Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.

@article{AbdelAziz2016DesignSO,
  title={Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies.},
  author={A. A. Abdel-Aziz and L. Abou-zeid and K. Eltahir and M. Mohamed and M. A. Abu El-Enin and A. El-Azab},
  journal={Bioorganic & medicinal chemistry},
  year={2016},
  volume={24 16},
  pages={
          3818-28
        }
}
A new series, 2-substituted mercapto-3-[2-(pyridin-2-yl)ethyl]-4(3H)-quinazolinone 1-21, was synthesized and evaluated for in vivo anti-inflammatory and analgesic activities and in vitro COX-1/COX-2 inhibition. Compounds 1, 4, 5, 6, 8, 10, 13, 14, 15, 16, and 17 exhibited potent anti-inflammatory and analgesic properties, with ED50 values of 50.3-112.1mg/kg and 12.3-111.3mg/kg, respectively. These values may be compared with those of diclofenac sodium (ED50=112.2 and 100.4mg/kg) and celecoxib… Expand
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References

SHOWING 1-10 OF 36 REFERENCES
Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors.
  • 114
Novel 4(3H)-quinazolinone analogs: synthesis and anticonvulsant activity
  • 36
...
1
2
3
4
...