期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 17, 页码 4440-4443出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.06.036
关键词
anti-inflammatory; selective COX-2 inhibitors; phenylazobenzenesulfonamide; resveratrol; isosterism; SAR
A series of phenylazobenzenesulfonamide derivatives were designed and synthesized for the evaluation as selective cyclo-oxygenase-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 (IC50's for COX-1: 23.28 mu M; COX-2: 2.04 mu M), being active but less COX-2 selective than celecoxib. (c) 2006 Elsevier Ltd. All rights reserved.
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