The post INDOMETHACIN Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>2-{1-[(4-Chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 357.8 g/mol |
2 | Physical appearance | Pale yellow to yellow-tan crystalline powder |
3 | Melting point | 158°C |
4 | Solubility | Practically insoluble in water; soluble in ethanol, acetone, ether, castor oil |
5 | Octanol/water partition coefficient | 4.27 |
6 | Presence of ring | Indole, phenyl |
7 | Number of chiral centers | Not present |
SAR of indomethacin can be summarized as follows:
i. Acylation of the ß-modified arylhadrazine (1) using chlorobenzoic acid by pyridine-catalyzed acylation to give α-acyl-arylhydrazine (2).
ii. Indole ring is formed by reaction of the (2) with α-Angelica lactone nder acidic conditions. [2]
Indomethacin is used for:
Side Effects
Side effects of indomethacin are:
Q.1 What can be the correct IUPAC nomenclature of Indomethacin?
a) 2-{1-[(4-Chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid
b) 2-{1-[(4-Chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl} propanoic acid
c) 2-{1-[(4-Chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}butanoic acid
d) 2-{1-[(4-Chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}pentanoic acid
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Indomethacin?
I. Replacement of the carboxyl group with other acidic functionalities increases the activity.
II. As the acidity of the carboxyl group increases, the anti-inflammatory activity of drug also increases and vice-versa.
III. Amide analogues are inactive.
a) I, II
b) I, II, III
c) III
d) I
Q.3 Number of chiral centers present in the structure of indomethacin is?
a) 0
b) 1
c) 2
d) 3
Q.4 Side effects of drug Indomethacin is/are?
a) Abdominal pain
b) Heart problems
c) Allergic reactions
d) All of the above
Q.5 Match the following drugs with their correct molecular weight.
i. Indomethacin | A. 357.8gm/mol |
ii. Bitolterol | B.225.28 gm/mol |
iii. Xylometazoline | C. 461.5gm/mol |
iv. Terbutaline | D.244.37 gm/mol |
a) i-A, ii-D, iii-C, iv-B
b) i-B, ii-A, iii-D, iv-C
c) i-A, ii-C, iii-D, iv-B
d) i-D, ii-C, iii-A, iv-B
Q.6 An example of drug from class NSAIDs is?
a) Indomethacin
b) Methyldopa
c) Prazosin
d) Methysergide
Q.7 The type of ring system found in the structure of Indomethacin is?
a) Indole
b) Pyrrole
c) Furan
d) No ring structure present
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1-a
2-d
3-a
4-d
5-c
6-a
7-a
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