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Selective COX-2 inhibitors. Part 2: Synthesis and biological evaluation of 4-benzylideneamino- and 4-phenyliminomethyl-benzenesulfonamides by Shwu-Jiuan Lin; Wei-Jern Tsai; Wen-Fei Chiou; Tsang-Hsiung Yang; Li-Ming Yang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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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), (IC 50 's for COX-1: 85.13 lM; COX-2: 0.74 lM; SI: 114.5), being more active COX-2 selective than celecoxib.

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Author

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

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2008

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)