The post EPHEDRINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(1R,2S)-2-(methylamino)-1-phenylpropan-1-ol.
Ephedrine is a mixed adrenergic agonist.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 165.23 g/mol |
2 | Physical appearance | Present in waxy solid, crystals or granular form |
3 | Melting point | 34 °C |
4 | Solubility | Water solubility is 0.38M; it is soluble in oils. |
5 | Octanol/water partition coefficient | 1.13 |
6 | Presence of ring | Benzene ring |
7 | Number of chiral centers | 2 |
The SAR of Adrenergic agonist can be discussed as follows:
R1 substitution:
R2 substitution:
R3 substitution on the aromatic ring:
If phenyl group has no phenolic substituent then it may act directly or indirectly. [2]
i. Benzaldehyde is converted into levo-1-phenyl-2-keto-1-propano through fermentation.
ii.The above compound is then condensed with the help of methylamine and reduced with free aluminum in moist ether to give ephedrine.
Ephedrine is used:
Side effects of propylhexedrine are:
MCQs
Q.1 Correct statements for the drug Ephedrine are?
I. Molecular weight is 165.23 gm/mol
II. Present in form of waxy solid
III. It is having no ring in its structure
IV. Its melting point is 34°C
a) I, II, IV
b) I, IV
c) I, II, III, IV
d) I, II, IV
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Ephedrine | A. (1R,2S)-2-(methylamino)-1-phenylpropan-1-ol |
ii. Metaraminol | B. 3-[(1R,2S)-2-amino-1-hydroxypropyl]phenol |
iii. Pseudoephedrine | C. (±)-1-cyclohexyl-N-methylpropan-2-amine |
iv. Propylhexedrine | D. (S,S)-2-methylamino-1-phenylpropan-1-ol. |
a) i-A, ii-B, iii-D, iv-C
b) i-B, ii-A, iii-D, iv-C
c) i-C, ii-D, iii-B, iv-A
d) i-B, ii-D, iii-A, iv-C
Q.3 Principle behind mechanism f action of Ephedrine is?
a) Direct and indirect action on the adrenergic receptors
b) Direct action on the adrenergic receptors
c) Indirect action on the adrenergic receptors
d) No involvement of the adrenergic receptors
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TTF
b) TFT
c) FTF
d) TTT
Q.5 Pick the correct statement related with the SAR of ephedrine.
a) When hydroxyl substituted carbon is in R configuration, activity is maximum.
b) When hydroxyl substituted carbon is in R configuration, activity is minimum..
c) Both configuration possess same activity.
d) Activity does not depend on the configuration of the hydroxyl substituted carbon.
Q.6 The correct sequence for the steps for synthesis of drug Ephedrine from benzaldehyde?
I. Condensation with methylamine
II. Reduction with Aluminium
III. Fermentation by yeast
a) I – II – III
b) II – III – I
c) I – III – II
d) III – I – II
Q.7 Side effect of drug Ephedrine is?
a) Dizziness
b) Restlessness
c) Nervousness
d) All of the above
1-d
2-a
3-a
4-a
5-a
6-d
7-d
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