The post SULINDAC Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>{(1Z)-5-fluoro-2-methyl-1-[4-(methylsulfinyl)benzylidene]-1H-indene-3-yl}acetic acid
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 356.4 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 183°C |
4 | Solubility | 3000 mg/L |
5 | Octanol/water partition coefficient | 3.42 |
6 | Presence of ring | Indene, phenyl |
7 | Number of chiral centers | Not present |
SAR of Sulindac can be summarized as follows:
i. Condensatio of n-fluorobenzaldehyde with propionic acid in the presence of sodium acetate give 4-fluoro-α-methylcinnamic acid.
ii. On reducing the double bond of the above formed compound by palladium on carbon catalyst, 4-fluoro-α-methyldihydrocinnamic acid is produces.
iii. Resultant undergoes cyclization in the presence of polyphosphoric acid to ive 5-fluoro-2-methyl-3-indanone.
iv. The last undergoes a knowvwnagel reaction with cyanoactic aid followed by decarboxylation to produce 5-fluoro-2-methyliden-3-acetic acid.
v. On condensation of the above formed compound with n-mercaptobenzaldehyde in the presence of sodium methoxide produces 5-fluoro-2-ethyl-1-(4-methylthiobenzyliden)-3-indeaetic acid.
vi. In the final step, the sulfur atom is oxidized by sodium periodate into sulfoxide o give Sulindac. [2]
Sulindac is used for:
Side Effects
Side effects of sulindac are:
Q.1 Match the following with correct SAR of the drug Sulindac.
i. Replacement of indole ring with indene ring results in | A. Increase in CNS and GI side effects |
ii. Z-isomer is | B. Decrease in CNS and GI side effects |
C. More potent than E-isomer | |
D. Less potent than E-isomer |
a) i-A, ii-C
b) i-A, ii-D
c) i-B, ii-C
d) i-B, ii-D
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) FFFF
b) FTFT
c) TFFT
d) FTTF
Q.3 Octanol/water partition coefficient of Sulindac is?
a) -2
b) -3.42
c) 2
d) 3.42
Q.4 Correct statement/s related with the mechanism of action of drug sulindac is/are?
a) It inhibits COX-1 enzymes
b) It inhibits COX-2 enzymes
c) It produces action on hypothalamus to produce antipyretic action
d) All of the above
Q.5 Which amongst the following is NOT a Medicinal use of drug sulindac?
a) As a general anesthesia
b) Reducing pain due to arthritis
c) Treatment of shoulder Bursitis
d) Treatment of shoulder tendonitis
Q.6 Which of the following drug and their classification are correct?
I. Sulindac: Nonsteroidal anti-inflammatory drug
II. Risperidone: Nitrogen mustard
III. Hyoscyamine: Cytotoxic agent
IV. Glutemide: epipodophyllotoxin drug
a) I, III, IV
b) I
c) II, III
d) I, II, III, IV
Q.7 Number of chitral carbons present in the structure of Sulindac?
a) 0
b)1
c) 2
d) 3
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1-c
2-a
3-d
4-d
5-a
6-b
7-a
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