Selective COX-2 inhibitors. Part 2: Synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides

Shwu Jiuan Lin, Wei Jern Tsai, Wen Fei Chiou, Tsang Hsiung Yang, Li Ming Yang

研究成果: 雜誌貢獻文章

25 引文 斯高帕斯(Scopus)

摘要

Two series of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamide derivatives were designed and synthesized for the evaluation as selective cyclooxygenase-2 (COX-2) inhibitors in a cellular assay using human whole blood (HWB). Extensive structure-activity relationships (SAR) were studied within these series. Several compounds were found to be novel and selective COX-2 inhibitors. Among them, the most potent and selective was 4-(3-carboxy-4-hydroxy-benzylideneamino)benzenesulfonamide (20, LA2135), (IC50's for COX-1: 85.13 μM; COX-2: 0.74 μM; SI: 114.5), being more active COX-2 selective than celecoxib.

原文英語
頁(從 - 到)2697-2706
頁數10
期刊Bioorganic and Medicinal Chemistry
16
發行號5
DOIs
出版狀態已發佈 - 三月 1 2008

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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