Dhokale, Sandhya R. <br/><br/>
SYNTHESIS, SCREENING OF NOVEL 1-SUBSTITUTED-3-(4-OX O-2-PHENYLQUINAZOLIN- 3(4H)-YL) UREA AND THIOUREA ANALOGUES AS POTENT ANT IBACTERIALS  

 - Vol.11(11) 
 - M P  Innovare Academic Sciences Pvt Ltd  2019 
 - 38-42p. 
<br/><br/> Objective: <br/>The proposed study is an attempt to determine antib<br/>acterial activity of synthesized novel 1-substitute<br/>d-3-(4-oxo-2-phenylquinazolin-<br/>3(4H)-yl) urea and thiourea analogues as potent anti<br/>bacterials against <br/>S. aureus <br/>and <br/>E. coli <br/>bacteria. <br/>Methods: <br/>The  present study  reports  new series of  1-substitut<br/>ed-3-(4-oxo-2-phenylquinazolin-3(4H)-yl) urea  and  t<br/>hiourea  derivatives  as  potent <br/>antibacterial  agents.  Reagents  used  in  the  present <br/>study  were  of  synthetic  grade  and  solvents  were  use<br/>d  after  distillation.  Novel  quinazolinone <br/>analogues  were  synthesized  by  considering  substitut<br/>ion  pattern,  characterization  of  the  synthesized  an<br/>alogues  was  performed  using  various <br/>techniques  like Thin  layer chromatography,  Melting <br/>point,  Infrared  spectroscopy,  Proton  NMR  spectromet<br/>ry and  Mass spectrometry.  TLC  of  the <br/>synthesized analogues was carried out by using (tol<br/>uene: methanol in the ratio 2:1), melting point was<br/> found by open capillary method, IR spectrum <br/>was  recorded  on  JASCO  V-530,  1H  NMR  was  recorded  on <br/>Bruker  Avance  Spectrometer  and  Mass  spectra  were  ob<br/>tained  from  G6460A,  triple <br/>quadrupole/MS/MS system. <br/>In vitro <br/>antibacterial activity was performed against <br/>S. aureus and E. coli.<br/>Results: <br/>Six derivatives of quinazolinone analogues were syn<br/>thesized. The structures of 1-substituted-3-(4-oxo-<br/>2-phenylquinazolin-3(4H)-yl) urea <br/>and  thiourea  derivatives  were  confirmed  by  physical<br/>  and  spectral  analysis.  Synthesized  molecules  showe<br/>d <br/>Rf<br/>  of  0.45-0.80  in  toluene:  methanol <br/>mobile  phase,  melting  point  was  carried  out  by open<br/>  capillary  method  and  were  in  range  of  90-210  °  C, <br/>IR  spectrum  was  recorded  in  range  of <br/>14000-400 cm<br/>-1<br/>and  showed characteristic  peaks of NH  and of C-O-NH,<br/>  1H  NMR of  the  compounds  was  distinct  to confirm  st<br/>ructures with  delta <br/>values  in  the  range  of  7.53-11.960,  Mass  spectra  pr<br/>oved  parent  peaks  of  synthesized  compounds confirmi<br/>ng  molecular  weight.  The  compounds <br/>were assayed for antibacterial activity against <br/>S. aureus <br/>and<br/> E. coli <br/>using ciprofloxacin as standard. The synthesized an<br/>alogues have shown good <br/>yield and comparable antibacterial 
<br/><br/><label>Subjects--Topical Terms: </label><br/>PHARMACEUTICS