The post ATENOLOL Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)propoxy]phenyl}acetamide.
Atenolol is a cardioselective ß-blocker.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 266.34 g/mol |
2 | Physical appearance | Present in white crystalline powder form. |
3 | Melting point | 159°C |
4 | Solubility | Water solubility is 0.05M |
5 | Octanol/water partition coefficient | 0.16 |
6 | Presence of ring | Benzene |
7 | Number of chiral centers | 1 |
i. Atenolol selectively binds with ß1-adrenergic receptors present in the vascular smooth muscles and the heart, and leads to block them.
ii. It leads to positive inotropic and chronotropic actions of endogenous catecholamines, which further results in inhibition of sympathetic stimulation.
iii. This activity decreases the heart rate, blood pressure and myocardial contractility.
iv. It also increases the AV node’s refractory period. [1]
i. 2-(4-hydroxyphenyl)acetamide reacts with 2-(chloromethyl)oxirane in presence of piperidine to give 4-(cyclopropylmethoxy)benzamide.
ii. Latter compound reacts with 2-aminopropan-1-ol to give atenolol.
Atenolol is used for treatment of:
Side Effects
Side effects of atenolol are:
Q.1 Choose the correct option related to the correct physicochemical properties of drug Atenolol.
I. Molecular weight is 266.34 gm/mol.
II. It is present in yellow oily liquid form.
III. Melting point is 159°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 Correct steps for the mechanism of action of the drug Atenolol?
I. Positive inotropic and chronotropic actions of endogenous catecholamine
II. Blocking of ß1-adrenergic receptors
III. Decrease in heart rate, blood pressure and myocardial contractility.
a) I – III – II
b) II – I – III
c) III – I – II
d) II – III – I
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 atenolol-
‘aryoxypropanolamines are …………………. than aryloxyethanolamines.
a) more selective
b) less selective
c) more potent
d) less potent
Q.6 The correct sequence for the steps for synthesis of drug atenolol from 2-(4-hydroxyphenyl)acetamide?
I. Reaction with 2-(chloromethhyl)oxirane in presence of piperidine
II. Reaction with 2-aminopropan-1-ol
III. Reaction with 2-(chloromethhyl)oxirane in presence of ammonia.
a) I – II
b) III – II
c) II – I
d) II – III
Q.7 Side effect of drug atenolol?
a) Lightheadedness
b) Depression
c) Shortness of breath
d) All of the above
1-c
2-d
3-b
4-a
5-c
6-a
7-d
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