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Bioorg Med Chem Lett. 2006 Sep 1;16(17):4440-3. Epub 2006 Jun 30.

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

Author information

1
Division of Medicinal Chemistry, National Research Institute of Chinese Medicine, Taipei, Taiwan.

Abstract

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 (IC(50)'s for COX-1: 23.28 microM; COX-2: 2.04 microM), being active but less COX-2 selective than celecoxib.

PMID:
16814546
DOI:
10.1016/j.bmcl.2006.06.036
[Indexed for MEDLINE]

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