The post FELBAMATE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(3-carbamoyloxy-2-phenylpropyl) carbamate
Felbamate is a carbamate derivative anticonvulsant drug.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 238.24 g/mol |
2 | Physical appearance | White powder |
3 | Melting point | 152°C |
4 | Solubility | Sparingly soluble in water, methanol, ethanol, chloroform. |
5 | Octanol/water partition coefficient | 0.3 |
6 | Presence of ring | Phenyl ring |
7 | Number of chiral centers | Not present |
i. Reaction of ethylchoroformate with ammonia to form ethyl carbamate.
ii. Ethyl carbamate undergoes reaction with quaternary ammonium salt to produce felbamate.
Felbamate is used for:
Side effects of Felbamate are:
Q.1 Choose the correct option related with the mechanism of action of drug Felbamate?
a) Antagonsim of the NMDA receptor glycine binding site blocks the effects of the excitory amino acids and suppresses seizure activity
b) Always decreases the seizure threshold
c) Always increases the spread of seizures
d) All of the above
Q.2 Therapeutic use of drug Felbamate is/are?
a) Prevention of seizures
b) Prevention of Diarrhea
c) Prevention of Hypertension
d) All of the above
Q.3 Which amongst the following are the correct statements with respect to the SAR of drug Felbamate?
I. If the volume of the substituents is too high, then the interaction with the receptor site will be effective.
II. If the volume of the substituent is too low, then it may not contact with all the regions of the receptors.
III. The C-2 – O-4 bond length does not the docking of the molecule at the particular site.
IV. Reduction in dipole moment of the drug increases the bioactivity.
a) I, IV
b) II, III
c) II, IV
d) I, III
Q.4 Ethyl carbamate can be converted into felbamate by reaction with?
a) Quarternary ammonium salt
b) Potassium cyanide
c) Potassium cyanate
d) Ethylchloroformate
Q.5 Correct sequence for the True/False for the physiochemical properties of the drug Felbamate is?
a) FFTF
b) TFFT
c) FTTF
d) TFFF
Q.6 Correct statements for the IUPAC nomenclatures of the drug are?
I. Felbamate: 5H-dibenzo[b,f]azepine-5-carboxamide.
II. Gabapentin: 1-(Aminomethyl)cyclohexaneacetic acid
III. Loxapine: 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine
IV. Secobarbital: 5-ethyl-5-pentan-2-yl-2-sulfanylidene-1,3-diazinane-4,6-dione
a) I, II
b) II, IV
c) II , III
d) III, IV
Q.7 Match the following drugs with their correct classifications-
i. Felbamate | A. Carbamate derivative anticonvulsant drug |
ii. Mtx | B. Vinca alkaloids |
iii. Vinblastin | C. Ethylenimine |
iv. Thiotepa | D. Folate antagonist |
a) i-B, ii-D, iii-C, iv-A
b) i-B, ii-C, iii-A, iv-D
c) i-C, ii-B, iii-D, iv-A
d) i-A, ii-D, iii-B, iv-C
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1-a
2-a
3-c
4-a
5-a
6-c
7-d
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