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]]>2,2′-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropanenitrile).
Anastrozole is an aromatase inhibitor. [1]
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 293.4 g/mol |
2 | Appearance | Off white powder form |
3 | Melting point | 82°C |
4 | Solubility | 0.53mg/ml in water |
5 | Octanol/water partition coefficient | 1.58 |
6 | Presence of ring | Aryl and triazole ring present |
7 | Number of chiral centers | Not present |
i. Aromatase enzymes are competitively inhibited by the drug.
ii. This leads to prevention of conversion of androgens to estrogen.
iii. Due to reduced availability of estrogen, estrogen –dependent tumors regress.
i. 3,5-bis(bromomethyl)toluene undergoes SN2 displacement reaction using potassium nitrile and tetrabutylammonium bromide as a phase transfer catalyst to give bis-nitrile compound.
ii. Bis-nitrile compound formed undergoes deprotonation with NaH and methylated afterwards with methyl iodide to give bis-dimethyated product.
iii. Product undergoes radical substitution reaction following the Wohl-Ziegler reaction using N-bromosuccinamide and benzoyl peroxide as the radical initiator.
iv. In the final step, benzylbromide undergoes SN2 displacement with sodium triazole to give anastrozole.
The drug used for the treatment of:
Q.1 What can be the correct IUPAC nomenclature of Anastrozole?
a) 2,2′-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropanenitrile)
b) 2,2′-phenylene]bis(2-methylpropanenitrile)
c) 5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]bis(2-methylpropanenitrile)
d) 2,2′-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Anastrozole?
I. Carbonyl groups are not necessary for the activity of drug.
II. Substitutions at C-6 and C-7 positions can increase the aromatase inhibition property.
III. Extend and conjugate the number of double bonds in convenient positions of A and B rings of the steroid at positions C-1, C-4 and C-6 can decrease the potency of the drug.
a) I
b) I & II
c) I & III
d) I, II & III
Q.3 The correct order for the mechanism of action of Anastrozole can be?
I. Regress in estrogen receptor positive tumors.
II. Reduction in the conversion of androgens to estrogen.
III. Competitive inhibition of aromatase enzyme.
a) III – I – II
b) I – III – II
c) III – II – I
d) I – II – III
Q.4 The drug Anastrozole is mainly used for the treatment of?
a) Chronic obstructive pulmonary disease
b) Neuromascular disorder
c) Siezures
d) Breast cancer
Q.5 Match the drugs with the correct classification.
i. Triptorelin | A. GnRH analogues |
ii. Bicalutamide | B. Antiandrogens |
iii. Anastrozole | C. Aromatase inhibitors |
iv. Dactinomycin | D. Antibiotics |
a) i-A, ii-D, iii-C, iv-B
b) i-D, ii-B, iii-C, iv-A
c) i-A, ii-B, iii-C, iv-D
d) i-D, ii-C, iii-B, iv-A
Q.6 How many statements below are true with respect to the side effects of the drug Anastrozole?
a) 1
b) 2
c) 3
d) 4
Q.7 The type of ring system found in Anastrozole is?
a) Triazole ring
b) Pteridine ring
c) Oxazophospharine ring
d) None of the above
1-a
2-c
3-c
4-d
5-c
6-d
7-a
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