The post DARIFENACIN Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
Darifenacin is an acetylcholine antagonist. It is a muscarinic antagonist.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 426.5 g/mol |
2 | Physical appearance | White crystalline powder |
3 | Melting point | More than 230°C |
4 | Solubility | Slightly soluble in water |
5 | Octanol/water partition coefficient | 4.5 |
5 | Presence of ring | Dihydrobenzofuran, cyclopentyle, phenyl |
6 | Number of chiral centers | 2 |
Darifenacin acts as selective antagonist for the muscarinic receptors (M3). M3 receptors are involved in contraction of bladder, and hence, the drug helps in relaxing bladder. [1]
Reaction of 3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)- pyrrolidine with 5-(2-bromoethyl)benzo[2,3-b]furan in presence of anhydrous K2CO3 in acetonitrile to get darifenacin. [2]
Darifenacin is used for:
Side effects of Darifenacin are:
Q.1 What can be the correct IUPAC nomenclature of Darifenacin?
a) (S)-2-[1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl] pyrrolidin-3-yl] -2,2-diphenyl-acetamide
b) (S)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol.
c) 7-Chloro-2,3-dihydro-2-oxo-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid
d) N,N-Dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide hemitartrate
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Darifenacin?
I. Either R1 or R2 must be heterocyclic or carbocyclic.
II. The R3 group can be hydrogen, hydroxyl, hydroxymethyl or amide.
III. Poorest derivatives has X as an ester.
IV. ‘X’ can also be either oxygen or absent completely.
a) I, II
b) III
c) III, IV
d) II
Q.3 Darifenacin can be obtained by reaction of 3-(S)-(-)-(1-carbamoyl-1,1-diphenylmethyl)- pyrrolidine with?
a) 5-(2-bromoethyl)benzo[2,3-b]furan
b) 1-phenylpropyl-4-methylphenol
c) 1,4-benzodiazepine-3-carboxylic acid
d) None of the above
Q.4 Side effects of drug darifenacin is/are?
a) Constipation
b) Headache
c) Dry mouth
d) All of the above
Q.5 Match the following drugs with their correct molecular weights-
i. Darifenacin | A.426.5 gm/mol |
ii. Tolterodine | B.307.4gm/mol |
iii. Chlorazepate | C. 325.5 gm/mol |
iv. Zolpidem | D. 314.72 gm/mol |
a) i-C, ii-B, iii-A, iv-D
b) i-C, ii-B, iii-D, iv-A
c) i-A, ii-C, iii-D, iv-B
d) i-B, ii-A, iii-D, iv-C
Q.6 An example of drug from class Acetylcholine antagonist?
a) Zolpidem
b) Chlorazepate
c) Amphetamine
d) Darifenacin
Q.7 The type of ring system found in the structure of darifenacin?
a) Dihydrobenzofurane
b) Pyrrolopyrimidine
c) Naphthalene
d) Pyrrolopyrrole ring
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1-a
2-b
3-a
4-d
5-c
6-d
7-a
The post DARIFENACIN 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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