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]]>S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 296.1 g/mol |
2 | Physical appearance | Crystals from ether-petroleum ether |
3 | Melting point | 283-285°C |
4 | Solubility | 2.73 mg/L in water |
5 | Octanol/water partition coefficient | 4.51 |
6 | Presence of ring | Phenyl |
7 | Number of chiral centers | Not present |
SAR of Diclofenac can be summarized as follows: The two-o-chloro groups are important for the activity of the drug. the twisting of the two o-chloro groups is necessary for the binding of the drug with COX active site.
i. Reaction of 2-chlorobenzoic acid and 2,6-dichloroaniline in the presence of sodium hydroxide and copper produces N-(2,6-dichlorophneyl)anthranylic acid.
ii. The carboxylic group of the last compound is reduced by lithium aluminum hydride to give 2-[(2,6-dichlorophenyl)-amino]-benzyl alcohol.
iii. The above formed compound is further chlorinated by thionyl chloride to produce 2-[(2,6-dichlorophenyl)-amino]-benzylchloride.
iv. On further reaction with sodium cyanide, 2-[(2,6-dichlorophenyl)-amino]benzyl cyanide is formed.
v. On hydrolysis of the nitrile group of last compound leads to formation of diclofenac. [2]
Diclofenac is used for:
Side effects of Diclofenac are:
Q.1 Choose the correct option related with the mechanism of action of drug Diclofenac?
a) Inhibits the activity of COX-1
b) Inhibits the activity of COX-2
c) Decreases in the production of prostaglandins
d) All of the above
Q.2 Medicinal use of drug Diclofenac is/are?
a) Reducing pain due to arthritis
b) Treatment of psoriases
c) Treatment of warts
d) All of the above
Q.3 Type of ring structure present in the Diclofenac is
a) Phenyl
b) Cyclohexane
c) Furan
d) Diazepine
Q.4 Number of chiral carbons present in the structure of diclofenac is?
a) 0
b) 1
c) 2
d) 3
Q.5 Correct sequence for the True/False for the physiochemical properties of the drug diclofenac is?
I. Molecular weight = 296.1gm/mol
II. Melting point = 147oC
III. Crystals from ether-petroleum ether
IV. Ring structure is absent
a) TFTF
b) TFFT
c) FTTF
d) TFFF
Q.6 Correct statements for the IUPAC nomenclatures of the drugs are?
I. Diclofenac:2-hydroxybenzoate
II. Levallorphan: 2-Chloro-N-(2-chloroethyl)-N-methylethan-1-amine
III. Dacarbazine: N,3-Bis(2-chloroethyl)-1,3,2-oxazaphosphinan-2-amide 2-oxide
IV. Carboplatin: (SP-4-2)-diamminedichloroplatinum(II)
a) I, IV
b) I, II, III, IV
c) II , III
d) None
Q.7 Match the following drugs with their correct classifications-
i. Diclofenac | A. Inhalational anesthetics |
ii. Bisoprolol | B. ß-adrenergic blocker |
iii. Thioridazine | C. Nonsteroidal anti-inflammatory drug |
iv. Enflurane | D. Phenothiazine antipsychotic drug |
a) i-B, ii-D, iii-C, iv-A
b) i-B, ii-C, iii-A, iv-D
c) i-C, ii-B, iii-D, iv-A
d) i-A, ii-D, iii-B, iv-C
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1-d
2-a
3-a
4-a
5-a
6-d
7-c
The post DICLOFENAC Synthesis, SAR,MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
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