期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 14, 页码 4035-4037出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.05.092
关键词
1,5-Diarylimidazoles; Prostaglandin production; COX-2 Inhibitors; Anti-inflammatory activity; 4-Methylsulfonylphenyl group
A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE(2) production from LPS-induced RAW 264.7 cells. Most of synthesized 1,5-diarylimidazoles exhibited strong inhibitory activities regardless of the position of the 4-methylsulfonylphenyl group. The 1,5-diarylimidazoles with a halogen atom (3c-3h, 3n-3p) gave mostly excellent inhibitory activities regardless of the position and species of the halogen atom. Whereas the 1,5-diarylimidazoles with two fluorine atoms (3k, 3l, 3r, 3s) showed rather reduced inhibitory activities. (C) 2010 Elsevier Ltd. All rights reserved.
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