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]]>5-(Pentan-2-yl)-5-(prop-2-en-1-yl)-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione
Thiamylal is a barbiturate sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 254.35g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 132-133°C |
4 | Octanol/water partition coefficient | 3023 |
5 | Solubility | Water solubility is 3.48e-04 M |
6 | Presence of ring | Pyrimidine |
7 | Number of chiral centers | 2 |
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.
Thiamylal can be synthesized by condensation of diethyl 2-allyl-2-(pentan-2-yl)malonate with thiourea.
Thiamylal is used for:
Side effects of Thiamylal are:
Q.1 Due to Potentiation of GABA receptors by Thiamylal?
a) Increase in opening duration of calcium channels
b) Increase in opening duration of the Chloride channels
c) Increase in opening duration of the Sodium channels
d) Decrease in opening duration of the calcium channels
Q.2 Therapeutic use of drug Thiamylal is/are?
a) Induction of surgical anesthetics
b) Inducing drowsiness
c) Reducing anxiety
d) All of the above
Q.3 Which amongst the following are the correct statements with respect to the SAR of drug Thiamylal
I. Tri-keto form is most stable in aqueous solution.
II. 4,6-dialcoholic tautomeric forms are least stable in aqueous solution.
III. 5,5-disubstituted barbituric acid is the prime requirement for the barbituares to be sedative hypnotics.
IV. Esterification of either of the 1,3-diazine nitrogens decreases hypnotic activity.
a) I, III, IV
b) II, IV
c) I, II, III
d) I, II, III, IV
Q.4 The starting chemicals required for the synthesis of drug Thiamylal?
a) Malonic ester
b) Barbital
c) Both a) and b)
d) None of the above
Q.5 Correct sequence for the True/False for the physiochemical properties of the drug Thiamylal is?
I. Molecular weight is 254.35 g/mol
II.It is present in liquid crystalline form
III. Melting point is 132.5oC
IV. No chiral carbons are present in the structure of barbital.
a) TFTF
b) TFFF
c) FFFT
d)FTTF
Q.6 Correct statements for the IUPAC nomenclatures of the drugs are?
I. Thiamylal: 5-(Pentan-2-yl)-5-(prop-2-en-1-yl)-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione.
II, Secobarbital: 5-(pentan-2-yl)-5-(prop-2-en-1-yl)-1,3-diazinane-2,4,6-trione
III. Quazepam: 5-butan-2-yl-5-ethyl-1,3-diazinane-2,4,6-trione
IV. Triazolam: 5-Ethyl-5-phenyl-1,3-diazinane-2,4,6-trione
a) II, III
b) II, IV
c) I, II, IV
d) I, II
Q.7 Match the following drugs with their correct classifications-
i. Thiamylal | A. Barbiturate sedative-hypnotic |
ii. Zolpidem | B.Benzazepine |
iii. Olanzapine | C. Nonbenzodiazepine agonist |
iv. Oxazepam | D. Benzodiazepine |
a) i-A, ii-C, iii-B, iv-D
b) i-B, ii-D, iii-A, iv-C
c) i-A, ii-D, iii-C, iv-B
d) i-C, ii-A, iii-B, iv-D
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1-b
2-d
3-d
4-a
5-a
6-d
7-a
The post THIAMYLAL Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
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