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]]>11-(1-Methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 290.4 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 152-154oC |
4 | Solubility | Very Soluble |
5 | Octanol/water partition coefficient | 3.59 |
5 | Presence of ring | Piperidine ring |
6 | Number of chiral centers | Not present |
General structure activity of first generation H1-receptors antagonist can be summarized as:
i. Phenylacetonitrile reacts with ethyl nicotinate in presence of sodium ethoxide to give 3-oxo-2-phenyl-3-(pyridin-3-yl)propanenitrile.
ii. The reaction of the last with hydrogen bromide produces 2-phenyl-1-(pyridin-3-yl)ethanone.
iii. The above formed compound is reacted with hydrazine in presence of sodium hydroxide in diethylene glycol to get 2-phenethylpyridine.
iv. On treatment of last with hydrogen peroxide in acetic acid produces an intermediate which on reaction with dimethyl sulfate followed by sodium cyanide in water gives 3-phenethylpyridine-2-carbonitrile.
v. The above formed compound is reacted with 1-methyl-4-piperidyl-magnesium chloride in aqueous hydrochloric solution to give (1-methylpiperidin-4-yl) (3-phenethylpyridin-2-yl) methanone.
vi. Azatadine is produced by reacting last with phosphoric acid. [1]
Azatadine is used for treatment of:
Side effects of Azatadine are:
Q.1 Correct statements from the following related with the physicochemical properties of drug Azatadine are?
I. Molecular weight: 350.2 gm/mol
II. Appearance: Solid
III. Melting Point: 105.5oC
IV. Solubility: Very soluble
a) I, II, IV
b) I, III, IV
c) II, IV
d) I, II, III, IV
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Azatadine | A. (RS)-6-(Difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methylsulfinyl]-1H-benzo[d]imidazole |
ii. Dimethindene | B. N,N-Dimethyl-2-[3-(1-pyridin-2-ylethyl)-1H-inden-2-yl]ethan-1-amine |
iii. Famotidine | C. 3-[({2-[(diaminomethylidene)amino]-1,3-thiazol-4-yl}methyl)sulfanyl]-N-sulfamoylpropanimidamide |
iv. Pentoprazole | D. 11-(1-Methylpiperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine |
a) i-D, ii-B, iii-C, iv-A
b) i-A, ii-B, iii-D, iv-C
c) i-B, ii-C, iii-A, iv-D
d) i-A, ii-C, iii-D, iv-B
Q.3 Mechanism of action of drug azatadine involves?
I. Competes for histamine at HA-receptor
II. Blocks α-adrenoceptors
III. Alkylation of DNA
a) I, III
b) I, IV
c) I, II, III
d) I
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFTF
b) TTFF
c) FFTF
d) TFFT
Q.5 Terminal nitrogen in the structure of first generation H1-receptor antagonist should be in which form?
a) Primary
b) Secondary
c) Tertiary
d) Quaternary
Q.6 Type of rings present in the structure of Azatadine?
I. Pyridine
II. Piperazine
III. Piperidine
IV. Benzodiazepine
a) I, IV
b) I
c) II, III
d) II
Q.7 Side effect of drug Azatadine is/are?
a) Difficulty urination
b) Sleepiness
c) Enlarged prostate
d) All of the above
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1-c
2-a
3-d
4-b
5-c
6-d
7-d
18.3.1965).
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