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]]>3-[1-[4-(4-fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-benzimidazol-2-one.
Droperidol is a buterophenone antipsychotic drug.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 379.4 g/mol |
2 | Physical appearance | White to light tan in color; micro-crystalline or amorphous powder |
3 | Melting point | 145.75°C |
4 | Solubility | 4.21 mg/L in water |
5 | Octanol/water partition coefficient | 3.5 |
6 | Presence of ring | Imidazole, pyridine, phenyl |
7 | Number of chiral centers | Not present |
Structure activity relationship of butyrophenones like compounds can be described as follows:
i. 1-bnzyl-3-carbethoxypiperidin-4-one is reacted with o-phenylendiamine to form 1,5-benzdiazepine.
ii. 1,5-benzdiazepine rearranges into 1-(1-benzyl-1,2,3,6-tetrahydro-4-piridyl)-2-benzymidazolone.
iii. Debenzylation of the product with hydrogen over a palladium catalyst into 1-(1,2,3,6-tetrahydro-4-piridyl)-2-benzimi-dazolon.
iv. On subsequent alkylation with 4’-chloro-4-fluorobutyrophenone gives droperidol. [1]
Droperidol is used for:
Side effects of droperidol are:
Q.1 What can be the correct IUPAC nomenclature of Droperidol?
a) 3-[1-[4-(4-fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-benzimidazol-2-one
b) N,N-dimethyl-9-[3-(4-methylpiperazin-1-yl)propylidene]-9H-thioxanthene-2-sulfonic acid
c) 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine
d) N,N-dimethyl-3-phenothiazin-10-ylpropan-1-amine
Q.2 Which amongst the following statements is/are INCORRECT related to the SAR of Droperidol?
I. Electron donating group at the meta-position of the phenyl ring has highest potency.
II. Potency decreases on decreasing the propyl chain of butyrophenone.
III. Replacing the keto oxygen with sulfur, carbon or hydroxyl group increases the potency.
a) I, III
b) I, II
c) III
d) None
Q.3 Number of chiral carbons present in the structure of droperidol?
a) 0
b) 1
c) 2
d) 3
Q.4 Side effects of drug droperidol is/are?
a) Hypotension
b) Sedation
c) Prolongation of QT interval
d) All of the above
Q.5 Match the following drugs with their correct melting points:
i. Droperidol | A.190-206 oC |
ii. Oseltamivir | B. 74oC |
iii. Umifenovir | C. 148oC |
iv. Darunavir | D.133-137oC |
a) i-A, ii-C, iii-B, iv-D
b) i-C, ii-A, iii-D, iv-B
c) i-C, ii-A, iii-B, iv-D
d) i-B, ii-D, iii-A, iv-C
Q.6 An example of drug from class buterophenone antipsychotic drug is?
a) Droperidol
b) Chlorpromazine
c) Tiotixene
d) Both a) and c)
Q.7 The type of ring system found in droperidol?
a) Phenyl
b) Imidazole
c) Pyridine
d) All of the above
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1-a
2-c
3-a
4-d
5-b
6-a
7-d
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