24313-72-2Relevant academic research and scientific papers
Selective COX-2 inhibitors. Part 2: Synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides
Lin, Shwu-Jiuan,Tsai, Wei-Jern,Chiou, Wen-Fei,Yang, Tsang-Hsiung,Yang, Li-Ming
, p. 2697 - 2706 (2008/09/21)
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.
