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]]>7-Chloro-1,3-dihydro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
Diazepam is a benzodiazepine sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 284.74 g/mol |
2 | Physical appearance | Colorless to yellow crystalline compound |
3 | Melting point | 132°C |
4 | Octanol/water partition coefficient | 2.44 |
5 | Solubility | 1 gm in 2 ml of chloroform; 1 gm in 39 ml of ether. |
6 | Presence of ring | Diazepine, benzene |
7 | Number of chiral centers | Not present |
i. Diazepam binds with different receptors present in the brain and spinal cord.
ii. This increases the inhibitory effects of the GABA.
iii. GABA involves in sleep induction, control of hypnosis, memory, anxiety, epilepsy and neuronal excitability. [1]
i. 2-amino-5-chlorobenzophenone undergoes cyclocondensation with the ethyl ester of glycine hydrochloride produces 7-chloro-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one.
ii. Methylation of the above formed compound with dimethylsulfate leads to the formation of diazepam. [3]
Diazepam is used for:
Side effects of diazepam are:
MCQ
Q.1 Binding of Diazepam with acetylcholine muscarinic receptors results in?
a) agonizing effect on muscarinic receptors
b) Antagonizing effect on muscarinic receptors
c) Do not produce any significant effect
d) Do not bind with muscarinic receptor
Q.2 Therapeutic use of drug Diazepam is/are?
a) Treatment of Acute alcohol withdrawal
b) Treatment of seizures
c) Treatment of anxiety
d) All of the above
Q.3 Which amongst the following are the correct statements with respect to the SAR of drug Diazepam?
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 decrease the functional anxiolytic activity.
IV. When Heterocycles used as ring A, drug shows poor pharmacological activity.
a) I, IV
b) I, II, IV
c) I, II, III, IV
d) II, III, IV
Q.4 Type of ring structures present in the structure of diazepam?
a) Quiniclidine
b) Quinoline
c) Diazepine
d) All of the above
Q.5 Correct sequence for the True/False for the physiochemical properties of the drug solifenacin?
I. Molecular weight is 284.74 gm/mol
II. Colorless to yellow crystalline compound
III. Melting point is between 132°C
IV. Diazepine ring is present
a) TFTF
b) TTTT
c) FFFF
d)FFFT
Q.6 Correct statements for the IUPAC nomenclatures of the are?
I. Solifenacin: (3R)-1-Azabicyclo[2 2 2]oct-3-yl (1S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate
II. Zaleplon: N-(3-(3-cyanopyrazolo[1,5-a] pyrimidin-7-yl)phenyl)-N-ethylacetamide
III. Alprazolam: 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
IV. Diazepam: 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a] [1,4]benzodiazepine
a) II, IV
b) I, II
c) I, III, IV
d) I, II, III, IV
Q.7 Match the following drugs with their correct classifications-
i. Solifenacin | A. Barbiturate sedative-hypnotic |
ii. Thiobarbital | B. Benzodiazepine sedative-hypnotic |
iii. Diazepam | C. Acetylcholine antagonist |
iv. Zaleplon | D. Nonbenzodiazepine sedative-hypnotic |
a) i-C, ii-A, iii-B, iv-D
b) i-B, ii-C, iii-A, iv-D
c) i-D, ii-A, iii-C, iv-B
d) i-A, ii-C, iii-B, iv-D
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1-d
2-d
3-c
4-c
5-b
6-b
7-a
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