Synthesis, Cyclooxygenase Inhibition, Anti-Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5-Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore.

@article{Abdellatif2016SynthesisCI,
  title={Synthesis, Cyclooxygenase Inhibition, Anti-Inflammatory Evaluation, and Ulcerogenic Liability of New 1,3,5-Triarylpyrazoline Derivatives Possessing a Methanesulfonyl Pharmacophore.},
  author={Khaled R A Abdellatif and Wael A. A. Fadaly and Amany A. Azouz},
  journal={Archiv der Pharmazie},
  year={2016},
  volume={349 10},
  pages={801-807}
}
A new series of 1,3,5-triarylpyrazolines 13a-l was synthesized and all prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and in vivo anti-inflammatory activity. All test compounds were more selective for the COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 13h was the most COX-2 selective compound (COX-2 selectivity index (SI) = 10.23) and the most potent anti-inflammatory derivative (ED50  = 60.1 µmol/kg) in comparison with celecoxib… CONTINUE READING