1,5-Diarylimidazoles with strong inhibitory activity against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells

A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells. Most of synthesized 1,5-diarylimidazoles exhibited strong inhibitory activities regardless of the pos...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (14), p.4035-4037
Main Authors: Che, Haiyan, Tuyen, Truong Ngoc, Kim, Hyun Pyo, Park, Haeil
Format: Article
Language:English
Subjects:
1,5-Diarylimidazoles
4-Methylsulfonylphenyl group
Animals
Anti-inflammatory activity
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Catalysis
Cell Line
COX-2 Inhibitors
Cyclooxygenase 2 Inhibitors - metabolism
Cyclooxygenase 2 Inhibitors - pharmacology
Dinoprostone - biosynthesis
Imidazoles - pharmacology
Lipopolysaccharides - pharmacology
Macrophages - drug effects
Macrophages - metabolism
Medical sciences
Mice
Pharmacology. Drug treatments
Prostaglandin production
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Summary:A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE2 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. A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE2 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.05.092