The post DEXTROPROPOXYPHENE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(1S,2R)-1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propionate
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 339.5 g/mol |
2 | Physical appearance | Forms crystals from petroleum ether |
3 | Melting point | 75.5°C |
4 | Solubility | 3.32 mg / L in water |
5 | Octanol/water partition coefficient | 4.18 |
6 | Presence of ring | Phenyl |
7 | Number of chiral centers | 2 |
SAR for Opiates can be summarized as follows:
i. Addition of the secondary amine to phenypropenyl ketone to give amino ketone called beta-dimethylaminobutrophenone.
ii. Grignard reaction of the amino ketone with benzylmagnesium chloride to yield the amino, hydrochloride-carbinols 4-Dimethylamino-1,2-diphenyl-3- methyl-2-butanol Hydrochloride.
iii. Acylation of the alpha-amino carbinol hydrochloride by addition of propionic anhydride and heating to reflux.[1]
Dextropropoxyphene is used for:
Side Effects
Side effects Dextropropoxyphene are:
Q.1 Choose the correct statements related with the physicochemical properties of drug Dextropropoxyphene.
I. Molecular weight = 339.5 gm/mol
II. It forms crystals in water
III. Melting point is 75.5oC
a) I, III
b) II
c) I
d) I, II
Q.2 Match the following of the drugs with their correct IUPAC names.
i. Dextropropoxyphene | A. (3-carbamoyloxy-2-phenylpropyl) carbamate
|
ii. Felbamate | B. 5-Ethyl-3-methyl-5-phenyl-imidazolidine-2,4-dione
|
iii. Mephenytoin | C. 5H-dibenzo[b,f]azepine-5-carboxamide
|
iv. Carbamazepine | D. (1S,2R)-1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propionate
|
a) i-C, ii-A, iii-B, iv-D
b) i-D, ii-A, iii-C, iv-B
c) i-D, ii-A, iii-B, iv-C
d) i-A, ii-C, iii-B, iv-D
Q.3 Dextropropoxyphene inhibits:
I. Exchange of GTP for GDP
II. Release of noradrenaline
III. Release of acetylcholine
IV. Release of Dopmaine
a) I , II, III, IV
b)II, III, IV
c) III , IV
d) IV
Q.4 Correct sequence for True/false for the classification of the drug can be?
a) TFFT
b) TTTT
c) TTFF
d) FFFF
Q.5 Find the correct statement amongst the following related with the SAR of Opiates?
a) Replacement of phenolic hydroxyl into –OCH3/-OC2H5 will make the drug less analgesic
b) Replacement of alcoholic hydroxyl with –OCH3 makes the compound less active.
c) Replacement of alcoholic hydroxyl with -OC2H5 makes the compound less active
d) Replacement of alcoholic hydroxyl with –OCOCH3 will also deactivates the compound
Q.6 Number of chiral carbons present in the structure of Dextropropoxyphene is?
a) 0
b) 1
c) 2
d) 3
Q.7 Side effect of drug Dextropropoxyphene include?
a) Fatal heart rhythm
b) Itching
c) Sore throat
d) All of the above
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1-a
2-c
3-b
4-b
5-a
6-c
7-d
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