The post TRIPROLIDINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>2-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-yl-prop-1-enyl]pyridine
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 278.4 g/mol |
2 | Physical appearance | Forms crystal from light petroleum |
3 | Melting point | 60oC |
4 | Solubility | 74.9 mg/LL |
5 | Octanol/water partition coefficient | 3.92 |
5 | Presence of ring | Phenyl, pyrrolidine |
6 | Number of chiral centers | Not present |
i. Triprolidine binds to histamine H1 receptors and blocks the action of endogenous histamine.
ii. This provides relief from the negative symptoms produced by the histamine.
Structure activity of alkyl amines antihistamines can be summarized as:
i. 4’-methylacetophenone, paraformaldehyde and pyrrolidine are reacted together to give 4’-methyl-3-pyrrolidinopropiophenone.
ii. The above formed compound is reacted with lithium and 2-bromopyridine to give 1-(pyridin-2-yl)-3-(pyrrolidin-1-yl)-1-p-tolylpropan-1-ol
iii. Last compound is treated with hydrochloric acid to give a mixture of cis- and trans-triprolidine.
iv. Cis and trans- forms can be separated by using ion exchangers. [2]
Triprolidine is used for treatment of:
Side effects of triprolidine are:
Q.1 “2-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-yl-prop-1-enyl]pyridine” is the IUPAC nomenclature of which drug?
a) Brompheniramine
b) Clemastine
c) Triprolidine
d) Tenoxicam
Q.2 Molecular weight of Triprolidine is?
a) 144.5 gm/mol
b) 278.4 gm/mo
c) 290.79 gm/mol
d) 134.32 gm/mol
Q.3 Match the following with correct classifications of the drugs.
i. Triprolidine | A. Alkylamine antihistamine drug |
ii. Verapamil | B. H2-antagonist |
iii. Ranitidine | C. Calcium channel blocker |
iv. Mercaptopurine | D. Antimetabolite antineoplastic agent |
a. i-A, ii-C, iii-B, iv-D
b. i-C, ii-D, iii-A, iv-B
c. i-D, ii-,B iii-A, iv-C
d. i-A, ii-D, iii-C, iv-B
Q.4 Which of the following mechanisms are involved for the action of Triprolidine drug?
I. Produces antagonistic effects on Nicotinic receptors
II. Produces antagonistic effects on H1 receptors
III. There is blockage of action of endogenous histamine
IV. It also alkylates the genetic material of cell causing death of neoplastic cells.
a) I, IV
b) II, III
c) I, III, IV
d) I, II, III
Q.5 Correct sequence for True and False for the given statements related with the SAR of class alkylamines antihistamines can be?
a) TFFT
b) TFTF
c) TTTT
d) FTFF
Q.6 The cis- and trans- forms of triprolidine can be separated using?
a) Ion exchanger
b) Free radicals
c) Hydrogen gas
d) None of the above
Q.7 The drug Triprolidine is mainly used for?
a) Treatment of sneezing
b) Treatment of watery eyes
c) Treatment of runny nose
d) All of the above
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1-c
2-b
3-a
4-b
5-c
6-a
7-d
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