The post LABETOLOL Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(RS)-2-Hydroxy-5-[1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl]benzamide.
Labetolol is a mixed α/ß blocker.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 328.4 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 188°C |
4 | Solubility | Water solubility is 3.56e-04 M |
5 | Octanol/water partition coefficient | 2.7 |
6 | Presence of ring | Benzene |
7 | Number of chiral centers | 2 |
i. N-alkylation of N-benzyl-N(4-phenyl-2-butyl)amine 5-bromoacetylsalicylamide forms aminoketone.
ii. Debenzylation of aminoketone by hydrogen using palladium-platinium on carbon catalyst yields labetolol.
Labetolol is used for treatment of:
Side effects of Labetolol are:
Q.1 Choose the correct option related to the correct physicochemical properties of drug labetolol.
I. Molecular weight is 266.34 gm/mol.
II. It is present in solid form.
III. Melting point is 188°C
a) I, II, III
b) II, III
c) I, III
d) I, II
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Atenolol | A. (±)-[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl][2-(2-methoxyphenoxy)ethyl]amine |
ii. Labetolol | B. (RS)-2-Hydroxy-5-[1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl]benzamide |
iii. Bisoprolol | C. (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-
3-(isopropylamino)propan-2-ol |
iv. Carvedilol | D. (RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide. |
a) i-B, ii-A, iii-C, iv-D
b) i-D, ii-A, iii-B, iv-C
c) i-A, ii-C, iii-D, iv-B
d) i-D, ii-A, iii-C, iv-B
Q.3 Pick the correct statement related with the mechanism of action of drug labetolol?
a) It selectively antagonizes α1-adrenergic receptors and nonselectively antagonizes ß-adrenergic receptors .
b) It nonselectively antagonizes α-adrenergic receptors and nonselectively antagonizes ß-adrenergic receptors .
c) It selectively antagonizes α2-adrenergic receptors and selectively antagonizes ß2-adrenergic receptors .
d) It nonselectively antagonizes α-adrenergic receptors and nonselectively antagonizes ß-adrenergic receptors .
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TTFF
b) TTFT
c) TFTF
d) FFTT
Q.5 Complete the following sentence related with structure activity relationship of Labetolol-
‘The ß-blocking activity is almost ………. That of α-blocking activity.
a) Half
b) Quarter
c) Double
d) 1.5 folds
Q.6 The correct sequence for the steps for synthesis of drug Labetolol from N-benzyl-N(4-phenyl-2-butyl)amine 5-bromoacetylsalicylamide
I. N-alkylation
II. Debenzylation
III. Hydrolysis
a) I – II
b) III – II
c) II – I
d) II – III
Q.7 Side effect of drug Labetolol?
a) Lightheadedness
b) scalp tingling
c) Decreased libido
d) All of the above
1-b
2-d
3-a
4-a
5-c
6-a
7-d
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