Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.

@article{Tsai2006SelectiveCI,
  title={Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.},
  author={W J Tsai and Y. S. Shiao and Shwu-Jiuan Lin and Wen-fei Chiou and Lie-Chwen Lin and Tsang-Hsiung Yang and C F Teng and Tain-Shung Wu and Li-ming Yang},
  journal={Bioorganic & medicinal chemistry letters},
  year={2006},
  volume={16 17},
  pages={4440-3}
}
A series of phenylazobenzenesulfonamide derivatives were designed and synthesized for the evaluation as selective cyclooxygenase-2 (COX-2) inhibitors in a cellular assay using human whole blood (HWB) and an enzymatic assay using purified ovine enzymes. Extensive structure-activity relationships (SAR) were studied within this series, and several of selective COX-2 inhibitors have been identified. Among them, compound 8, 4-(4-amino-2-methylsulfanyl-phenylazo)benzenesulfonamide, showed a potent… CONTINUE READING

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