCI value | B. Decreases the activity |
C. Increases the activity | |
D. Decreases the activity |
a) i-A, ii-C
b) i-A, ii-D
c) i-B, ii-C
d) i-B, ii-D
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) TFFT
b)TFFF
c) TTTT
d) FFFF
Q.3 Molecular weight of Esomeprazole is?
a) 453 gm/mol
b) 432.0 gm/mol
c) 187.4 gm/mol
d) 345.4 gm/mol
Q.4 Esomeprazole acts on which system?
a) Sodium potassium pump
b) The respiratory system
c) H+/K+ ATPase pump
d) All of the above
Q.5 Which amongst the following is not a therapeutic use of drug Esomeprazole?
a) GERD
b) Erosive esophagitis
c) Itching
d) Heart burn symptoms
Q.6 Which of the following drug and their classification are correct?
I. Esomeprazole: Proton pump inhibitor
II. Meprilcaine: Local anesthetics
III. Rabeprazole: Diuretics
III. Quinidine: Anti-arrhythmic drug
a) I, III
b) II, III, IV
c) III, IV
d) I, II, IV
Q.7 Number of chiral carbons present in the structure of Esomeprazole?
a) 0
b) 3
c) 4
d) 5
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1-b
2-d
3-d
4-c
5-c
6-d
7-a
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