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]]>N,N-Dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide hemitartrate
Zolpidem is a nonbenzodiazepine GABAA agonist
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 307.4 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 196°C |
4 | Octanol/water partition coefficient | 3.02 |
5 | Solubility | 23 mg/ml |
6 | Presence of ring | Imidazopyridine, benzene |
7 | Number of chiral centers | Not present |
i. Reaction of 2-amino-5-methylpyridine (1) with 2-bromo-4-methylacetophenone (2) to give imidazopyridine (3).
ii. (3) undergoes aminomethylation to form amine (4)
iii. (4) is methylated with methyliodide and leads to formation of quaternary ammonium salt (5).
iv. Reaction of (5) with sodium cyanide produces nitrile (6).
v. (6) on acidinc hhydrolysis gets convert into corresponding acid chloride which on heating with dimethylamine produces zolpidem. [2]
Zolpidem is used for:
Side effects of Zolpidem are:
Q.1 What can be the correct IUPAC nomenclature of Zolpidem?
a) (S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
b) (S)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol.
c) 7-Chloro-2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid
d) N,N-Dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide hemitartrate
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Zolpidem?
I. Ring A should include an aromatic or heteroaromatic ring for binding with 5-phenyl-1,4-benzodiazepin-2-one derivatives.
II. An electronegative group at 7-position of the ring A increases the functional anxiolytic activity.
III. Substitutions at 6, 8 or 9 position with electronegative group on ring A will increase the functional anxiolytic activity.
IV. When Heterocycles used as ring A, drug shows poor pharmacological activity.
a) I, II
b) III
c) III, IV
d) II
Q.3 Corrects sequence of the steps involved in the synthesis of Zolpidem from 2-amino-5-methylpyridine?
I. Aminomethylation
II. Methylation
III. Reaction with 2-bromo-4-methylacetophenone
IV. Acidic hydrolysis
V. Reaction with sodium cyanide
a) III- II – I- IV – V
b) II – I – III- IV – V
c) III – I – II – V – IV
d) I – III – II- V – IV
Q.4 Side effects of drug Zolpidem is/are?
a) Hallucinations
b) Dizziness
c) Depression
d) All of the above
Q.5 Match the following drugs with their correct molecular weights-
i. Darifenacin | A.426.5 gm/mol |
ii. Tolterodine | B.307.4gm/mol |
iii. Chlorazepate | C. 325.5 gm/mol |
iv. Zolpidem | D. 314.72 gm/mol |
a) i-C, ii-B, iii-A, iv-D
b) i-C, ii-B, iii-D, iv-A
c) i-A, ii-C, iii-D, iv-B
d) i-B, ii-A, iii-D, iv-C
Q.6 An example of drug from class nonbezodiazepine sedative hypnotic?
a) Methysergide
b) Zolpidem
c) Amphetamine
d) Tolterodine
Q.7 The type of ring system found in the structure of Chlorazepate?
a) Dihydrobenzofurane
b) Pyrrolopyrimidine
c) Imidazopyridine
d) Pyrrolopyrrole ring
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1-d
2-b
3-c
4-d
5-c
6-b
7-c
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