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]]>(RS)-[4-(1-Hydroxy-2-tert-butylamino-ethyl)-2-(4-methylbenzoyl)oxy-phenyl] 4-methylbenzoate.
Bitolterol is ß2-adrenergic agonist. [1]
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 461.5g/mol |
2 | Physical appearance | Off-white solid |
3 | Flash point | 341.2 |
4 | Solubility | Water solubility is 0.00048 mg / ml |
5 | Octanol/water partition coefficient | 5.8 |
6 | Presence of ring | Benzene ring present |
7 | Number of chiral centers | 1 |
Relaxation of the smooth muscles surrounding the air flow tubes through agonsim of ß2 adrenergic receptors. This result in increase in the diameter of the air flow tubes and thus, ease in breathing.
R1 substitution:
R2 substitution:
R3 substitution on the aromatic ring:
i. Reaction of 2-(tert-butylamino)-1-(3,4-dihydroxyphenyl)ethanone and 4-methylbenzoyl chloride gives compound (1).
ii. Reduction of compound (1) produces Bitolterol.
Bitolterol is given for the relief of bronchospasm during asthma and Chronic Obstructive Pulmonary Diseases.
Some of the side effects of bitolterol are
Q.1 Match the following with correct SAR of the drug Bitolterol-
i. Large lipophillic groups at R1 | A. Elimination of α-activity |
ii. N-substituent at R1 | B. Afford compounds with α-blocking activity. |
iii. Ethyl group at R2 | C. Provides selectivity for different receptors |
iv. 3’, 5’-dihydroxy compounds | D. Orally active drug |
a) i-A, ii-D, iii-B, iv-C
b) i-B, ii-C, iii-A, iv-D
c) i-B, ii-C, iii-D, iv-A
d) i-D, ii-B, iii-A, iv-C
Q.2 correct sequence for the True/False for correct IUPAC names of the drug can be?
a) TFTF
b) FFFT
c) TFFF
d) FFTT
Q.3 Water solubility of Bitolterol is?
a) 0.00048 mg/ml
b) 48 mg/ml
c) 2 mg/ml
d) 480 mg/ml
Q.4 Agonism of ß2-adrenergic receptors by Bitolterol leads to?
a) Relaxation of smooth muscles surrounding air flow
b) Increase in diameter of the air flow tubes.
c) Ease in breathing
d) All of the above
Q.5 Which amongst the following is a therapeutic use of drug Bitolterol?
a) Relief in bronchospasm
b) For treatment of ulcers
c) Treatment of insomia
d) None of the above
Q.6 Which of the following drug and their classification are correct?
I. Flutamide: Progestin
II. Etoposide: Epipodophyllotoxin
III. Bitolterol: Nonselective adrenergic agonist
IV. Methamphhetamine: Mixed acting sympathomimetics
a) II, III
b) I, IV
c) I, II, III, IV
d) I
Q.7 Bitolterol can be synthesized by the reaction of-
a) 2-(tert-butylamino)-1-(3,4-dihydroxyphenyl)ethanone and 4-methylbenzoyl chloride; followed by reduction
b) 2-(tert-butylamino)-1-(3,4-dihydroxyphenyl)ethanone and 4-methylbenzoyl chloride; followed by hydrolysis
c) (1-naphthyl)acetonitrile and ethnol; followed by reduction
d) (1-naphthyl)acetonitrile and ethanol; followed by hydrolysis
1-b
2-c
3-a
4-d
5-a
6-a
7-a
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