The post AUROTHIOGLUCOSE Synthesis, SAR, MCQ, Structure, Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>gold(1+);(3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxane-2-thiolate
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 392.18 g/mol |
2 | Physical appearance | Yellow crystals |
3 | Melting point | >107oC |
4 | Solubility | Soluble in water with decomposition; slightly soluble in propylene glycol; insoluble in acetone |
5 | Octanol/water partition coefficient | -2.50 (log Kow) |
6 | Presence of ring | Pyran |
7 | Number of chiral centers | 5 |
General SAR for Gold compounds DMARDs can be summarized as follows:
i. Addition of solution of gold bromide to the aqueous solution of thioglucose, containing sulfur dioxide.
ii. Precipitate can be obtained after heating solution and adding ethanol.[2]
Aurothioglucose is used for:
Side effects of Aurothioglucose are:
Q.1 Mechanism of action of Aurothioglucose is due to?
a) Inhibitting effect on the activity of adenyl cyclase in the human lymphocyte membrane and membrane of T and B lymphocytes
b) Inhibition of Acetylcholinestrase which hen results in the decrease in the level of acetylcholine at the synapse
c) Alkylation of the genetic material which help in killing the neoplastic cells
d) None of the above
Q.2 Therapeutic use of drug Aurothioglucose is/are?
a) Treatment of Rheumatoid arthritis
b) Treatment of malignant tumors
c) As an anesthetic agent
d) All of the above
Q.3 Which amongst the following are the correct statements with respect to the SAR of Gold compounds DMARDs?
I. Monovalent gold is less active than trivalent or colloidal gold.
II. Attachment of the gold with the sulfur containing ligand is essential for the activity of the drug.
III. Complexation of the gold ions with phosphine decreases the bioavailability.
IV. Injectible gold compounds should be monocoordinated.
a) I, II, III, IV
b) II, IV
c) I, III, IV
d) II, III
Q.4 Aurothioglucose can be synthesized by adding gold bromide to?
a) Dihydrofuran
b) Glycopyrrolate
c) Thioglucose
d) Both a) and c)
Q.5 Correct sequence for the True/False for the physiochemical properties of the drug Aurothioglucose?
a) TFFT
b) FFTF
c) TTFF
d) FFFF
Q.6 Correct statements for the IUPAC nomenclatures of the drugs are?
I. Aurothioglucose: gold(1+);(3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxane-2-thiolate
II. Carboplatin: (SP-4-2)-diamminedichloroplatinum(II)
III. Lopinavir: 1,4-dihydroxy-5,8-bis[2-(2-hydroxyethylamino)ethylamino]-anthracene-9,10-dione.
IV. Chloraquine: 2-amino-1H-purine-6(7H)-thione
a) I, II
b) II, III, IV
c) I, IV
d) I, II, III, IV
Q.7 Match the following drugs with their correct classifications-
i. Aurothioglucose | A. Benzodiazepine sedative hypnotic |
ii. Quazepam | B. DMARDs |
iii. Bisoprolol | C. Cholinergic agonist |
iv. Acetylcholine | D. ß-adrenergic antagonist |
a) i-A, ii-D, iii-B, iv-C
b) i-B, ii-A, iii-D, iv-C
c) i-B, ii-C, iii-A, iv-D
d) i-A, ii-B, iii-C, iv-D
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1-a
2-a
3-b
4-c
5-c
6-a
7-b
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