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]]>4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 477 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 222.1°C |
4 | Solubility | 405 mg/L in water |
5 | Octanol/water partition coefficient | 5.5 |
6 | Presence of ring | Phenyl, piperidine |
7 | Number of chiral centers | Not present |
SAR for Opiates can be summarized as follows:
i. Ring opening of compound 2,2-diohenyl-4-hydroxubutyric acid y lactone with 48% HBr in acetic acid to get 4-bromo-2,2-diphenylbutyric acid.
ii. Reaction of last with thionyl chloride in chloroform produces 4-bromo-2,2-diphenylbutyroyl chloride.
iii. Compound formed in ii. Step is dissolved in toluene and dimetylamine and sodium carbonate in water are carefully added to it at low temperature to get tetrahydro-3,3-diphenyl-2-furylidene ammonium salt.
iv. Coupling of dimethyl(tetrahydro-3,3-diphenyl-2-furylidene)ammonium bromide with 4-(4-chlorophenyl)piperidin-4-ol on refluxing reagents in isobutyl methyl ketone in presence of excess sodium carbonate produces the Loperamide drug. [1]
Loperamide is used for:
Side effects Loperamide are:
Q.1 “4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-N,N-dimethyl-2,2-diphenylbutanamide” is the IUPAC nomenclature of which drug?
a) Chlorpromazine
b) Sevoflurane
c) Loperamide
d) Thioridazine
Q.2 Correct melting point of the drug Loperamide is?
a) 154°C
b) 782°C
c) 222°C
d) 157°C
Q.3 Match the following with correct classifications of the drugs.
i. Loperamide | A. Antidiarrheal agent |
ii. Diazepam | B. ß-blockers |
iii. Halothane | C. Sedative hypnotic |
iv. Betazolol | D. Anticonvulsant drug |
a) i-A, ii-C, iii-D, iv-B
b) i-C, ii-A, iii-B, iv-D
c) i-D, ii-C, iii-A, iv-B
d) i-A, ii-D, iii-C, iv-B
Q.4 Mechanism of action of drug Loperamide includes?
I. It is a selective α-blocker.
II. It increases the intestinal motility.
III. Peristaltic activity is inhibited by the drug.
IV. Drug can also bind with calmodulin at higher concentrations.
a) III, IV
b) II, IV
c) I, III, IV
d) I, II
Q.5 Correct sequence for True and False for the given statements related with the SAR of opiate drugs?
a) FFTT
b) TFTF
c) TFFT
d) TTTT
Q.6 Type of ring present in the structure of Loperamide is?
a) Piperidine
b) Pyridine
c) Pyrimidine
d) Pyrrole
Q.7 The drug loperamide is used for?
a) Treatment of diarrhea
b) Treatment of pain
c) As an anti-inflammatory agent
d) All of the above
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1-c
2-c
3-a
4-a
5-d
6-a
7-a
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