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]]>5-Phenyl-5-ethyl-1-methylbarbituric acid
Mephobarbital is a barbiturate sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 246.26g/mol |
2 | Physical appearance | White crystals |
3 | Melting point | 176°C |
4 | Octanol/water partition coefficient | 1.84 |
5 | Solubility | Slightly soluble in water |
6 | Presence of ring | Pyridine, phenyl |
7 | Number of chiral centers | 1 |
i. Drug binds with different binding sites associated with chloride ionopore at the GABAA
ii. This results in increase in the duration of time for the opening of the chloride ionopore.
iii. As a result, the post synaptic inhibitory effect of GABA in the thalamus is prolonged.
i. Ethylbenzoate reacts with ethyl chloroformate in presence of sodium hydride to give diethyl 2-phenylmalonate.
ii. diethyl 2-phenylmalonate undergoes alkylation to produce ethyl 2-ethyl-4-methoxy-3-oxo-2-phenylbutanoate.
iii. On condensation with methylurea, mephobarbital is yielded. [2]
Mephobarbital is used:
Side effects of Mephobarbital are:
Q.1 “5-Phenyl-5-ethyl-1-methylbarbituric acid” is the IUPAC nomenclature of which drug?
a) Mephobarbital
b) Acyclovir
c) Zidovudin
d) Abacavir
Q.2 Correct statement related to the solubility of mephobarbital in water is?
a) Very soluble
b) Soluble
c) Slightly soluble
d) Practically insoluble
Q.3 Match the following with correct classifications of the drugs.
i. Mephobarbital | A. Muscarinic agonist |
ii. Methacholine | B. Nicotinic antagonist |
iii. Atropine | C. Barbiturate sedative-hypnotic |
iv. Metocurine | D. Muscarinic antagonist |
a) i-C, ii-A, iii-D, iv-B
b) i-B, ii-A, iii-D, iv-C
c) i-A, ii-C, iii-B, iv-D
d) i-D, ii-A, iii-B, iv-C
Q.4 Correct steps for the mechanism of action of the drug Mephobarbital
I. Binding of drug with GABA molecule
II. Binding of Drug with GABAA receptor
III. Increase in GABA affinity
IV. Increase in opening duration of the chloride channel
a) IV – II – I
b) I – III – IV
c) I – II – IV
d) II – III – IV
Q.5 Correct sequence for True and False for the given statements related with the SAR of drug Mephobarbital.
a) TFFT
b) FTTF
c) FFTF
d) TTFT
Q.6 Starting materials for the synthesis of mephobarbital is/are?
a) Ethylbenzoate
b) Ethylchloroformate
c) Both a) and b)
d) None of the above
Q.7 The drug Mephobarbital is mainly used for?
a) As an anticonvulsive drug
b) For the treatment of HIV
c) For Treatment of Goiter
d) All of the above
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1-a
2-c
3-a
4-d
5-a
6-c
7-a
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