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]]>2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole.
Naphazoline is a α1-adenergic agonist.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 210.27 |
2 | Physical appearance | Solid |
3 | Melting point | 257°C |
4 | Solubility | Water solubility is 0.0381 mg / ml |
5 | Octanol/water partition coefficient | 3.88 |
6 | Presence of ring | Naphthalene and imidazoline rings present |
7 | Number of chiral centers | Not present |
R1 substitution:
R2 substitution:
R3 substitution on the aromatic ring:
i. (1-naphthyl)acetonitrile reacts with ethanol to give an iminoester.
ii. The iminoester undergoes cyclization reaction when reacts with ethylinediamine to give naphazoline.
Naphazoline is used as a degongestant.
Some of the side effects of naphazoline are
Q.1 Correct statements for the Naphazoline drug are?
I. Molecular weight is 210.27gm/mol
II. Water solubility is 31 mg/ml
III. Present as yellow oily liquid at room temperature.
IV. Octanol/water partition coefficient is 3.88
a) I, III
b) I, IV
c) I, II, III
d) IV
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Naphazoline | A. (RS)-[4-(1-Hydroxy-2-tert-butylamino-ethyl)-2-(4-methylbenzoyl)oxy-phenyl] 4-methylbenzoate |
ii. Bitolterol | B. 2-[(4-tert-butyl-2,6-dimethylphenyl)methyl]- 4,5-dihydro-1H-imidazole |
iii. Xylometazoline | C. 3-(4,5-Dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethyl-6-tert-butyl-phenol |
iv. Oxymetazoline | D. 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole |
a) i-D, ii-A, iii-B, iv-C
b) i-A, ii-C, iii-D, iv-B
c) i-B, ii-C, iii-D, iv-A
d) i-A, ii-D, iii-, iv-B
Q.3 Correct steps for the mechanism of action of the drug Naphazoline?
I. Vasoconstriction
II. Realease of norepinephrine
III. Decrease in the congestion
IV. Stimulation of αadrenergic receptors
a) I – IV – III – II
b) III – II – I – IV
c) I – III – II – IV
d) IV – III – II – I
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) FFTF
b) FTFF
c) TFFF
d) FFFF
Q.5 Large lipophillic groups at R1 substitution can-
a) Afford compounds with α-blocking activity
b) Provides maximal direct activity
c) Increase both α and ß activity
d) None of the above
Q.6 The correct sequence for the steps for synthesis of drug naphazoline from (1-naphthyl)acetonitrile?
I. Reaction with ethanol
II. Reaction with Sulfuric acid
III. Reaction with ethylenediamine
IV. Hydrogenation
a) I – III
b) II – III
c) III – II
d) III – IV
Q.7 Side effect of drug Naphazoline includes?
a) Hair loss
b) Decrease in blood count
c) Rhinitis medicamentosa
d) Liver abnormalities
1-b
2-a
3-d
4-d
5-a
6-a
7-c
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