The post BUCLIZINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] piperazine
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 433 g/mol |
2 | Physical appearance | Liquid |
3 | Melting point | 218oC |
4 | Solubility | 2.46e-04 g/L |
5 | Octanol/water partition coefficient | 7.1 |
5 | Presence of ring | Piperazine, phenyl |
6 | Number of chiral centers | 1 |
Structure activity of piperizine antihistamines can be summarized as:
i. 4-chlorobenzhydryl chloride is reacted with ethyl piperazine N-carboxylate to give ethyl-4-(4-chlorobenzhydryl)piperazine-1-carboxylate.
ii. The above formed compound is treated with NaOH to get 1-(4-chlorobenzhydryl)piperazine.
iii. The last is reacted with 4-tert-butyybenzyl chloride to get Buclizine. [1]
Buclizine is used for treatment of:
Side effects of Buclizine are:
Q.1 What can be the correct IUPAC nomenclature of Buclizine?
a) (RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] pyrimidine
b) (R)-(+)-2-([3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl)-1H-benzo[d]imidazole
c) (RS)-1-[(4-chlorophenyl)- phenyl-methyl]-4- [(4-tert-butylphenyl) methyl] piperazine
d) (R)-(+)-2-([3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl)-imidazole
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Piperazine antihistamines?
I. These are the derivatives of Ehanol.
II. The connecting moiety is CHN group
III. Primary structural difference is nature of para aromatic ring substituent
a) I
b) II, III
c) I, III
d) I, II, III
Q.3 Types of rings present in the structure of Buclizine?
I. Piperazine
II. Pyridine
III. Pyrolle
IV. Phenyl
a) I, III
b) I, IV
c) II, IV
d) II, III
Q.4 Side effects of drug Buclizine is/are?
a) Drowsiness
b) Vomitting
c) Headache
d) All of the above
Q.5 Match the following drugs with their correct molecular weight-
i. Buclizine | A. 426.6 gm/mol |
ii. Hydroxyzine | B. 266.4gm/mol |
iii. Oxatomide | C. 433 gm/mol |
iv. Cyclizine | D. 374.9 gm/mol |
a) i-A, ii-B, iii-C, iv-D
b) i-C, ii-A, iii-B, iv-D
c) i-C, ii-D, iii-A, iv-B
d) i-A, ii-C, iii-D, iv-B
Q.6 An example of drug from class piperazine antihistamine drug?
a) Buclizine
b) Cimetidine
c) Glycopyrrolate
d) All of the above
Q.7 Octanol/water partition coefficient of Buclizine is?
a) 2.5
b) 3.2
c) 4.8
d) 7.1
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ANSWERS
1-c
2-a
3-b
4-d
5-c
6-a
7-d
REFERENCES
[1] DE 964 048 (H. Morren; appl. 1952; B-prior. 1951).
The post BUCLIZINE 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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