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

Wei Jern Tsai, Young Ji Shiao, Shwu Jiuan Lin, Wen Fei Chiou, Lie Chwen Lin, Tsang Hsiung Yang, Che Ming Teng, Tain Shung Wu, Li Ming Yang

研究成果: Article同行評審

44 引文 斯高帕斯(Scopus)

摘要

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 inhibitory activity to the cyclooxygenase enzymes (IC50's for COX-1: 23.28 μM; COX-2: 2.04 μM), being active but less COX-2 selective than celecoxib.

原文English
頁(從 - 到)4440-4443
頁數4
期刊Bioorganic and Medicinal Chemistry Letters
16
發行號17
DOIs
出版狀態Published - 2006 9月 1

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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