The post PHYSOSTIGMINE Synthesis, SAR, MCQ, Structure, Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 275.35 g/mol |
2 | Physical appearance | White microcrystalline powder |
3 | Melting point | 105.5oC |
4 | Solubility | Slightly soluble in water; very soluble in dichloromethane |
5 | Octanol/water partition coefficient | 1.58 |
6 | Presence of ring | Pyrrolo-pyrrole |
7 | Number of chiral centers | 2 |
General SAR for carbamates anticholinestrases can be summarized as follows:
i. p-ethoxymethylaniline is reacted with α-bromopropionyl bromide in the presence of aluminum chloride to give 1,3-dimethyl-5-ethoxyindolin-2-one.
ii. The above formed compound is reacted with chloroacetonitrile in the presence of sodium ethoxide to give 1,3-dimethyl-5-ethoxy-3-canomethylindolin-2-one.
iii. On resucing the amine group which is later methoxided produces 1,3-dimethyl-5ethoxy-3-(ß-methylaminoethyl)indolin-2-one.
iv. Reduction of the carbonyl group to give an aminoalcohol
v. On dehydration of the aminoalcohol, 1,3a,8-trimethyl-2,3,3a,8a-tetrahydrophyrrolo[2,3b]-5-ethoxyindol is produced.
vi. By the help of hydrogen bromide, the ethoxyprotecting group is removed to give a compound with a phenolhydroxyl group.
vii. On reaction of the above formed compound with methylisocyanate yields physostigmine.[2]
Physostigmine is used for:
Side effects of physostigmine are:
Q.1 Match the following with correct SAR of the class Carbamates cholinestrases-
i. Replacement of the xanthone nucleus with other aryl groups | A. Increases the AChE activity |
ii. Replacement of the flexible chain f the drug with rigid alkyne chain | B. Decreases the AChE activity |
C. leads to loss of activity | |
D. leads to a compound with higher AChE activity |
a) i-A, ii-C
b) i-A, ii-D
c) i-B, ii-C
d) i-B, ii-D
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
b) FFFF
c) TTTT
d) TFFT
Q.3 Molecular weight of drug Physostigmine is?
a) 275.35 gm/mol
b) 154.28 gm/mol
c) 406.21 gm/mol
d) 162.1 gm/mol
Q.4 Physostigmine mechanism of action includes?
a) It inhibits Acetylcholinestrase enzyme
b) The level of acetylcholine at the synapse decreases
c) It exerts effect on COX-1 and on COX-2
d) All of the above
Q.5 Which amongst the following is a therapeutic use of drug Physostigmine?
a) Treatment of Glaucoma
b) Reducing pain due to arthritis
c) Controlling vomiting
d) All of the above
Q.6 Which of the following drug and their classification are correct?
I. Physostigmine: NSAID
II. Vinblastin: Propionic acid derivative
III. Enflurane: Inhalational anesthetics
IV. Alprazolem: Benzodiazepine sedative-hypnotic
a) III, IV
b) I, II, III
c) I, II, III, IV
d) II
Q.7 Number of chiral carbons resent in the structure of Physostigmine is?
a) 4
b) 2
c) 1
d) 0
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1-d
2-c
3-c
4-a
5-a
6-a
7-b
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