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]]>7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione
Quazepam is a benzodiazepine sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 386.8 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 137.5-139°C |
4 | Octanol/water partition coefficient | 4.03 |
5 | Solubility | 2.31e-03 g/L |
6 | Presence of ring | Diazepine, benzene |
7 | Number of chiral centers | 1 |
i. Quazepam binds nonspecifically with benzodiazepine receptors BNZ1.
ii. It coupled with GABAA receptors and increases the GABA affinity for the GABA receptor.
iii. This results in opening of the chloride channel and thus, causes hyperpolarization of the cell membrane which prevents further excitation of the cell.
i. (2-amino-5-chlorophenyl)(2-fluorophenyl)methanone reacts with 2,2,2-trifluoroethyl trichloromethanesulfonate to give (2-(2,2,2-trifluoroethylamino)-5-chlorophenyl) (2-fluorophenyl)methanone.
ii. Compound reacts with 2-bromoacetylchloride followed by reaction with isoindoline-1,3-dione and hydrazine to give an unstable compound which on further reaction with phosphorus pentasulfide give quazepam.
Quazepam is used for:
Side effects of Quazepam are:
MCQ
Q.1 Correct statements related with the physicochemical properties of drug quazepam?
I. Molecular weight = 386.8 gm/mol
II. Physical appearance: Solid
III. Melting point: 137K
IV. Triazole ring present
a) I, III
b) II, IV
c) I, II
d) I, II, IV
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Quazepam | A. 8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine |
ii. Epinephrine | B. 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione
|
iii. Norepinephrine | C. (R)-4-(2-amino-1-hydroxyethyl)benzene-1,2-diol |
iv. Estazolam | D. (R)-4-(1-Hydroxy-2-(methylamino)ethyl)benzene-1,2-diol
|
a) i-B, ii-C, iii-A, iv-D
b) i-A, ii-C, iii-B, iv-D
c) i-D, ii-A, iii-C, iv-B
d) i-B, ii-D, iii-C, iv-A
Q.3 Correct steps for the mechanism of action of the drug Quazepam?
I. Binds with BNZ1 receptors
II. Increase in GABA affinity for GABA receptors
III. Opening of chloride channel
IV. Hyperpolarisation
a) I – II – III – IV
b) II – I – III – IV
c) III – I – II – IV
d) II – IV – III – I
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFTF
b) FFTF
c) TFFF
d) FTFT
Q.5 Introduction of the electronegative group at 7-position of the ring A of drug quazepam leads to?
a) Decrease in lipophyllicity
b) Increase in lipophyllicity
c) Increase in anxiolytic property
d) Decrease in anxiolytic property
Q.6 The correct sequence for the steps for synthesis of drug quazepam from (2-amino-5-chlorophenyl)(2-fluorophenyl)methanone is?
I. Reaction with isoindolin-1,3-dione and hydrazine
II. Reaction with phosphorous pentasulfde
III. Reaction with 2-bromo aetylchloride
IV. Reaction with 2,2,2-trifluoroethyl trichloromethylsulfonate
a) IV – III – I – II
b) I – II – III – IV
c) I – III – IV – II
d) IV- II – III –I
Q.7 Side effect of drug quazepam?
a) Anxiety
b) Loss of coordination
c) Blurred vision
d) All of the above
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1-c
2-d
3-a
4-c
5-c
6-a
7-d
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