The post RISPERIDONE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one.
Risperidone is an atypical antipsychotic drug.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 410.5 g/mol |
2 | Physical appearance | White to slightly beige powder |
3 | Melting point | 170°C |
4 | Solubility | Practically insoluble in water; soluble in methanol |
5 | Octanol/water partition coefficient | log Kow = 3.49 |
6 | Presence of ring | Benzo[d]isoxazole, piperidine, pyridopyrimidine |
7 | Number of chiral centers | Not present |
Structure activity relationship of butyrophenones like compounds can be described as follows:
i. 1,3-difluorobenzene in acylated using 1-acetyl-4-piperidine-carbonyl chloride in dichloromethane using aluminum chloride as Lewis acid to produce 1-(4-(2,4-difluorobenzoyl)piperidin-1-yl)ethan-1-one.
ii. Then the protecting acetyl group is removed by hydrolysis in 6N hydrochloric acid on reflux to get (2,4-difluorophenyl)(piperidin-4-yl)methanone.
iii. The product is converted into oxime by reaction with hydroxylamine hydrochloride in ethanol in the presence of N,N-diethylenethanamine.
iv. Oxime undergoes cyclization to form 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazoleny refluxing with 50% potassium hydroxide solution in water.
v. Risperidone is finally obtained by alkylation of the last formed compound with 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one on heating in dimethylformamide I the presence of sodium carbonate and potassium iodide. [1]
Risperidone is used for:
Side Effects
Side effects of Risperidone are:
Q.1 The correct statement related with the SAR of drug risperidone is?
a) Replacing the keto group with sulfur increases the activity
b) Replacing the keto group with carbon increases the activity
c) Replacing the keto group with sulfur decreases the activity
d) Replacing the keto group with sulfur or carbon decreases the activity
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) FFTF
b) TTFF
c) FTFF
d) FFFT
Q.3 Correct statement related with the solubility of Risperidone is?
a) Practically insoluble in water
b) Slightly soluble in water
c) Soluble in water
d) Freely soluble in water
Q.4 Pick the correct statement?
a) Risperidone inhibits D2 dopaminergic receptors
b) Risperidone acts as antagonist for α1 receptors
c) Risperidone acts as antagonist for H1 histamine receptors
d) All of the above
Q.5 Which amongst the following is a therapeutic use of drug Risperidone?
a) Treatment of Schizophrenia
b) Treatment of Bipolar disorder
c) Both a) and b)
d) None of the above
Q.6 Which of the following drug and their classification are correct?
I. Risperidone: Antipsychotic drug
II. Atazanavir: HIV protease inhibitor
III. Clozapine: Nitrogen mustard
IV. Thiopental: Barbiturate sedative hypnotic
a) I, II, IV
b) I, IV
c) III, IV
d) I, II, IV
Q.7 Number of chiral carbons present in the structure of Risperidone?
a) 1
b) 2
c) 3
d) 0
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1-d
2-c
3-a
4-d
5-c
6-b
7-d
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