The post AMPRENAVIR Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(3S)-oxolan-3-yl N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropyl)(4-aminobenzene)sulfonamido]-1-phenylbutan-2-yl]carbamate
Amprenavir is an HIV protease inhibitor.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 505.6 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | °C |
4 | Solubility | 40 mg/L in water |
5 | Octanol/water partition coefficient | log Kow = 2.2 at 25oC |
6 | Presence of ring | Furan, phenyl |
7 | Number of chiral centers | 3 |
i. Inhibition of HIV viral proteinase enzyme by amprenavir.
ii. Noninfectious, immature viral particles are produced.
Co-catalyzed stereo centered hydrolytic kinetic resolution of racemic 2-(1-azido-2-phenylethyl)oxirane as the chirality inducing step. There is also synthesis of (S)-3-hydroxytetrahydrofuran with 98% enantiomeric property.[2]
Side effects of Amprenavir are:
Q.1 What can be the brand name for drug Amprenavir?
a) Agenerase
b) Anethane
c) Xylocaine
d) Tricaine
Q.2 Which amongst the following statements is/are incorrect related to the SAR of amprenavir?
I. The receptors are bean shaped having a predominantly hydrophobic pocket in the upper half of the region with distinct ‘V’ shape.
II. The hydrophilic region is present at the periphery having H-bond acceptor rich area which can also accommodate a positive salt bridge in the form of terminal aromatic ring.
III. The bean shape structure of the inhibitor has a prominent H-bond acceptor region lies in the center depression.
IV. In the iomic or hydrophilic sites, ligands may form H-bonds with the active site of the receptor.
a) I, II
b) II, IV
c) III
d) None
Q.3 Type of ring present in the structure of Amprenavir?
I. Phenyl
II. Cyclopentane
III. Pyrimidine
IV. Furan
a) I, III
b) II, III
c) I, IV
d) II, IV
Q.4 Side effects of drug Amprenavir is/are?
a) Nausea
b) Vomitting
c) Diarrhea
d) All of the above
Q.5 Match the following drugs with their correct molecular weights-
i. Amprenavir | A. 226.27 gm/mol |
ii. Amobarbital | B. 294.27 gm/mol |
iii. Estazolam | C. 505.6 gm/mol |
iv. Quazepam | D. 386.6 gm/mol |
a) i-C, ii-A, iii-B, iv-D
b) i-D, ii-B, iii-C, iv-A
c) i-B, ii-A, iii-D, iv-C
d) i-A, ii-B, iii-C, iv-D
Q.6 An example of drug from class HIV protease inhibitor is?
a) Cytarabine
b) Methotraxate
c) Amprenavir
d) 5-FU
Q.7 Number of chiral centers present in the structure of Amprenavir?
a) 0
b) 1
c) 2
d) 3
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1-a
2-d
3-c
4-d
5-a
6-c
7-d
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