ALUMINA CATALYST: SYNTHESIS OF NOVEL QUINAZOLINE DE RIVATIVES AND THEIR SOLUBILITY INCREASES THROUGH INCLUSION WITH β-CYCLO DEXTRIN
By: Hossain, Mossaraf
.
Contributor(s): Nanda, Ashish Kumar.
Publisher: M P Innovare Academic Sciences Pvt Ltd 2019Edition: Vol.11(2).Description: 51-58p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
International journal of pharmacy and pharmaceutical scienceSummary: Objective:
To synthesis a novel methodology of bioactive quina
zoline derivatives under greener process to an exce
llent yields and increases their
solubility via inclusion with β-cyclodextrin (CD).
Methods:
Derivatives of quinazoline compounds were prepared
by the mixture of 3-amino-2-phenylquinazolin-4(3H)-
one, derived from 2-phenyl-
4H-benzo[1,3]oxazin-4-one by refluxing with hydrazi
ne, substituted aromatic aldehyde and alumina intim
ately in an agate mortar and pestle under
solvent-free condition. Using various techniques fo
r preparing inclusion complexes, kneaded method is
the best method for encapsulation in host-
guest complex chemistry. All compounds including in
clusion complexes were characterised by spectral me
thods.
Results:
Synthesized a series of novel quinazoline compounds
under a very easier greener process with a commerc
ially available reagent. However,
their low bioavailability, due to low absorption an
d solubility, can limit their potential application
s. CD was used to resolve this solubility problem.
CD can easily accommodated the guest molecules to e
ncapsulate inside its cavity due to interior the hy
drophobic nature with a hydrophilic exterior
part to form thermodynamically more stable molecula
r microcapsules, commonly name as host-guest comple
xes or inclusion complexes. In this
sense, CD was utilized to enhance not only the solu
bility and bioavailability of these quinazoline com
pounds but also their antibacterial capacity.
The formation of inclusion complex was thus confirm
ed by ultraviolet-visible spectroscopy (UV-VIS), Fo
urier Transform Infrared Spectrometry (FT-
IR), differential scanning calorimetry (DSC) and so
lubility study technique.
Conclusion:
Here we have successfully unfolded an eco-friendly
methodology for the synthesis of derivatives of qui
nazoline and increased their
solubility via host-guest inclusion technique. From
the spectral analysis, it was concluded that the q
uinazoline compound is fully encapsulated
inside the cavity of the CD.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2020888 |
Objective:
To synthesis a novel methodology of bioactive quina
zoline derivatives under greener process to an exce
llent yields and increases their
solubility via inclusion with β-cyclodextrin (CD).
Methods:
Derivatives of quinazoline compounds were prepared
by the mixture of 3-amino-2-phenylquinazolin-4(3H)-
one, derived from 2-phenyl-
4H-benzo[1,3]oxazin-4-one by refluxing with hydrazi
ne, substituted aromatic aldehyde and alumina intim
ately in an agate mortar and pestle under
solvent-free condition. Using various techniques fo
r preparing inclusion complexes, kneaded method is
the best method for encapsulation in host-
guest complex chemistry. All compounds including in
clusion complexes were characterised by spectral me
thods.
Results:
Synthesized a series of novel quinazoline compounds
under a very easier greener process with a commerc
ially available reagent. However,
their low bioavailability, due to low absorption an
d solubility, can limit their potential application
s. CD was used to resolve this solubility problem.
CD can easily accommodated the guest molecules to e
ncapsulate inside its cavity due to interior the hy
drophobic nature with a hydrophilic exterior
part to form thermodynamically more stable molecula
r microcapsules, commonly name as host-guest comple
xes or inclusion complexes. In this
sense, CD was utilized to enhance not only the solu
bility and bioavailability of these quinazoline com
pounds but also their antibacterial capacity.
The formation of inclusion complex was thus confirm
ed by ultraviolet-visible spectroscopy (UV-VIS), Fo
urier Transform Infrared Spectrometry (FT-
IR), differential scanning calorimetry (DSC) and so
lubility study technique.
Conclusion:
Here we have successfully unfolded an eco-friendly
methodology for the synthesis of derivatives of qui
nazoline and increased their
solubility via host-guest inclusion technique. From
the spectral analysis, it was concluded that the q
uinazoline compound is fully encapsulated
inside the cavity of the CD.
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