Objective:
The proposed study is an attempt to determine antib
acterial activity of synthesized novel 1-substitute
d-3-(4-oxo-2-phenylquinazolin-
3(4H)-yl) urea and thiourea analogues as potent anti
bacterials against
S. aureus
and
E. coli
bacteria.
Methods:
The present study reports new series of 1-substitut
ed-3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea and t
hiourea derivatives as potent
antibacterial agents. Reagents used in the present
study were of synthetic grade and solvents were use
d after distillation. Novel quinazolinone
analogues were synthesized by considering substitut
ion pattern, characterization of the synthesized an
alogues was performed using various
techniques like Thin layer chromatography, Melting
point, Infrared spectroscopy, Proton NMR spectromet
ry and Mass spectrometry. TLC of the
synthesized analogues was carried out by using (tol
uene: methanol in the ratio 2:1), melting point was
found by open capillary method, IR spectrum
was recorded on JASCO V-530, 1H NMR was recorded on
Bruker Avance Spectrometer and Mass spectra were ob
tained from G6460A, triple
quadrupole/MS/MS system.
In vitro
antibacterial activity was performed against
S. aureus and E. coli.
Results:
Six derivatives of quinazolinone analogues were syn
thesized. The structures of 1-substituted-3-(4-oxo-
2-phenylquinazolin-3(4H)-yl) urea
and thiourea derivatives were confirmed by physical
and spectral analysis. Synthesized molecules showe
d
Rf
of 0.45-0.80 in toluene: methanol
mobile phase, melting point was carried out by open
capillary method and were in range of 90-210 ° C,
IR spectrum was recorded in range of
14000-400 cm
-1
and showed characteristic peaks of NH and of C-O-NH,
1H NMR of the compounds was distinct to confirm st
ructures with delta
values in the range of 7.53-11.960, Mass spectra pr
oved parent peaks of synthesized compounds confirmi
ng molecular weight. The compounds
were assayed for antibacterial activity against
S. aureus
and
E. coli
using ciprofloxacin as standard. The synthesized an
alogues have shown good
yield and comparable antibacterial