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

…, WJ Tsai, WF Chiou, TH Yang, LM Yang

Index: Lin, Shwu-Jiuan; Tsai, Wei-Jern; Chiou, Wen-Fei; Yang, Tsang-Hsiung; Yang, Li-Ming Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 5 p. 2697 - 2706

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Citation Number: 19

Abstract

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 ...