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]]>Methyl (RS)-3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate.
Esmolol is a cardioselective ß1-adrenergic antagonist
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 295.37 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 90°C |
4 | Solubility | Very soluble in hydrochloride salt |
5 | Octanol/water partition coefficient | 1.7 |
6 | Presence of ring | Benzene |
7 | Number of chiral centers | 1 |
i. Methyl 3-(4-hydroxyphenyl)propanoate reacts with 2-(chloromethyl)oxirane to give methyl 3-(4-((oxirane-2-yl)methoxy)phenyl)propanoate.
ii. The latter compound is reacted with propan-2-amine to give esmolol.
Esmolol is used for treatment of:
Side Effects
Side effects of esmolol are:
Q.1 What can be the correct IUPAC nomenclature of Esmolol?
a) (RS)-1-(1-methylethylamino)-3-(1-naphthyloxy)propan-2-ol.
b) Methyl (RS)-3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate
c) (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-3-(isopropylamino)propan-2-ol
d) (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxybenzamide
Q.2 Which amongst the following statements is/are incorrect related to the SAR of esmolol?
I. Increasing the chain length of the side chain prevents appropriate binding of the required functional groups to the same receptors side.
II. Side chain of aryloxypropanolamines can adopt a conformation that places the hydroxyl and amine groups into approximately the same position in space.
III. Aryloxypropalonamines permits a close overlap with the arylethanomine side chain.
a) I, III
b) II, III
c) I, II, III
d) I, II
Q.3 The correct order for the synthesis of drug esmolol from Methyl 3-(4-hydroxyphenyl)propanoate can be?
Reaction with 2-(chloromethyl)oxirane
Reaction with propan-2-amine
III. Reduction with help of Pt-Pd catalyst
a) III – II – I
b) I – III – II
c) I – II
d) III – I
Q.4 Side effects of drug Esmolol is/are?
a) Headache
b) Fast heart rate
c) Anxiety
d) All of the above
Q.5 Match the following drugs with their correct molecular weights-
i. Propranolol | A. 295.37 gm/mol |
ii. Esmolol | B. 309.4 gm/mol |
iii. Bisoprolol | C. 325.4 gm/mol |
iv. Metipranolol | D. 259.34 gm/mol |
a) i-B, ii-A, iii-D, iv-C
b) i-B, ii-A, iii-C, iv-D
c) i-B, ii-C, iii-A, iv-D
d) i-D, ii-A, iii-C, iv-B
Q.6 An example of drug from class ß1-adrenergic antagonist?
a) Dopamine
b) Dobutamine
c) Propranolol
d) Esmolol
Q.7 The type of ring system found in Esmolol?
a) Naphthalene
b) Carbazoline
c) Imidazoline
d) Benzene
1-b
2-c
3-c
4-d
5-d
6-d
7-d
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